US2009304583A1PendingUtilityA1

Pathological tissue detection and treatment employing targeted benzoindole optical agents

62
Assignee: ACHILEFU SAMUELPriority: Oct 17, 2001Filed: Dec 22, 2008Published: Dec 10, 2009
Est. expiryOct 17, 2021(expired)· nominal 20-yr term from priority
Inventors:Samuel AchilefuRichard B. DorshowRaghavan RajagopalanJoseph E. Bugai
A61P 35/00A61K 49/0034A61K 41/0057C07D 209/60A61K 49/0052C09B 23/086A61P 9/10C07D 417/14C09B 47/00A61K 47/62A61K 49/0056C07D 417/04A61K 49/0032A61P 35/04
62
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Claims

Abstract

Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Claims

exact text as granted — not AI-modified
1 . A compound of the following formula 
       
         
           
           
               
               
           
         
       
       wherein
 W 1  and W 2  may be the same or different and are selected from the group consisting of —O, —NR 12 , —S, and —Se; 
 Y 1 , Y 2 , Z 1 , and Z 2  are independently selected from hydrogen, tumor-specific agent, phototherapy agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 )—NHCO-Bm, —CH 2 —CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) b —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Bm, —CH 2 (CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Bm, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CHrNHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; 
 K 1  and K 2  are independently selected from C 1 -C 30  alkyl, C 5 -C 30  aryl, C 1 -C 30  alkoxyl, C 1 -C 30  polyalkoxyalkyl, C 1 -C 30  polyhydroxyalkyl, C 5 -C 30  polyhydroxyaryl, C 1 -C 30  aminoalkyl, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 , —(CH 2 ) a —CO—, —(CH 2 ) a , —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 X 1  and X 2  are independently selected from nitrogen and —CR 14 R 15 ; 
 A 1  is a single or a double bond; 
 B 1 , C 1 , and D 1  are independently selected from —O—, —S—, —Se—, —P—, —CR 10 R 11 , —CR 11 , alkyl, NR 12 , and —C═O; 
 A 1 , B 1 , C 1 , and D 1  may together form a 6- to 12-membered carbocyclic ring or a 6- to 12-membered heterocyclic ring optionally containing one or more oxygen, nitrogen, or sulfur atom; 
 a 1  and b 1  independently vary from 0 to 5; 
 R 1  to R 13  and R 18  are independently selected from hydrogen, C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20 ) polyhydroxyaryl, C 1 -C 10  aminoalkyl, cyano, nitro, halogen, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —OH, —(CH 2 ) a —CO 2 H, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —OH and —CH 2 —(CH 2 OCH 2 ) b —CO 2 H; 
 R 14  to R 17  are independently selected from hydrogen, C 1 -C 10  alkyl. C 5 -C 20  aryl. C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20  polyhydroxyaryl, C 1 -C 10  aminoalkyl, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH, —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 Bm and Dm are independently selected from bioactive peptide, protein, cell, antibody, antibody fragment, saccharide, glycopeptide, peptidomimetic, drug, drug mimic, hormone, metal chelating agent, radioactive or nonradioactive metal complex, echogenic agent, photoactive molecule, and phototherapy agent; 
 a and c independently vary from 1 to 20; and 
 b and d independently vary from 1 to 100. 
 
     
     
         2 . The compound of  claim 1  wherein
 W 1  and W 2  are —NR 12 ;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         3 . The compound of  claim 1  wherein
 W 1  and W 2  are —O;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CON H, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         4 . The compound of  claim 1  wherein
 W 1  and W 2  are —S;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         5 . The compound of  claim 1  wherein
 W 1  and W 2  are —Se;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         6 . The compound of any of  claims 2 - 5  wherein
 each K 1  and K 2  is —(CH 2 ) 4 CO—;   each X 1  and X 2  is a single bond;   each R 19  to R 31 , Y 1  and Z 1  is H;   Y 2  is a tumor-specific agent; and   Z 2  is a phototherapy agent.   
     
