Piperidinyl targeting compounds that selectively bind integrins

Abstract

The present invention relates to the synthesis and biological application of piperidinoyl carboxylic acid integrin antagonists affinity moiety of IFormula (I): and Formula (II): These affinity moieties maybe used with imaging agents or liposomes to target cells that express the α v β 3 , α v β 5 , or α v β 6 integrin receptors.

What is claimed is:  
     
         1 . A targeting ligand having a formula selected from the group consisting of Formula (I):  
       
         
           
           
               
               
           
         
       
       wherein 
 W is selected from the group consisting of —C 0-6 alkyl(R 1 ), —C 1-6 alkyl(R 1a ), —C 0-6 alkyl-aryl(R 1 ,R 8 ), —C 0-6 alkyl-heterocyclyl(R 1 ,R 8 ), —C 0-6 alkoxy(R 1 ), —C 0-6 alkoxy-aryl(R 1 ,R 8 ), and —C 0-6 alkoxy-heterocyclyl(R 1 ,R 8 );  
 R 1  is selected from the group consisting of hydrogen, —N(R 4 ) 2 , —N(R 4 )(R 5 ), —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) and -heteroaryl(R 8 );  
 R 1a  is selected from the group consisting of —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ) and —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is selected from the group consisting of hydrogen and —C 1-8 alkyl(R 7 );  
 R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 9 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-8 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) and —SO 2 -aryl(R 8 );  
 R 6  is selected from the group consisting of -cycloalkyl(R 8 ), -heterocyclyl(R 8 ), -aryl(R 8 ) and -heteroaryl(R 8 );  
 R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-8 alkoxy(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-C 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl-NH—C 1-8 alkyl(R 9 ), —SO 2 -C 1-8 -alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo) 1-3 , hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 );  
 R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 1a ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), -cycloalkyl(R 10 ) and -aryl(R 10 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C 1-8 alkoxy(R 9 ), —O-cycloalkyl(R 1a ), —O-aryl(R 1a ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —NHC(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 1a ), —NHC(═O)—NH 2 , —NHC(═O)—NH—C 1-8 alkyl(R 9 ), —NHC(═O)—N(C 1-8 alkyl(R 9 )) 2 , —NHC(═O)—NH-aryl(R 1a ), —NHC(═O)—O—C 1-8 alkyl(R 9 ), —NHC(═O)—O-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —NHC(═O)-cycloalkyl(R 10 ), —NHC(═O)-heterocyclyl(R 10 ), —NHC(═O)-aryl(R 1a ), —NHC(═O)-heteroaryl(R 1a ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 1a ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(RP a), —NHSO 2 —C 1-8 alkyl(R 9 ), —NHSO 2 -aryl(R 1a ), —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-C 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl-NH—C 1-8 alkyl(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ), and -heteroaryl(R 10 ) when attached to a carbon atom;  
 R 9  is selected from the group consisting of hydrogen, —C 1-8 alkoxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-8 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro and oxo;  
 R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl and —SO 2 —N(C 1-8 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl, —C 1-8 alkoxy, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom;  
 q is 0, 1, 2, or 3;  
 R 2a  is selected from the group consisting of —C 1-8 alkyl(R 7 )(R 11 ), —C 2-8 alkenyl(R 7 )(R 11 ), —C 2-8 alkynyl(R 7 )(R 11 ), -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ) and -heteroaryl(R 8 )(R 12 );  
 R 11  is selected from the group consisting of —C 1-8 alkyl(R 14 ), —O—C 1-8 alkyl(R 14 ), —NH—C 1-8 alkyl(R 14 ), —S—C 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —C(═O)OC 1-8 alkyl(R 14 ), —C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)OC 1-8 alkyl(R 14 ), —O—C(═O)NHC 1-8 alkyl(R 14 ), —NH—C(═O)OC 1-8 alkyl(R 14 ), —NH—C(═O)NHC 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkylC(═O)(R 14 ), —O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)C 1-8 alkylC(═O)(R 14 ), —C(═O)OC 1-8 alkylC(═O)(R 14 ), —O—C(═O)OC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 14 ), —C(═O)NHC 1-8 alkylC(═O)(R 14 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 );  
 R 12  is selected from the group consisting of —C 1-8 alkyl(R 14 ), —O—C 1-8 alkyl(R 14 ), —NH—C 1-8 alkyl(R 14 ), —S—C 1-8 alkyl(R 14 ), —CH 2 O—C 1-8 alkyl(R 14 ), —CH 2 NH—C 1-8 alkyl(R 14 ), —CH 2 S—C 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —CH 2 O—C(═O)C 1-8 alkyl(R 14 ), —CH 2 NH—C(═O)C 1-8 alkyl(R 14 ), —C(═O)OC 1-8 alkyl(R 14 ), —C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)OC 1-8 alkyl(R 14 ), —O—C(═O)NHC 1-8 alkyl(R 14 ), —NH—C(═O)OC 1-8 alkyl(R 14 ), —NH—C(═O)NHC 1-8 alkyl(R 14 ), —CH 2 O—C(═O)OC 1-8 alkyl(R 14 ), —CH 2 O—C(═O)NHC 1-8 alkyl(R 14 ), —CH 2 NH—C(═O)OC 1-8 alkyl(R 14 ), —CH 2 NH—C(═O)NHC 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkylC(═O)(R 14 ), —O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)C 1-8 alkylC(═O)(R 14 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 14 ), —CH 2 NH—C(═O)C 1-8 alkylC(═O)(R 14 ), —C(═O)OC 1-8 alkylC(═O)(R 14 ), —O—C(═O)OC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 14 ), —CH 2 O—C(═O)OC 1-8 alkylC(═O)(R 14 ), —CH 2 NH—C(═O)OC 1-8 alkylC(═O)(R 14 ), —C(═O)NHC 1-8 alkylC(═O)(R 14 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 H 2 C(R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 H 2 (R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 H 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2  SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2  SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 C(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 C(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 H 2 CO) r CH 2 C(═O)(R 14 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 );  
 R 14  when R 11  and R 12  terminates with a C(═O) is selected from the group consisting of hydrogen, OH, —OC 1-4 alkyl and NH 2 ; otherwise R 14  is selected from the group consisting of —OH, —SH, COOH, and —COOC 1-4 alkyl;  
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-8 alkoxy, —O—C 1-8 alkylcarbonylC 1-8 alkyl, —O—C 8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-8 alkyl, —O—C 1-8 alkyl-O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide, —O—C 1-8 alkyl-C(O)—NH—C 8 alkyl, —O—C 1-8 alkyl-C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl;  
 and pharmaceutically acceptable salts, racemic mixtures and enantiomers thereof.  
 
     
     
         2 . The targeting ligand of  claim 1  wherein W is selected from the group consisting of —C 0-4 alkyl(R 1 ) and —C 0-4 alkyl-aryl(R 1 ,R 8 ).  
     
     
         3 . The targeting ligand of  claim 1  wherein W is —C 0-4 alkyl(R 1 ) or —C 0-4 alkyl-phenyl(R 1 ,R 8 ).  
     
     
         4 . The targeting ligand of  claim 1  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) and -heteroaryl(R 8 ).  
     
     
         5 . The targeting ligand of  claim 1  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -dihydro-1H-pyrrolo[2,3-b]pyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ), -tetrahydro-1,8-naphthyridinyl(R 8 ), -tetrahydro-1H-azepino[2,3-b]pyridinyl(R 8 ) and -pyridinyl(R 8 ).  
     
