Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade

Abstract

The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

1 - 8 . (canceled)  
     
     
         9 . A compound having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is the Formula:  
                     
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 A is selected from the group consisting of single covalent bond and (CH(R 15 )) pa —(W 7 )rr wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is selected from the group consisting of (R 7 )NC(O) and N(R 7 );  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of a covalent single bond, O, S, NH, and CH 2 ;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, amidocarbonyl, halo, haloalkyl, and cyano;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D 5 , D 6 , J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5 , D 6 , J 5 , and J 6  are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 , with the provisos that no more than one of R 20  and R 21  is hydroxy and that no more than one of R 23  and R 24  is hydroxy;  
 R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
 Q s  is selected from the group consisting of a single covalent bond, CH 2 , and CH 2 CH 2 .  
 
     
     
         10 . The compound as recited in  claim 9  or a pharmaceutically acceptable salt thereof, wherein; 
 B is the Formula:                          R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of single covalent bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single bond, O, S, NH, and CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydride, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                                            R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 23  and R 24  is hydroxy;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy; and    Q s  is selected from the group consisting of a single covalent bond, CH 2  and CH 2 CH 2 .    
     
     
         11 . The compound as recited in  claim 10  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, and 3-trifluoromethylphenyl;    A is selected from the group consisting of CH 2 , CH 3 CH, CF 3 CH, NHC(O), CH 2 CH 2 ,and CH 2 CH 2 CH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, hydroxymethyl, methoxyamino, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single bond, O, S, NH, and CH 2 ;    Q is selected from the group consisting of 5-amino-3-amidocarbonylphenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, benzyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 2,6-dichlorophenyl, 3-cyanophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         12 . The compound as recited in  claim 9  having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is the Formula:  
                     
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 A is selected from the group consisting of single covalent bond and (CH(R 15 )) pa —(W 7 ) rr  wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );  
 R 7  is selected from the group consisting of hydrido and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is a covalent single bond;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkylamidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, aminoalkyl, hydroxy, amino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxyamido, carboxyalkyl, and cyano;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D 5 , D 6 , J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5  D 6 , J 5 , and J 6  are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 ;  
 R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and alkyl; and  
 Q s  is CH 2 .  
 
     
     
         13 . The compound as recited in  claim 12  or a pharmaceutically acceptable salt thereof, wherein; 
 B is the Formula:                          R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q b ;    A is selected from the group consisting of single covalent bond, NH, N(CH 3 ), CH 2 , CH 3 CH, and CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10  (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12   1  and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, carboxy, and cyano.    Q b  is selected from the group consisting of NR 20 R 21  and C(NR 25 )NR 23 R 24 , with the proviso that said Q b  group is bonded directly to a carbon atom;    R 20 , R 21 , R 23 , R 24  and R 25  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         14 . The compound as recited in  claim 13  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, and phenyl;    A is selected from the group consisting of CH 2 , CH 3 CH, CF 3 CH, NHC(O), CH 2 CH 2 ,and CH 2 CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro;    R 2  is selected from the group consisting of 5-amino-3-amidocarbonylphenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, benzyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         15 . The compound as recited in  claim 14  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, and phenyl;    A is selected from the group consisting of CH 2 , NHC(O), CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro;    R 2  is selected from the group consisting of 3-aminophenyl, benzyl, 3-chlorophenyl, 3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl; and    Y 0  is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro4-amdinobenzyl.    
     
     
         16 . A compound as recited in  claim 9 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-dimethylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 2-methylphenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is 3-aminophenyl, A is C(O)NH, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is 3-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-(N-methylamino)phenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-methylsulfonamidophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is 4-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-methylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-methylphenyl, B is 4-phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydrido;    R 2  is phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-dimethylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 2-methylphenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is phenyl, B is 3-aminophenyl, A is C(O)NH, Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is phenyl, B is 3-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-(N-methylamino)phenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-methylsulfonamidophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is phenyl, B is 4-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-methylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is phenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-methylphenyl, B is 4-phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxy, and X O  is fluoro;    R 2  is 3-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-dimethylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 2-methylphenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is phenyl, B is 3-aminophenyl, A is C(O)NH, Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is phenyl, B is 3-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-(N-methylamino)phenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-methylsulfonamidophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is phenyl, B is 4-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-methylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is phenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is amino, and X O  is hydrido;    R 2  is 3-methylphenyl, B is 4-phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R1 is amino, and X O  is hydrido;    R 2  is 3-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-dimethylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 2-methylphenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is 3-aminophenyl, A is C(O)NH, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is 3-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-(N-methylamino)phenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-methylsulfonamidophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is 4-amidinophenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-methylaminophenyl, B is phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido; or    R 2  is 3-methylphenyl, B is 4-phenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido.    
     