     
         7 . The compound of  claim 6  wherein the tumor-specific agent is a bioactive peptide containing 2 to 30 amino acid units. 
     
     
         8 . The compound of  claim 7  wherein the tumor-specific agent is octreotate and bombesin (7-14). 
     
     
         9 . The compound of  claim 6  wherein the phototherapy agent is a photosensitizer. 
     
     
         10 . The compound of  claim 9  wherein the photosensitizer is 2-[1-hexyloxyethyl]-2-devinylpyropheophorbide-a. 
     
     
         11 . A pharmaceutically acceptable composition comprising a compound of formula 
       
         
           
           
               
               
           
         
       
       wherein
 W 1  and W 2  may be the same or different and are selected from the group consisting of —O, —NR 12 , —S, and —Se; 
 Y 1 , Y 2 , Z 1 , and Z 2  are independently selected from hydrogen, tumor-specific agent, phototherapy agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) b —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Bm, —CH 2 (CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Bm, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CHrNHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; 
 K 1  and K 2  are independently selected from C 1 -C 30  alkyl, C 5 -C 30  aryl, C 1 -C 30  alkoxyl, C 1 -C 30  polyalkoxyalkyl, C 1 -C 30  polyhydroxyalkyl, C 5 -C 30  polyhydroxyaryl, C 1 -C 30  aminoalkyl, saccharlde, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 , —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 X 1  and X 2  are independently selected from nitrogen and —CR 14 R 15 ; 
 A 1  is a single or a double bond; 
 B 1 , C 1 , and D 1  are independently selected from —O—, —S—, —Se—, —P—, —CR 10 R 11 , —CR 11 , alkyl, NR 12 , and —C═O; 
 A 1 , B 1 , C 1 , and D 1  may together form a 6- to 12-membered carbocyclic ring or a 6- to 12-membered heterocyclic ring optionally containing one or more oxygen, nitrogen, or sulfur atom; 
 a 1  and b 1  independently vary from 0 to 5; 
 R 14  to R 13  and R 18  are independently selected from hydrogen, C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20 )polyhydroxyaryl, C 1 -C 10  aminoalkyl, cyano, nitro, halogen, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —OH, —(CH 2 ) a —CO 2 H, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —OH and —CH 2 —(CH 2 OCH 2 ) b —CO 2 H; 
 R 14  to R 17  are independently selected from hydrogen, C 1 -C 10  alkyl. C 5 -C 20  aryl. C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20  polyhydroxyaryl, C 1 -C 10  aminoalkyl, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH, —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 Bm and Dm are independently selected from bioactive peptide, protein, cell, antibody, antibody fragment, saccharide, glycopeptide, peptidomimetic, drug, drug mimic, hormone, metal chelating agent, radioactive or nonradioactive metal complex, echogenic agent, photoactive molecule, and phototherapy agent; 
 a and c independently vary from 1 to 20; and 
 b and d independently vary from 1 to 100. 
 
       and at least one excipient in a pharmaceutically acceptable composition. 
     
     
         12 . The composition of  claim 11  wherein
 W 1  and W 2  are —NR 12 ;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         13 . The composition of  claim 11  wherein
 W 1  and W 2  are —O;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         14 . The composition of  claim 11  wherein
 W 1  and W 2  are —S;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         15 . The composition of  claim 11  wherein
 W 1  and W 2  are —Se;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         16 . A method of performing a diagnostic procedure to detect or image a tumor or performing a therapeutic procedure on a tumor or monitoring organ function, the method comprising
 administering to an individual an effective amount of a compound of the following formula   
       
         
           
           
               
               
           