     
         6 . The targeting ligand of  claim 1  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -tetrahydropyrimidinyl(R 8 ) and -tetrahydro-1,8-naphthyridinyl(R 8 ).  
     
     
         7 . The targeting ligand of  claim 1  wherein R 1a  is selected from the group consisting of —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) and —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 .  
     
     
         8 . The targeting ligand of  claim 1  wherein R 4  is selected from the group consisting of hydrogen and —C 1-4 alkyl(R 7 ).  
     
     
         9 . The targeting ligand of  claim 1  wherein R 4  is hydrogen.  
     
     
         10 . The targeting ligand of  claim 1  wherein R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 8 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 9 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-4 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) and —SO 2 -aryl(R 8 ).  
     
     
         11 . The targeting ligand of  claim 1  wherein R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —CO 2 —R 4 , —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —SO 2 —C 1-4 alkyl(R 7 ) and —SO 2 —N(R 4 ) 2 .  
     
     
         12 . The targeting ligand of  claim 1  wherein R 6  is selected from the group consisting of -heterocyclyl(R 8 ) and -heteroaryl(R 8 ).  
     
     
         13 . The targeting ligand of  claim 1  wherein R 6  is selected from the group consisting of -dihydroimidazolyl(R 8 ), -tetrahydropyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ) and -pyridinyl(R 8 ).  
     
     
         14 . The targeting ligand of  claim 1  wherein R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl-NH—C 1-4 alkyl(R 9 ), —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo) 1-3 , hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 ).  
     
     
         15 . The targeting ligand of  claim 1  wherein R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , (halo) 1-3 , hydroxy and oxo.  
     
     
         16 . The targeting ligand of  claim 1  wherein R 7  is hydrogen.  
     
     
         17 . The targeting ligand of  claim 1  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), -cycloalkyl(R 10 ) and -aryl(R 10 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-cycloalkyl(R 10 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl-R 11 ) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl-NH—C 1-4 alkyl(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 ) when attached to a carbon atom.  
     
     
         18 . The targeting ligand of  claim 1  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ) and —SO 2 —NH 2  when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         19 . The targeting ligand of  claim 1  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen and —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , halo, hydroxy and oxo when attached to a carbon atom.  
     
     
         20 . The targeting ligand of  claim 1  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen and —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ) and hydroxy when attached to a carbon atom.  
     
     
         21 . The targeting ligand of  claim 1  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro and oxo.  
     
     
         22 . The targeting ligand of  claim 1  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —CO 2 H, —C(═O)—C 1-4 alkoxy, (halo) 1-3 , hydroxy and oxo.  
     
     
         23 . The targeting ligand of  claim 1  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , (halo) 1-3  and hydroxy.  
     
     
         24 . The targeting ligand  claim 1  wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl and —SO 2 —N(C 1-4 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         25 . The targeting ligand of  claim 1  wherein (R 10 ) 14  is selected from the group consisting of hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —CO 2 H, —CO 2 —C 1-4 alkyl, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         26 . The targeting ligand of  claim 1  wherein R 10  is hydrogen.  
     
     
         27 . The targeting ligand of  claim 1  wherein R 2a  is selected from the group consisting of —C 1-4 alkyl (R 7 )(R 11 ), —C 2-4 alkenyl(R 7 )(R 11 ), —C 2-4 alkynyl(R 7 )(R 11 ), -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 12 ).  
     
     
         28 . The targeting ligand of  claim 1  wherein R 2a  is selected from the group consisting of -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 11 ).  
     
     
         29 . The targeting ligand of  claim 1  wherein R 2a  is selected from the group consisting of -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 11 ).  
     
     
         30 . The targeting ligand  claim 1  wherein R 2a  is selected from the group consisting of -tetrahydropyrimidinyl(R 8 )(R 12 ), -1,3-benzodioxolyl(R 8 )(R 12 ), -dihydrobenzofuranyl(R 8 )(R 12 ), -tetrahydroquinolinyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), -pyridinyl(R 8 )(R 12 ), -pyrimidinyl(R 8 )(R 12 ), and -quinolinyl(R 8 )(R 12 ).  
     
     
         31 . The targeting ligand of  claim 1  wherein R 11  is selected from the group consisting of —C 1-8 alkyl(R 14 ), —O—C 1-8 alkyl(R 14 ), —NH—C 1-8 alkyl(R 14 ), —S—C 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —C(═O)OC 1-8 alkyl(R 14 ), —C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)OC 1-8 alkyl(R 14 ), —O—C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)C 1-8 alkylC(═O)(R 14 ), —C(═O)OC 1-8 alkylC(═O)(R 14 ), —O—C(═O)OC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 14 ), —C(═O)NHC 1-8 alkylC(═O)(R 14 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ).  
     
     
         32 . The targeting ligand of  claim 1  wherein R 11  is selected from the group consisting of —C 1-8 alkyl(R 14 ), —O—C 1-8 alkyl(R 14 ), —NH—C 1-8 alkyl(R 14 ), —S—C 1-8 alkyl(R 14 ), —C(═O)C 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —C(═O)OC 1-8 alkyl(R 14 ), —C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)OC 1-8 alkyl(R 14 ), —O—C(═O)NHC 1-8 alkyl(R 14 ), —O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)C 1-8 alkylC(═O)(R 14 ), —C(═O)OC 1-8 alkylC(═O)(R 14 ), —O—C(═O)OC 1-8 alkylC(═O)(R 14 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 14 ), —C(═O)NHC 1-8 alkylC(═O)(R 14 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), and —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ).  
     
     
         33 . The targeting ligand of  claim 1  wherein R 12  is selected from the group consisting of —C 1-6 alkyl(R 14 ), —O—C 1-6 alkyl(R 14 ), —NH—C 4 alkyl(R 14 ), —S—C 1-6 alkyl(R 14 ), —CH 2 O—C 1-6 alkyl(R 14 ), —CH 2 NH—C 1-6 alkyl(R 14 ), —CH 2 S—C 1-6 alkyl(R 14 ), —C(═O)C 1-6 alkyl(R 14 ), —O—C(═O)C 1-6 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —CH 2 O—C(═O)C 1-8 alkyl(R 14 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 14 ), —C(═O)OC 1-6 alkyl(R 14 ), —C(═O)NHC 1-6 alkyl(R 14 ), —O—C(═O)OC 1-6 alkyl(R 14 ), —O—C(═O)NHC 1-6 alkyl(R 14 ), —NH—C(═O)OC 1-6 alkyl(R 14 ), —NH—C(═O)NHC 1-6 alkyl(R 14 ), —NH—C(═O)C 1-6 alkylC(═O)(R 14 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ).  
     
     
         34 . The targeting ligand of  claim 1  wherein q is 1, 2 or 3.  
     
     
         35 . The targeting ligand  claim 1  wherein Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-4 alkoxy, —O—C 1-8 alkylcarbonylC 1-4 alkyl, —O—C 1-8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-6 alkyl, C 1-8 alkyl-OC(O)—C 1-6 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide, C 1-8 alkyl-C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl-C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl.  
     
     
         36 . The targeting ligand of  claim 1  wherein the targeting ligand is conjugated to an radioactive element.  
     
     
         37 . The targeting ligand of  claim 1  wherein the targeting ligand is conjugated to an imagining agent.  
     
     
         38 . The targeting ligand of  claim 37  wherein the imagining agent is selected from the group consisting of  99 Tc,  125 I,  18 F,  11 C, and  64 Cu.  
     