     
         17 . A compound having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;  
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 A is selected from the group consisting of single covalent bond and (CH(R15)) pa —(W 7 ) rr  wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is selected from the group consisting of (R 7 )NC(O) and N(R 7 );  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of a covalent single bond, O, S, NH, and CH 2 ;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, amidocarbonyl, halo, haloalkyl, and cyano;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D 5 , D6, J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5  D 6 , J 5 , and J 6  are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the provisos that no more than one of R 20  and R 21  is hydroxy and that no more than one of R 23  and R 24  is hydroxy;  
 R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
 Q s  is selected from the group consisting of a single covalent bond, CH 2 , and CH 2 CH 2 .  
 
     
     
         18 . The compound as recited in  claim 17  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propynyl, 2-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1 -ethyl-2-butynyl, 1 -heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1 -methyl-2-hexenyl, 1 -methyl-3-hexenyl, 1 -methyl-4-hexenyl, 1 -methyl-5-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1 -ethyl-2-pentenyl, 1 -ethyl-3-pentenyl, 1 -ethyl4-pentenyl, 1 -butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33  R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of single covalent bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single O, S, NH, and CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                                            R 16  , R 17  , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(N R 25  )N R 23 R 24  , and N (R  26 )C(N R 25  )N(R  23  )(R  24 ), with the provisos that no more than one of R 20  and R  21  is hydroxy at the same time and that no more than one of R 23  and R 24  is hydroxy;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy; and    Q s  is selected from the group consisting of a single covalent bond, CH 2 , and CH 2 CH 2 .    
     
     
         19 . The compound as recited in  claim 18  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl,(S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 3-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;    A is selected from the group consisting of single covalent bond, CH 2 , NHC(O), CH 2 CH 2 , CH 2 CH 2 CH 2 , and CH 3 CHCH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, hydroxymethyl, methoxyamino, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single O, S, NH, and CH 2 ;    Q is selected from the group consisting of 5-amino-3-amidocarbonylphenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, benzyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 2,6-dichlorophenyl, 3-cyanophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(N R 25 )N R 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         20 . The compound as recited in  claim 17  having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;  
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 A is selected from the group consisting of single covalent bond and (CH(R 15 )) pa —(W 7 ) rr  wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );  
 R 7  is selected from the group consisting of hydrido and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is a covalent single bond;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkylamidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, aminoalkyl, hydroxy, amino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxyamido, carboxyalkyl, and cyano;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D5, D 6 , J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5  D 6 , J 5 , and J6 are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 ;  
 R 20 , R 21 , R 23 , R 24   1  R 25 , and R 26  are independently selected from the group consisting of hydrido and alkyl; and  
 Q s  is CH 2 .  
 
     
     
         21 . The compound as recited in  claim 17  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q b ;    A is selected from the group consisting of: 
 (i) a single covalent bond, NH, N(CH 3 ), CH 2 , CH 3 CH, and CH 2 CH 2 ; and  
 (ii) CH 2 N(CH 3 ), CH 2 N(CH 2 CH 3 ), CH 2 CH 2 N(CH 3 ), and CH 2 CH 2 N(CH 2 CH 3 ) with the proviso that B is hydrido;  
   X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, carboxy, and cyano.    Q b  is selected from the group consisting of NR 20 R 21 , C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that said Q b  group is bonded directly to a carbon atom;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         22 . The compound as recited in  claim 21  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl,(S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 3-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;    A is selected from the group consisting of single covalent bond, CH 2 , CH 3 CH, and CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro;    R 2  is selected from the group consisting of 5-amino-3-amidocarbonylphenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, benzyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 2,6-dichlorophenyl, 3-cyanophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         23 - 24 . (canceled)  
     
     
         25 . A compound having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of C3-C7 cycloalkyl and C4 saturated heterocyclyl, wherein (a) each ring carbon is optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment, is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , and (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 :  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, amidocarbonyl, halo, haloalkyl, and cyano;  
 R 33  and R 34  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 A is selected from the group consisting of single covalent bond and (CH(R 15 )) pa —(W 7 ) rr  wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is selected from the group consisting of (R 7 )NC(O) and N(R 7 );  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of a covalent single O, S, NH, and CH 2 ;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D 5 , D 6 , J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5 , D 6 , J 5 , and J 6  are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 , with the provisos that no more than one of R 20  and R 21  is hydroxy and that no more than one of R 23  and R 24  is hydroxy;  
 R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
 Q s  is selected from the group consisting of a single covalent bond, CH 2 , and CH 2 CH 2 .  
 