         
       
       wherein
 W 1  and W 2  may be the same or different and are selected from the group consisting of —O, —NR 12 , —S, and —Se; 
 Y 1 , Y 2 , Z 1 , and Z 2  are independently selected from hydrogen, tumor-specific agent, phototherapy agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 )—NHCO-Bm, —CH 2 —CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Bm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) b —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Bm, —CH 2 (CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Bm, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) b —CONH-Dm, —(CH 2 ) a —N(R 12 )—(CH 2 ) c —NHCO-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 ) a —N(R 12 )—CH 2 —(CH 2 OCH 2 ) b —CHrNHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —CONH-Dm. —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—(CH 2 ) a —NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —N(R 12 )—CH 2 —(CH 2 OCH 2 ) d —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; 
 K 1  and K 2  are independently selected from C 1 -C 30  alkyl, C 5 -C 30  aryl, C 1 -C 30  alkoxyl, C 1 -C 30  polyalkoxyalkyl, C 1 -C 30  polyhydroxyalkyl, C 5 -C 30  polyhydroxyaryl, C 1 -C 30  aminoalkyl, saccharlde, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 , —(CH 2 ) a —CO—, —(CH 2 ) a , —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 X 1  and X 2  are independently selected from nitrogen and —CR 14 R 15 ; 
 A 1  is a single or a double bond; 
 B 1 , C 1 , and D 1  are independently selected from —O—, —S—, —Se—, —P—, —CR 10 R 11 , —CR 11 , alkyl, NR 12 , and —C═O; 
 A 1 , B 1 , C 1 , and D 1  may together form a 6- to 12-membered carbocyclic ring or a 6- to 12-membered heterocyclic ring optionally containing one or more oxygen, nitrogen, or sulfur atom; 
 a 1  and b 1  independently vary from 0 to 5; 
 R 1  to R 13  and R 18  are independently selected from hydrogen, C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20 ) polyhydroxyaryl, C 1 -C 10  aminoalkyl, cyano, nitro, halogen, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —OH, —(CH 2 ) a —CO 2 H, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —OH and —CH 2 —(CH 2 OCH 2 ) b —CO 2 H; 
 R 14  to R 17  are independently selected from hydrogen, C 1 -C 10  alkyl. C 5 -C 20  aryl. C 1 -C 10  alkoxyl, C 1 -C 10  polyalkoxyalkyl, C 1 -C 20  polyhydroxyalkyl, C 5 -C 20  polyhydroxyaryl, C 1 -C 10  aminoalkyl, saccharide, peptide, —CH 2 (CH 2 OCH 2 ) b —CH 2 —, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CHa-CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, —(CH 2 ) a —O—, and —CH 2 —(CH 2 OCH 2 ) b —CO—; 
 Bm and Dm are independently selected from bioactive peptide, protein, cell, antibody, antibody fragment, saccharide, glycopeptide, peptidomimetic, drug, drug mimic, hormone, metal chelating agent, radioactive or nonradioactive metal complex, echogenic agent, photoactive molecule, and phototherapy agent; 
 a and c independently vary from 1 to 20; and 
 b and d independently vary from 1 to 100; 
 and thereafter, performing the diagnostic or therapeutic procedure or monitoring organ function. 
 
     
     
         17 . The method of  claim 16  wherein
 W 1  and W 2  are —NR 12 ;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide; Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent; a and c independently vary from 1 to 10; b and d independently vary from 1 to 30; with the proviso that at least one of Y 1 , Y 2 , Z 1 , and Z 2  is a tumor-specific agent or a phototherapy agent or contains Bm or Dm.   
     
     
         18 . The method of  claim 16  wherein
 W 1  and W 2  are —O;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 )—NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide;   Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent;   a and c independently vary from 1 to 10; and   b and d independently vary from 1 to 30.   
     
     
         19 . The method of  claim 16  wherein
 W 1  and W 2  are —S;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide; Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent; a and c independently vary from 1 to 10; b and d independently vary from 1 to 30; with the proviso that at least one of Y 1 , Y 2 , Z 1 , and Z 2  is a tumor-specific agent or a phototherapy agent or contains Bm or Dm.   
     