     
         39 . A targeting ligand of Formula (I):  
       
         
           
           
               
               
           
         
       
       wherein 
 W is selected from the group consisting of —C 0-4 alkyl(R 1 ) and —C 0-4 alkyl-phenyl(R 1 ,R 8 );  
 R 1  is —NH(R 6 );  
 R 2a  is selected from the group consisting of -tetrahydropyrimidinyl(R 8 )(R 12 ), -1,3-benzodioxolyl(R 8 )(R 12 ), -dihydrobenzofuranyl(R 8 )(R 12 ), -tetrahydroquinolinyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), -pyridinyl(R 8 )(R 12 ), -pyrimidinyl(R 8 )(R 12 ), and -quinolinyl(R 8 )(R 12 ).  
 R 6  is selected from the group consisting of -dihydroimidazolyl(R 8 ), -tetrahydropyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ) and -pyridinyl(R 8 );  
 R 8  is one to four substituents independently selected from the group consisting of hydrogen and —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ) and hydroxy when attached to a carbon atom;  
 R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , (halo) 1-3  and hydroxy;  
 R 10  is independently selected from the group consisting of hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —CO 2 H, —CO 2 —C 1-4 alkyl, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , halo, hydroxy, nitro and oxo when attached to a carbon atom;  
 q is 1, 2 or 3;  
 R 12  is selected from the group consisting of —C 1-6 alkyl(R 14 ), —O—C 1-6 alkyl(R 14 ), —NH—C 1-4 alkyl(R 14 ), —S—C 1-6 alkyl(R 14 ), —CH 2 O—C 1-6 alkyl(R 14 ), —CH 2 NH—C 1-6 alkyl(R 14 ), —CH 2 S—C 1-6 alkyl(R 14 ), —C(═O)C 1-6 alkyl(R 14 ), —O—C(═O)C 1-6 alkyl(R 14 ), —NH—C(═O)C 1-8 alkyl(R 14 ), —CH 2 O—C(═O)C 1-8 alkyl(R 14 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 14 ), —C(═O)OC 1-6 alkyl(R 14 ), —C(═O)NHC 1-6 alkyl(R 14 ), —O—C(═O)OC 1-6 alkyl(R 14 ), —O—C(═O)NHC 1-6 alkyl(R 14 ), —NH—C(═O)OC 1-6 alkyl(R 14 ), —NH—C(═O)NHC 1-6 alkyl(R 14 ), —NH—C(═O)C 1-6 alkylC(═O)(R 14 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 14 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 H 2 O) r CH 2 CH 2 (R 14 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 H 2 C(R 14 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 14 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 14 );  
 R 14  when R 11  and R 12  terminates with a C(═O) is selected from the group consisting of hydrogen, OH, —OC 1-4 alkyl and NH 2 ; otherwise R 14  is selected from the group consisting of —OH, —SH, COOH, and —COOC 1-4 alkyl; 
 Z is slected from the group consisting hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-8 alkoxy, —O—C 1-8 alkylcarbonylC 1-8 alkyl, —O—C 1-8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-8 alkyl, —O—C 1-8 alkyl-O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 8 alkylamide, —O—C 1-8 alkyl-C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl-C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl;  
 
 and pharmaceutically acceptable salts, racemic mixtures and enantiomers thereof.  
 
     
     
         40 . A targeting conjugate having a formula selected from the group consisting of  
       
         
           
           
               
               
           
         
       
       and Formula (II):  
       wherein 
 W is selected from the group consisting of —C 0-6 alkyl(R 1 ), —C 1-6 alkyl(R 1a ), —C 0-6 alkyl-aryl(R 1 ,R 8 ), —C 0-6 alkyl-heterocyclyl(R 1 ,R 8 ), —C 0-6 alkoxy(R 1 ), —CO 0-6 alkoxy-aryl(R 1 ,R 8 ), and —C 0-6 alkoxy-heterocyclyl(R 1 ,R 8 );  
 R 1  is selected from the group consisting of hydrogen, —N(R 4 ) 2 , —N(R 4 )(R 5 ), —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) and -heteroaryl(R 8 );  
 R 1a  is selected from the group consisting of —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ) and —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is selected from the group consisting of hydrogen and —C 1-8 alkyl(R 7 );  
 R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 9 ), —C(═O)—N(R 4 )-aryl(R 8 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-8 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) and —SO 2 -aryl(R 8 );  
 R 6  is selected from the group consisting of -cycloalkyl(R 8 ), -heterocyclyl(R 8 ), -aryl(R 8 ) and -heteroaryl(R 8 );  
 R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-8 alkoxy(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-C 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl-NH—C 1-8 alkyl(R 9 ), —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo)-3, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 );  
 R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(RP a), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), -cycloalkyl(R 10 ) and -aryl(R 10 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C 1-8 alkoxy(R 9 ), —O-cycloalkyl(R 1a ), —O-aryl(R 1a ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —NHC(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —NHC(═O)—NH 2 , —NHC(═O)—NH—C 1-8 alkyl(R 9 ), —NHC(═O)—N(C 1-8 alkyl(R 9 )) 2 , —NHC(═O)—NH-aryl(R 1a ), —NHC(═O)—O—C 1-8 alkyl(R 9 ), —NHC(═O)—O-aryl(R 1a ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 1a ), —C(═O)-aryl(R 1a ), —C(═O)-heteroaryl(R 1a ), —NHC(═O)-cycloalkyl(R 10 ), —NHC(═O)-heterocyclyl(R 10 ), —NHC(═O)-aryl(R 10 ), —NHC(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 1a ), —NHSO 2 —C 1-8 alkyl(R 9 ), —NHSO 2 -aryl(R 10 ), —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl-C 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl-NH—C 1-8 alkyl(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ), and -heteroaryl(R 10 ) when attached to a carbon atom;  
 R 9  is selected from the group consisting of hydrogen, —C 1-8 alkoxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-8 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro and oxo;  
 R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl and —SO 2 —N(C 1-8 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl, —C 1-8 alkoxy, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom;  
 q is 0, 1, 2, or 3;  
 R 2a  is selected from the group consisting of —C 1-8 alkyl(R 7 )(R 11 ), —C 2-8 alkenyl(R 7 )(R 11 ), —C 2-8 alkynyl(R 7 )(R 1 ), -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ) and -heteroaryl(R 8 )(R 12 );  
 R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —NH—C(═O)OC 1-8 alkyl(R 13 ), —NH—C(═O)NHC 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkylC(═O)(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 R 12  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —CH 2 O—C 1-8 alkyl(R 13 ), —CH 2 NH—C 1-8 alkyl(R 13 ), —CH 2 S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —NH—C(═O)OC 1-8 alkyl(R 13 ), —NH—C(═O)NHC 1-8 alkyl(R 13 ), —CH 2 O—C(═O)OC 1-8 alkyl(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)OC 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkylC(═O)(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 C(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 C(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 C(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                                                                                                                                   
  wherein the unit —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 750 to 5000 daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of 
 the C 11  saturated chain of lauric acid,  
 the C 13  saturated chain of myristoic acid,  
 the C 15  saturated chain of palmitoic acid,  
 the C 17  saturated chain of stearoic acid,  
 the C 17  mono-unsaturated chain of oleoic acid, and  
 the C 17  di-unsaturated chain of linoleic acid;  
 
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-8 alkoxy, O—C 1-8 alkylcarbonylC 1-8 alkyl, —O—C 1-8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-8 alkyl, —O—C 1-8 alkyl-O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide, —O—C 1-8 alkyl-C(O)—NH—C 1-8 alkyl, O—C 8 alkyl-C(O)—N(C 1-8 alkyl) 2 , and —NHC(O)C 1-8 alkyl; 
 and pharmaceutically acceptable salts, racemic mixtures and enantiomers thereof.  
 
 
     
     
         41 . The targeting conjugate of  claim 40  wherein W is selected from the group consisting of —C 0-4 alkyl(R 1 ) and —C 0-4 alkyl-aryl(R 1 ,R 8 ).  
     
     
         42 . The targeting conjugate of  claim 40  wherein W is —C 0-4 alkyl(R 1 ) or —C 0-4 alkyl-phenyl(R 1 ,R 8 ).  
     
     
         43 . The targeting conjugate of  claim 40  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) and -heteroaryl(R 9 ).  
     
     
         44 . The targeting conjugate of  claim 40  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -dihydro-1H-pyrrolo[2,3-b]pyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ), -tetrahydro-1,8-naphthyridinyl(R 8 ), -tetrahydro-1H-azepino[2,3-b]pyridinyl(R 8 ) and -pyridinyl(R 8 ).  
     
     
         45 . The targeting conjugate of  claim 40  wherein R 1  is selected from the group consisting of —N(R 4 )(R 6 ), -tetrahydropyrimidinyl(R 8 ) and -tetrahydro-1,8-naphthyridinyl(R 8 ).  
     
     
         46 . The targeting conjugate of  claim 40  wherein R 1a  is selected from the group consisting of —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) and —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 .  
     
     
         47 . The targeting conjugate of  claim 40  wherein R 4  is selected from the group consisting of hydrogen and —C 1-4 alkyl(R 7 ).  
     
     
         48 . The targeting conjugate of  claim 40  wherein R 4  is hydrogen.  
     
     
         49 . The targeting conjugate of  claim 40  wherein R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 9 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 9 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-4 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) and —SO 2 -aryl(R 8 ).  
     
     
         50 . The targeting conjugate of  claim 40  wherein R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —CO 2 —R 4 , —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —SO 2 —C 1-4 alkyl(R 7 ) and —SO 2 —N(R 4 ) 2 .  
     
     
         51 . The targeting conjugate of  claim 40  wherein R 6  is selected from the group consisting of -heterocyclyl(R 8 ) and -heteroaryl(R 8 ).  
     
     
         52 . The targeting conjugate of  claim 40  wherein R 6  is selected from the group consisting of -dihydroimidazolyl(R 8 ), -tetrahydropyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ) and -pyridinyl(R 8 ).  
     
     
         53 . The targeting conjugate of  claim 40  wherein R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl-NH—C 1-4 alkyl(R 9 ), —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo) 1-3 , hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 ).  
     
     
         54 . The targeting conjugate of  claim 40  wherein R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , (halo) 13 , hydroxy and oxo.  
     
     
         55 . The targeting conjugate of  claim 40  wherein R 7  is hydrogen.  
     
     
         56 . The targeting conjugate of  claim 40  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—C 4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), -cycloalkyl(R 10 ) and -aryl(R 10 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-cycloalkyl(R 10 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl-R 11 ) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 1a ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl-NH—C 1-4 alkyl(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 ) when attached to a carbon atom.  
     
     
         57 . The targeting conjugate of  claim 40  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ) and —SO 2 —NH 2  when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         58 . The targeting conjugate of  claim 40  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen and —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 1a ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , halo, hydroxy and oxo when attached to a carbon atom.  
     
     
         59 . The targeting conjugate of  claim 40  wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen and —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ) and hydroxy when attached to a carbon atom.  
     
     
         60 . The targeting conjugate of  claim 40  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro and oxo.  
     
     
         61 . The targeting conjugate of  claim 40  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —CO 2 H, —C(═O)—C 1-4 alkoxy, (halo) 1-3 , hydroxy and oxo.  
     
     
         62 . The targeting conjugate of  claim 40  wherein R 9  is selected from the group consisting of hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , (halo) 1-3  and hydroxy.  
     
     
         63 . The targeting conjugate  claim 40  wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl and —SO 2 —N(C 1-4 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         64 . The targeting conjugate of  claim 40  wherein (R 10 ) 1-4  is selected from the group consisting of hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —CO 2 H, —CO 2 —C 1-4 alkyl, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , halo, hydroxy, nitro and oxo when attached to a carbon atom.  
     
     
         65 . The targeting conjugate of  claim 40  wherein R 10  is hydrogen.  
     
     
         66 . The targeting conjugate of  claim 40  wherein R 2a  is selected from the group consisting of —C 1-4 alkyl (R 7 )(R 11 ), —C 2-4 alkenyl(R 7 )(R 11 ), —C 2-4 alkynyl(R 7 )(R 11 ), -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 12 ).  
     
     
         67 . The targeting conjugate of  claim 40  wherein R 2a  is selected from the group consisting of -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 11 ).  
     
     
         68 . The targeting conjugate of  claim 40  wherein R 2a  is selected from the group consisting of -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), and -heteroaryl(R 8 )(R 11 ).  
     
     
         69 . The targeting conjugate  claim 40  wherein R 2a  is selected from the group consisting of -tetrahydropyrimidinyl(R 8 )(R 12 ), -1,3-benzodioxolyl(R 8 )(R 12 ), -dihydrobenzofuranyl(R 8 )(R 12 ), -tetrahydroquinolinyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), -pyridinyl(R 8 )(R 12 ), -pyrimidinyl(R 8 )(R 12 ), and -quinolinyl(R 8 )(R 12 ).  
     
     
         70 . The targeting conjugate of  claim 40  wherein R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 H 2 O) r CH 2 C(═O)(R 13 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ).  
     
     
         71 . The targeting conjugate of  claim 40  wherein R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), and —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ).  
     
     
         72 . The targeting conjugate of  claim 40  wherein R 12  is selected from the group consisting of —C 1-6 alkyl(R 13 ), —O—C 1-6 alkyl(R 13 ), —NH—C 1-4 alkyl(R 13 ), —S—C 1-6 alkyl(R 13 ), —CH 2 O—C 1-8 alkyl(R 13 ), —CH 2 NH—C 1-6 alkyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —C(═O)C 1-6 alkyl(R 13 ), —O—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —C(═O)OC 1-6 alkyl(R 13 ), —C(═O)NHC 1-6 alkyl(R 13 ), —O—C(═O)OC 1-6 alkyl(R 13 ), —O—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)OC 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 22 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
       wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
       
         
           
           
               
               
           
         
       
       and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         73 . The targeting conjugate of  claim 40  wherein R 12  is selected from the group consisting of —CH 2 O—C 1-6 alkyl(R 13 ), —CH 2 NH—C 1-6 alkyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ).  
       wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
       
         
           
           
               
               
           
         
       
       and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         74 . The targeting conjugate of  claim 40  wherein said —O—(CH 2 CH 2 O—) p — or  
       
         
           
           
               
               
           
         
       
       of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 2000 to 5000 daltons.  
     
     
         75 . The targeting conjugate of  claim 40  wherein wherein Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of the C 1-5  saturated chain of palmitoic acid, 
 the C 1-7  saturated chain of stearoic acid, and the C 17  mono-unsaturated chain of oleoic acid.  
 