     
         20 . The method of  claim 16  wherein
 W 1  and W 2  are —Se;   Y 1  and Y 2  are selected from the group consisting of hydrogen, tumor-specific agent, —CONH-Bm, —NHCO-Bm, —(CH 2 ) a —CONH-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Bm, —(CH 2 ) a —NHCO-Bm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Bm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ;   Z 1  and Z 2  are independently selected from the group consisting of hydrogen, phototherapy agent, —CONH-Dm, —NHCO-Dm, —(CH 2 ) a —CONH-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH-Dm, —(CH 2 )—NHCO-Dm, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO-Dm, —(CH 2 ) a —NR 12 R 13 , and —CH 2 (CH 2 OCH 2 ) b —CH 2 NR 12 R 13 ; K 1  and K 2  are independently selected from the group consisting of C 1 -C 10  alkyl, C 5 -C 20  aryl, C 1 -C 20  alkoxyl, C 1 -C 20  aminoalkyl, —(CH 2 ) a —CO—, —(CH 2 ) a —CONH—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —CONH—, —(CH 2 ) a —NHCO—, —CH 2 —(CH 2 OCH 2 ) b —CH 2 —NHCO—, and —CH 2 —(CH 2 OCH 2 ) b —CO—;   X 1  and X 2  are single bonds, or are independently selected from the group consisting of nitrogen, —CR 14 —, —CR 14 R 15 , and —NR 16 R 17 ;   a 1  and b 1  independently vary from 0 to 3;   Bm is selected from the group consisting of bioactive peptide containing 2 to 30 amino acid units, protein, antibody fragment, mono- and oligosaccharide; Dm is selected from the group consisting of photosensitizer, photoactive molecule, and phototherapy agent; a and c independently vary from 1 to 10; b and d independently vary from 1 to 30; with the proviso that at least one of Y 1 , Y 2 , Z 1 , and Z 2  is a tumor-specific agent or a phototherapy agent or contains Bm or Dm.   
     
     
         21 . The method of any of  claims 17 - 20  wherein
 each K 1  and K 2  is —(CH 2 ) 4 CO—;   each X 1  and X 2  is a single bond;   each R 19  to R 31 , Y 1  and Z 1  is H;   Y 2  is a tumor-specific agent; and   Z 2  is a phototherapy agent.   
     
     
         22 . The method of  claim 21  wherein the tumor-specific agent is a bioactive peptide containing 2 to 30 amino acid units. 
     
     
         23 . The method of  claim 22  wherein the tumor-specific agent is octreotate and bombesin (7-14). 
     
     
         24 . The method of  claim 21  wherein the phototherapy agent is a photosensitizer. 
     
     
         25 . The method of  claim 24  wherein the photosensitizer is 2-[1-hexyloxyethyl]-2-devinylpyropheophorbide-a. 
     
     
         26 . The method of  claim 16  wherein the procedure utilizes light of wavelength in the region of 300-1300 nm. 
     
     
         27 . The method of  claim 16  wherein the diagnostic procedure is optical tomography. 
     
     
         28 . The method of  claim 16  wherein the diagnostic procedure is fluorescence endoscopy. 
     
     
         29 . The method of  claim 16  wherein the procedure further comprises a step of imaging and therapy selected from the group consisting of absorption, light scattering, photoacoustic and sonofluoresence technique. 
     
     
         30 . The method of  claim 16  wherein the procedure is for diagnosing and treating atherosclerotic plaques and blood clots. 
     
     
         31 . The method of  claim 16  wherein the procedure comprises administering localized therapy. 
     
     
         32 . The method of  claim 16  wherein the therapeutic procedure comprises photodynamic therapy. 
     
     
         33 . The method of  claim 16  wherein the therapeutic procedure comprises laser assisted guided surgery (LAGS) for the detection and treatment of micrometastases.

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