     
     
         76 . The targeting conjugate of  claim 40  wherein 
 W is preferably is selected from the group consisting of —C 0-4 alkyl(R 1 ), —C 1-4 alkyl(R 1a ), —C 0-4 alkyl-aryl(R 1 ,R 8 ), —C 0-4 alkyl-heterocyclyl(R 1 ,R 8 ), —C 0-4 alkoxy(R 1 ), —C 0-4 alkoxy-aryl(R 1 ,R 8 ), and —C 0-4 alkoxy-heterocyclyl(R 1 ,R 8 );  
 R 1  is —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) or -heteroaryl(R 8 );  
 R 1a  is —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) or —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is hydrogen or —C 1-4 alkyl(R 7 );  
 R 5  is —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 8 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-4 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) or —SO 2 -aryl(R 8 );  
 R 6  is -heterocyclyl(R 8 ) or -heteroaryl(R 8 );  
 R 7  is one to two substituents independently selected from hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl-C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl-NH—C 1-4 alkyl(R 9 ), —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo)-3, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) or -heteroaryl(R 10 );  
 R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ) or —SO 2 —NH 2  when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro or oxo when attached to a carbon atom;  
 R 9  is hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro or oxo;  
 R 10  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl or —SO 2 —N(C 1-4 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , cyano, halo, hydroxy, nitro or oxo when attached to a carbon atom;  
 R 2a  is -cycloalkyl(R 8 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ) or -heteroaryl(R 8 )(R 12 );  
 q is 1, 2 or 3.  
 R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 R 12  is selected from the group consisting of —C 1-6 alkyl(R 13 ), —O—C 1-6 alkyl(R 13 ), —NH—C 1-4 alkyl(R 13 ), —S—C 1-6 alkyl(R 13 ), —CH 2 O—C 1-6 alkyl(R 13 ), —CH 2 NH—C 1-6 alkyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —C(═O)C 16 alkyl(R 13 ), —O—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —C(═O)OC 1-6 alkyl(R 13 ), —C(═O)NHC 1-6 alkyl(R 13 ), —O—C(═O)OC 1-6 alkyl(R 13 ), —O—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)OC 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R) 3), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     
  and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                       
 said —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 750 to 5000 daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of  
 the C 11  saturated chain of lauric acid,  
 the C 15  saturated chain of palmitoic acid,  
 the C 17  saturated chain of stearoic acid,  
 the C 17  mono-unsaturated chain of oleoic acid, and  
 the C 17  di-unsaturated chain of linoleic acid;  
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-4 alkoxy, —O—C 1-8 alkylcarbonylC 1-4 alkyl, —O—C 1-8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-6 alkyl, —O—C 1-8 alkyl-O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide —O—C 1-8 alkyl-C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl-C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl.  
 
     
     
         77 . The targeting conjugate of  claim 40  wherein 
 W is preferably —C 0-4 alkyl(R 1 ) or —C 0-4 alkyl-phenyl(R 1 ,R 8 );  
 R 1  is —N(R 4 )(R 6 ), -tetrahydropyrimidinyl(R 8 ) or -tetrahydro-1,8-naphthyridinyl(R 8 );  
 R 1a  is —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) or —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is hydrogen;  
 R 5  is —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —CO 2 —R 4 , —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —SO 2 —C 1-4 alkyl(R 7 ) or —SO 2 —N(R 4 ) 2 ;  
 R 6  is -dihydroimidazolyl(R 8 ), -tetrahydropyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ) or -pyridinyl(R 8 );  
 R 7  is hydrogen;  
 R 8  is one to four substituents independently selected from hydrogen or —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 )-O-aryl(R 10 ) or hydroxy when attached to a carbon atom;  
 R 9  is hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , (halo) 1-3  or hydroxy;  
 R 10  is hydrogen;  
 R 2a  is -tetrahydropyrimidinyl(R 8 )(R 12 ), -1,3-benzodioxolyl(R 8 )(R 12 ), -dihydrobenzofuranyl(R 8 )(R 12 ), -tetrahydroquinolinyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), -pyridinyl(R 8 )(R 12 ), -pyrimidinyl(R 8 )(R 12 ) or -quinolinyl(R 8 )(R 12 );  
 q is 1 or 2;  
 R 12  is selected from the group consisting of  
 —CH 2 —O—(CH 2 ) 4 (R 13 )—,  
 —CH 2 —NH—(CH 2 ) 4 (R 13 )—,  
 —CH 2 —S—(CH 2 ) 4 (R 13 )—,  
 —CH 2 —O—(CH 2 ) 6 (R 13 )—,  
 —CH 2 —NH—(CH 2 ) 6 (R 13 )—,  
 —CH 2 —S—(CH 2 ) 6 (R 13 )—,  
 —NH—C(═O)—(CH 2 ) 4 (R 13 )—,  
 —NH—C(═O)—(CH 2 ) 7 (R 13 )—,  
 —NH—C(═O)NH—(CH 2 ) 3 (R 13 )—,  
 —NH—C(═O)NH—(CH 2 ) 6 (R 13 )—,  
 —CH 2 NH—C(═O)NH—(CH 2 ) 2 (R 13 )—,  
 —CH 2 NH—C(═O)NH—(CH 2 ) 5 (R 13 )—,  
 —NHC(═O)—(CH 2 ) 2 —C(═O)(R 13 )—,  
 —NHC(═O)—(CH 2 ) 3 —C(═O)(R 13 )—,  
 —NHC(═O)—(CH 2 ) 4 —C(═O)(R 13 )—,  
 —OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —NHCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —NHCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —OCH 2 CH 2 OCH 2 C(═O)(R 13 )—,  
 —OCH 2 CH 2 OCH 2 CH 2 OCH 2 C(═O)(R 13 )—,  
 —NHC(═O)CH 2 OCH 2 CH 2 (R 13 )—,  
 —NHC(═O)CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 NHCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 SCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 NHCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 SCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—,  
 —CH 2 NHC(═O)CH 2 OCH 2 C(═O)(R 13 )—, and  
 —NHC(═O)CH 2 OCH 2 C(═O)(R 13 )—;  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of                          
 wherein said —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer selected from 2000 (PEG 2000), 3400 (PEG  3400 ), or 5000 (PEG 5000) Daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and is the C 1-7  saturated chain of stearoic acid;  
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl-OH, —O—C 1-8 alkylC 1-4 alkoxy, —O—C 1-8 alkylcarbonylC 1-4 alkyl, —O—C 1-8 alkyl-CO 2 H, —O—C 1-8 alkyl-C(O)O—C 1-6 alkyl, —O—C 1-8 alkyl-O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl-NH 2 , —O—C 1-8 alkyl-NH—C 1-8 alkyl, —O—C 1-8 alkyl-N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide —O—C 1-8 alkyl-C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl-C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl.  
 
     
     
         78 . A therapeutic liposome composition sensitized to a target cell, comprising 
 (i) a liposomal composition composed of pre-formed liposomes having an entrapped therapeutic agent; and    (ii) a plurality of targeting conjugates, each conjugate composed of (a) a lipid having a polar head group and a hydrophobic tail, (b) a hydrophilic polymer having a proximal end and a distal end, where the polymer is attached at its proximal end to the head group of the lipid, and (c) a targeting ligand attached to the distal end of the polymer.    
     
     
         79 . The liposome of  claim 78  wherein the targeting conjugate has a formula selected from the group consisting of Formula (I):  
       
         
           
           
               
               
           
         
       
       wherein 
 W is selected from the group consisting of —C 0-6 alkyl(R 1 ), —C 1-6 alkyl(R 1a ), —C 0-6 alkyl-aryl(R 1 ,R 8 ), —C 0-6 alkyl-heterocyclyl(R 1 ,R 8 ), —C 0-6 alkoxy(R 1 ), —C 0-6 alkoxy-aryl(R 1 ,R 8 ), and —C 0-6 alkoxy-heterocyclyl(R 1 ,R 8 );  
 R 1  is selected from the group consisting of hydrogen, —N(R 4 ) 2 , —N(R 4 )(R 5 ), —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) and -heteroaryl(R 8 );  
 R 1a  is selected from the group consisting of —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ) and —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is selected from the group consisting of hydrogen and —C 1-8 alkyl(R 7 );  
 R 5  is selected from the group consisting of —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 8 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-8 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-8 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) and —SO 2 -aryl(R 8 );  
 R 6  is selected from the group consisting of -cycloalkyl(R 8 ), -heterocyclyl(R 8 ), -aryl(R 8 ) and -heteroaryl(R 8 );  
 R 7  is one to two substituents independently selected from the group consisting of hydrogen, —C 1-8 alkoxy(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl—S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl—C 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl—NH—C 1-8 alkyl(R 9 ), —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo) 1-3 , hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) and -heteroaryl(R 10 );  
 R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), -cycloalkyl(R 10 ) and -aryl(R 10 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl(R 9 ), —C 1-8 alkoxy(R 9 ), —O-cycloalkyl(R 10 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—C 1-8 alkyl(R 9 ), —NHC(═O)—C 1-8 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl(R 9 ), —C(═O)—N(C 1-8 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —NHC(═O)—NH 2 , —NHC(═O)—NH—C 1-8 alkyl(R 9 ), —NHC(═O)—N(C 1-8 alkyl(R 9 )) 2 , —NHC(═O)—NH-aryl(R 10 ), —NHC(═O)—O—C 1-8 alkyl(R 9 ), —NHC(═O)—O-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —NHC(═O)-cycloalkyl(R 10 ), —NHC(═O)-heterocyclyl(R 10 ), —NHC(═O)-aryl(R 10 ), —NHC(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-8 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SO 2 —C 1-8 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl(R 9 ), —SO 2 —N(C 1-8 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), —NHSO 2 —C 1-8 alkyl(R 9 ), —NHSO 2 -aryl(R 10 ), —SH, —S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkyl—S—C 1-8 alkyl(R 9 ), —S—C 1-8 alkylC 1-8 alkoxy(R 9 ), —S—C 1-8 alkyl—NH—C 1-8 alkyl(R 9 ), —NH 2 , —NH—C 1-8 alkyl(R 9 ), —N(C 1-8 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ), and -heteroaryl(R 10 ) when attached to a carbon atom;  
 R 9  is selected from the group consisting of hydrogen, —C 1-8 alkoxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-8 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro and oxo;  
 R 10  is one to four substituents independently selected from the group consisting of hydrogen, C 1-8 alkyl, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl and —SO 2 —N(C 1-8 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from the group consisting of hydrogen, —C 1-8 alkyl, —C 1-8 alkoxy, —C(═O)H, —C(═O)—C 1-8 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-8 alkyl, —C(═O)—N(C 1-8 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-8 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-8 alkyl, —SO 2 —N(C 1-8 alkyl) 2 , —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , cyano, halo, hydroxy, nitro and oxo when attached to a carbon atom;  
 q is 0, 1, 2, or 3;  
 R 2a  is selected from the group consisting of —C 1-8 alkyl(R 7 )(R 11 ), —C 2-8 alkenyl(R 7 )(R 11 ), —C 2-8 alkynyl(R 7 )(R 11 ), -cycloalkyl(R 7 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ) and -heteroaryl(R 8 )(R 12 );  
 R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —NH—C(═O)OC 1-8 alkyl(R 13 ), —NH—C(═O)NHC 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkylC(═O)(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(RI 3 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 R 12  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —CH 2 O—C 1-8 alkyl(R 13 ), —CH 2 NH—C 1-8 alkyl(R 13 ), —CH 2 S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —NH—C(═O)OC 1-8 alkyl(R 13 ), —NH—C(═O)NHC 1-8 alkyl(R 13 ), —CH 2 O—C(═O)OC 1-8 alkyl(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)OC 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkylC(═O)(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                                                           
 wherein the unit —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 750 to 5000 daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of 
 the C 11  saturated chain of lauric acid,  
 the C 13  saturated chain of myristoic acid,  
 the C 15  saturated chain of palmitoic acid,  
 the C 17  saturated chain of stearoic acid,  
 the C 17  mono-unsaturated chain of oleoic acid, and  
 the C 17  di-unsaturated chain of linoleic acid;  
 
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl—OH, —O—C 1-8 alkylC 1-8 alkoxy, O—C 1-8 alkylcarbonylC 1-8 alkyl, —O—C 1-8 alkyl—CO 2 H, —O—C 1-8 alkyl—C(O)O—C 1-8 alkyl, O—C 1-8 alkyl—O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl—NH 2 , —O—C 1-8 alkyl—NH—C 1-8 alkyl, O—C 1-8 alkyl—N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide, —O—C 1-8 alkyl—C(O)—NH—C 1-8 alkyl, O—C 1-8 alkyl—C(O)—N(C 1-8 alkyl) 2 , and —NHC(O)C 1-8 alkyl;  
 and pharmaceutically acceptable salts, racemic mixtures and enantiomers thereof.  
 
     
     
         80 . The liposome of  claim 79  wherein R 12  is selected from the group consisting of —C 1-6 alkyl(R 13 ), —O—C 1-6 alkyl(R 13 ), —NH—C 1-4 alkyl(R 13 ), —S—C 1-6 alkyl(R 13 ), —CH 2 O—C 1-6 alkyl(R 13 ), —CH 2 NH—C 1-6 alkyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —C(═O)C 1-6 alkyl(R 13 ), —O—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —C(═O)OC 1-6 alkyl(R 13 ), —C(═O)NHC 1-6 alkyl(R 13 ), —O—C(═O)OC 1-6 alkyl(R 13 ), —O—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)OC 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ); 
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                       
 
     
     
         81 . The liposome of  claim 79  wherein R 12  is selected from the group consisting of —CH 2 O—C 1-6 alkyl(R 13 ), —CH 2 NH—C 1-6 akyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ). 
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                       
 
     
     
         82 . The liposome of  claim 79  wherein said —O—(CH 2 CH 2 O—) p — or  
       
         
           
           
               
               
           
         
       
       of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 2000 to 5000 daltons.  
     
     
         83 . The liposome of  claim 79  wherein wherein Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of the C 15  saturated chain of palmitoic acid, the C 17  saturated chain of stearoic acid, and the C 17  mono-unsaturated chain of oleoic acid.  
     
     
         84 . The liposome of  claim 79  wherein 
 W is preferably is selected from the group consisting of —C 0-4 alkyl(R 1 ), —C 1-4 alkyl(R 1a ), —C 0-4 alkyl-aryl(R 1 ,R 8 ), —C 0-4 alkyl-heterocyclyl(R 1 ,R 8 ), —C 0-4 alkoxy(R 1 ), —C 0-4 alkoxy-aryl(R 1 ,R 8 ), and —C 0-4 alkoxy-heterocyclyl(R 1 ,R 8 );  
 R 1  is —N(R 4 )(R 6 ), -heterocyclyl(R 8 ) or -heteroaryl(R 8 );  
 R 1a  is —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) or —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is hydrogen or —C 1-4 alkyl(R 7 );  
 R 5  is —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —C(═O)-cycloalkyl(R 8 ), —C(═O)-heterocyclyl(R 8 ), —C(═O)-aryl(R 8 ), —C(═O)-heteroaryl(R 8 ), —C(═O)—N(R 4 )-cycloalkyl(R 8 ), —C(═O)—N(R 4 )-aryl(R 8 ), —CO 2 —R 4 , —CO 2 -cycloalkyl(R 8 ), —CO 2 -aryl(R 8 ), —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ), —N(R 4 )—C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 , —SO 2 —C 1-4 alkyl(R 7 ), —SO 2 —N(R 4 ) 2 , —SO 2 -cycloalkyl(R 8 ) or —SO 2 -aryl(R 8 );  
 R 6  is -heterocyclyl(R 8 ) or -heteroaryl(R 8 );  
 R 7  is one to two substituents independently selected from hydrogen, —C 1-4 alkoxy(R 9 ), —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , —C(═O)H, —C(═O)—C 1-4 alkyl(R 9 ), —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —C(═O)—NH-aryl(R 10 ), —C(═O)-cycloalkyl(R 10 ), —C(═O)-heterocyclyl(R 10 ), —C(═O)-aryl(R 10 ), —C(═O)-heteroaryl(R 10 ), —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —CO 2 -aryl(R 10 ), —C(═NH)—NH 2 , —SH, —S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl—S—C 1-4 alkyl(R 9 ), —S—C 1-4 alkyl—C 1-4 alkoxy(R 9 ), —S—C 1-4 alkyl—NH—C 1-4 alkyl(R 9 ), —SO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl(R 9 ), —SO 2 —N(C 1-4 alkyl(R 9 )) 2 , —SO 2 -aryl(R 10 ), cyano, (halo) 1-3 , hydroxy, nitro, oxo, -cycloalkyl(R 10 ), -heterocyclyl(R 10 ), -aryl(R 10 ) or -heteroaryl(R 10 );  
 R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ) or —SO 2 —NH 2  when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 ), —O-aryl(R 10 ), —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl(R 9 ), —C(═O)—N(C 1-4 alkyl(R 9 )) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl(R 9 ), —SO 2 —NH 2 , —NH 2 , —NH—C 1-4 alkyl(R 9 ), —N(C 1-4 alkyl(R 9 )) 2 , cyano, halo, hydroxy, nitro or oxo when attached to a carbon atom;  
 R 9  is hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , —C(═O)H, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , cyano, (halo) 1-3 , hydroxy, nitro or oxo;  
 R 10  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl or —SO 2 —N(C 1-4 alkyl) 2  when attached to a nitrogen atom; and, wherein R 10  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl, —C 1-4 alkoxy, —C(═O)H, —C(═O)—C 1-4 alkyl, —C(═O)—NH 2 , —C(═O)—NH—C 1-4 alkyl, —C(═O)—N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 —C 1-4 alkyl, —SO 2 —C 1-4 alkyl, —SO 2 —NH 2 , —SO 2 —NH—C 1-4 alkyl, —SO 2 —N(C 1-4 alkyl) 2 , —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , cyano, halo, hydroxy, nitro or oxo when attached to a carbon atom;  
 R 2a  is -cycloalkyl(R 8 )(R 11 ), -heterocyclyl(R 8 )(R 12 ), -aryl(R 8 )(R 12 ) or -heteroaryl(R 8 )(R 12 );  
 q is 1, 2 or 3.  
 R 11  is selected from the group consisting of —C 1-8 alkyl(R 13 ), —O—C 1-8 alkyl(R 13 ), —NH—C 1-8 alkyl(R 13 ), —S—C 1-8 alkyl(R 13 ), —C(═O)C 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —C(═O)OC 1-8 alkyl(R 13 ), —C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)OC 1-8 alkyl(R 13 ), —O—C(═O)NHC 1-8 alkyl(R 13 ), —O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)C 1-8 alkylC(═O)(R 13 ), —C(═O)OC 1-8 alkylC(═O)(R 13 ), —O—C(═O)OC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)OC 1-8 alkylC(═O)(R 13 ), —C(═O)NHC 1-8 alkylC(═O)(R 13 ), —O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —C(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 R 12  is selected from the group consisting of —C 1-6 alkyl(R 13 ), —O—C 1-6 alkyl(R 13 ), —NH—C 1-4 alkyl(R 13 ), —S 1-6 alkyl(R 13 ), —CH 2 O—C 1-6 alkyl(R 13 ), —CH 2 NH—C 1-6 alkyl(R 13 ), —CH 2 S—C 1-6 alkyl(R 13 ), —C(═O)C 1-6 alkyl(R 13 ), —O—C(═O)C 1-6 alkyl(R 13 ), —NH—C(═O)C 1-8 alkyl(R 13 ), —CH 2 O—C(═O)C 1-8 alkyl(R 13 ), —CH 2 NH—C(═O)C 1-6 alkyl(R 13 ), —C(═O)OC 1-6 alkyl(R 13 ), —C(═O)NHC 1-6 alkyl(R 13 ), —O—C(═O)OC 1-6 alkyl(R 13 ), —O—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)OC 1-6 alkyl(R 13 ), —NH—C(═O)NHC 1-6 alkyl(R 13 ), —NH—C(═O)C 1-6 alkylC(═O)(R 13 ), —CH 2 O—C(═O)C 1-8 alkylC(═O)(R 13 ), —NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 O—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —CH 2 NH—C(═O)NHC 1-8 alkylC(═O)(R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 CH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —SO 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 SCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 CH 2 (R 13 ), —CH 2 OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —OC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 OC(═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NH(C═O)CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), —CH 2 NHC(═O)OCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 ), and —CH 2 NHC(═O)NHCH 2 CH 2 O(CH 2 CH 2 O) r CH 2 C(═O)(R 13 );  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                                       
 said —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer ranging in molecular weight from 750 to 5000 daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and are selected from the group consisting of 
 the C 11  saturated chain of lauric acid,  
 the C 15  saturated chain of palmitoic acid,  
 the C 17  saturated chain of stearoic acid,  
 the C 17  mono-unsaturated chain of oleoic acid, and  
 the C 17  di-unsaturated chain of linoleic acid;  
 
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl—OH, —O—C 1-8 alkyl 1-4 alkoxy, —O—C 1-8 alkylcarbonylC 1-4 alkyl, —O—C 1-8 alkyl—CO 2 H, —O—C 1-8 alkyl—C(O)O—C 1-6 alkyl, —O—C 1-8 alkyl—O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl—NH 2 , —O—C 1-8 alkyl—NH—C 1-8 alkyl, —O—C 1-8 alkyl—N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide—O—C 1-8 alkyl—C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl—C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl.  
 
     
     
         85 . The liposome of  claim 79  wherein 
 W is preferably —C 0-4 alkyl(R 1 ) or —C 0-4 alkyl—phenyl(R 1 ,R 8 );  
 R 1  is —N(R 4 )(R 6 ), -tetrahydropyrimidinyl(R 8 ) or -tetrahydro- 1 , 8 -naphthyridinyl(R 8 );  
 R 1a  is —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —C(═N—R 4 )—N(R 4 )—C(═O)—R 4 , —C(═N—R 4 )—N(R 4 )—C(═O)—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )—CO 2 —R 4 , —C(═N—R 4 )—N(R 4 )—SO 2 —C 1-4 alkyl(R 7 ) or —C(═N—R 4 )—N(R 4 )—SO 2 —N(R 4 ) 2 ;  
 R 4  is hydrogen;  
 R 5  is —C(═O)—R 4 , —C(═O)—N(R 4 ) 2 , —CO 2 —R 4 , —C(R 4 )(═N—R 4 ), —C(═N—R 4 )—N(R 4 ) 2 , —C(═N—R 4 )—N(R 4 )(R 6 ), —N(R 4 )—C(R 4 )(═N—R 4 ), —N(R 4 )—C(═N—R 4 )—N(R 4 ) 2 , —N(R 4 )—C(═N—R 4 )—N(R 4 )(R 6 ), —SO 2 —C 1-4 alkyl(R 7 ) or —SO 2 —N(R 4 ) 2 ;  
 R 6  is -dihydroimidazolyl(R 8 ), -tetrahydropyridinyl(R 8 ), -tetrahydropyrimidinyl(R 8 ) or -pyridinyl(R 8 );  
 R 7  is hydrogen;  
 R 8  is one to four substituents independently selected from hydrogen or —C 1-4 alkyl(R 9 ) when attached to a nitrogen atom; and, wherein R 8  is one to four substituents independently selected from hydrogen, —C 1-4 alkyl(R 9 ), —C 1-4 alkoxy(R 9 )—O-aryl(R 10 ) or hydroxy when attached to a carbon atom;  
 R 9  is hydrogen, —C 1-4 alkoxy, —NH 2 , —NH—C 1-4 alkyl, —N(C 1-4 alkyl) 2 , (halo) 1-3 , or hydroxy;  
 R 10  is hydrogen;  
 R 2a  is -tetrahydropyrimidinyl(R 8 )(R 12 ), - 1 , 3 -benzodioxolyl(R 8 )(R 12 ), -dihydrobenzofuranyl(R 8 )(R 12 ), -tetrahydroquinolinyl(R 8 )(R 12 ), -phenyl(R 8 )(R 12 ), -naphthalenyl(R 8 )(R 12 ), -pyridinyl(R 8 )(R 12 ), -pyrimidinyl(R 8 )(R 12 ) or -quinolinyl(R 8 )(R 12 );  
 q is 1 or 2;  
 R 12  is selected from the group consisting of —CH 2 —O—(CH 2 ) 4 (R 13 )—, —CH 2 —NH—(CH 2 ) 4 (R 13 )—, —CH 2 —S—(CH 2 ) 4 (R 13 )—, —CH 2 —O—(CH 2 ) 6 (R 13 )—, —CH 2 —NH—(CH 2 ) 6 (R 13 )—, —CH 2 —S—(CH 2 ) 6 (R 13 )—, —NH—C(═O)—(CH 2 ) 4 (R 13 )—, —NH—C(═O)—(CH 2 ) 7 (R 13 )—, —NH—C(═O)NH—(CH 2 ) 3 (R 13 )—, —NH—C(═O)NH—(CH 2 ) 6 (R 13 )—, —CH 2 NH—C(═O)NH—(CH 2 ) 2 (R 13 )—, —CH 2 NH—C(═O)NH—((CH 2 ) 5 (R 13 )—, —NHC(═O)—(CH 2 ) 2 —C(═O)(R 13 )—, —NHC(═O)—(CH 2 ) 3 —C(═O)(R 13 )—, —NHC(═O)—(CH 2 ) 4 —C(═O)(R 13 )—, —OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —NHCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —NHCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —OCH 2 CH 2 OCH 2 C(═O)(R 13 )—, —OCH 2 CH 2 OCH 2 CH 2 OCH 2 C(═O)(R 13 )—, —NHC(═O)CH 2 OCH 2 CH 2 (R 13 )—, —NHC(═O)CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 NHCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 SCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 NHCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 SCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 (R 13 )—, —CH 2 NHC(═O)CH 2 OCH 2 C(═O)(R 13 )—, and —NHC(═O)CH 2 OCH 2 C(═O)(R 13 )—;  
 wherein when R 11  or R 12  terminates with a —C(═O)—, R 13  is selected from the group consisting of  
                     
 and when R 11  or R 12  does not terminate with a —C(═O)—, R 13  is selected from the group consisting of  
                     
 wherein said —O—(CH 2 CH 2 O—) p — or  
                     
  of R 12  and R 13  is a polyethylene glycol (PEG) polymer selected from 2000 (PEG 2000), 3400 (PEG 3400), or 5000 (PEG 5000) Daltons;  
 r is an integer from 0 to 8;  
 Q and Q 1  of substituents R 12  and R 13  are the same within a given compound and is the C 17  saturated chain of stearoic acid;  
 Z is selected from the group consisting of hydroxy, —NH 2 , —NH—C 1-8 alkyl, —N(C 1-8 alkyl) 2 , —O—C 1-8 alkyl, —O—C 1-8 alkyl—OH, —O—C 1-8 alkylC 1-4 alkoxy, —O—C 1-8 alkylcarbonylC 1-4 alkyl, —O—C 1-8 alkyl—CO 2 H, —O—C 1-8 alkyl—C(O)O—C 1-6 alkyl, —O—C 1-8 alkyl—O—C(O)C 1-8 alkyl, —O—C 1-8 alkyl—NH 2 , —O—C 1-8 alkyl—NH—C 1-8 alkyl, —O—C 1-8 alkyl—N(C 1-8 alkyl) 2 , —O—C 1-8 alkylamide—O—C 1-8 alkyl—C(O)—NH—C 1-8 alkyl, —O—C 1-8 alkyl—C(O)—N(C 1-8 alkyl) 2  and —NHC(O)C 1-8 alkyl.  
 
     
     
         86 . The therapeutic liposome composition of  claim 78  wherein the therapeutic agent is selected from the group consisting of steroids, immunosuppressants, antihistamines, non-steroidal anti-asthamtics, non-steroidal anti-inflammatory agents, cyclooxygenase- 2  inhibitors, cytotoxic agents, gene therapy agents, radiotherapy agents, and imaging agents.  
     
     
         87 . The therapeutic liposome composition of  claim 78  wherein the therapeutic agent is a cytotoxic drug.  
     
     
         88 . The therapeutic liposome composition of  claim 87  wherein the cytotoxic drug is selected from the group consisting of anthracycline antibiotics, platinum compounds, topoisomerase 1 inhibitors, and vinca alkaloids.  
     
     
         89 . The therapeutic liposome composition of  claim 87  wherein the cytotoxic agent is selected from the group consisting of doxorubicin, daunorubicin, epirubicin, idarubicin, cisplatin, carboplatin, ormaplatin, oxaliplatin, zeniplatin, enloplatin, lobaplatin, spiroplatin, ((-)-(R)- 2 -aminomethylpyrrolidine ( 1 , 1 -cyclobutane dicarboxylato)platinum), (SP- 4 - 3 (R) 1 , 1 -cyclobutane-dicarboxylato( 2 -)-( 2 -methyl- 1 , 4 -butanediamine-N,N′)platinum), nedaplatin, (bis-acetato-ammine-dichloro-cyclohexylamine-platinum(IV), topotecan, irinotecan, ( 7 -( 4 -methylpiperazino-methylene)- 10 , 11 -ethylenedioxy- 20 (S)-camptothecin),  7 -( 2 -(N-isopropylamino)ethyl)-( 20 S)-camptothecin,  9 -aminocamptothecin,  9 -nitrocamptothecin, vincristine, vinblastine, vinleurosine, vinrodisine, vinorelbine, and vindesine.  
     
     
         90 . The therapeutic liposome composition of  claim 87  wherein the cytotoxic agent is selected from the group consisting of doxorubicin, daunorubicin, epirubicin, idarubicin, cisplatin, including salts.