     
     
         26 . The compound as recited in  claim 25  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-3-yl, cyclopentyl, cyclohexyl, norbornyl, bicyclo[3.1.0]hexan-6-yl, and cycloheptyl, wherein (a) each ring carbon is optionally substituted with R 33 , (b) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (c) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (d) a ring carbon or nitrogen, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , and (e) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, fluoro, chloro, bromo, and cyano;    R 33  and R34 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of single covalent bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single O, S, NH, and CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    Y 0  is selected from the group consisting of:                                            R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 23  and R 24  is hydroxy at the same time;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy; and    Q s  is selected from the group consisting of a single covalent bond, CH 2  and CH 2 CH 2 .    
     
     
         27 . The compound as recited in  claim 26  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl,and bicyclo[3.1.0]hexan-6-yl;    A is selected from the group consisting of single covalent bond, CH 2 , NHC(O), CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, hydroxymethyl, methoxyamino, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a covalent single O, S, NH, and CH 2 ;    Q is selected from the group consisting of 5-amino-3-amidocarbonylphenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, benzyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 2,6-dichlorophenyl, 3-cyanophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydride, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         28 . The compound as recited in  claim 25  having the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of C3-C7 cycloalkyl and C4 saturated heterocyclyl, wherein (a) each ring carbon is optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment, is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11   1  and (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, aminoalkyl, hydroxy, amino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxyamido, and cyano;  
 R 33  and R 34  are independently selected from the group consisting of hydrido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, and cyano;  
 A is selected from the group consisting of single covalent bond and (CH(R 15 )) pa —(W 7 ) rr  wherein rr is an integer selected from 0 through 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );  
 R 7  is selected from the group consisting of hydrido and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 R 1  and X O  are independently selected from the group consisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo;  
 R 2  is Z 0 -Q;  
 Z 0  is a covalent single bond;  
 Q is selected from the group consisting of aryl and heteroaryl wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, lower alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, monoalkylamidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, aminoalkyl, hydroxy, amino, lower alkylamino, alkylsulfonamido, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxyamido, carboxyalkyl, and cyano;  
 Y 0  is formula (IV):  
                     
 wherein D 5 , D 6 , J 5 , and J 6  are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K 2  is C, no more than one of D 5 , D 6 , J 5 , and J 6  is O, no more than one of D 5 , D 6 , J 5 , and J 6  is S, one of D 5 , D 6 , J 5 , and J 6  must be a covalent bond when two of D 5 , D 6 , J 5 , and J 6  are O and S, and no more than four of D 5 , D 6 , J 5 , and J 6  are N;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 ;  
 R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and alkyl; and  
 Q s  is CH 2 .  
 
     
     
         29 . The compound as recited in  claim 28  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and bicyclo[3.1.0]hexan-6-yl, wherein (a) each ring carbon is optionally substituted with R 33 , (b) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (c) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (d) a ring carbon or nitrogen, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , and (e) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    R 33  is selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, carboxy, amino, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of single covalent bond, NH, N(CH 3 ), CH 2 , CH 3 CH, CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, and chloro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, carboxy, and cyano.    Q b  is selected from the group consisting of NR 20 R 21  and C(NR 25 )NR 23 R 24 , with the proviso that said Q b  group is bonded directly to a carbon atom;    R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         30 . The compound as recited in  claim 29  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,and azetidin-3-yl;    A is selected from the group consisting of a single covalent bond, CH 2 , NHC(O), CH 2 CH 2  and CH 2 CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro;    R 2  is selected from the group consisting of 3-aminophenyl, 2,6-dichlorophenyl, 2-hydroxyphenyl, 5-amino-2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is selected from the group consisting of hydrido and C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         31 . The compound as recited in  claim 30  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,and azetidin-3-yl;    A is selected from the group consisting of a single covalent bond, CH 2 , CH 2 CH 2  and CH 2 CH 2 CH 2 ;    X O  is selected from the group consisting of hydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;    R 1  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro;    R 2  is selected from the group consisting of 3-aminophenyl, 2,6-dichlorophenyl, 2-hydroxyphenyl, phenyl, 5-amino-2-thienyl, and 3-thienyl; and    Y 0  is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.    
     
     
         32 . A compound as recited in  claim 25 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is cycylopropyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopropyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-3-fluorobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 5-amino-2-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopropyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclohexyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R1 is aminomethyl, and X O  is hydrido;    R 2  is 2-hydroxyphenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is phenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R1 is aminomethyl, and X O  is hydrido;    R 2  is 2,6-dichlorophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is aminomethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cycylopropyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclopropyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-3-fluorobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 5-amino-2-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclopropyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cyclohexyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 2-hydroxyphenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is phenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 2,6-dichlorophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydrido, and X O  is hydroxymethyl;    R 2  is 3-aminophenyl, B is cycylopropyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopropyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidino-3-fluorobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 5-amino-2-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopropyl, A is CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclopentyl, A is single bond, Y 0  is 4-amidino-2-fluorobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclohexyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 2-hydroxyphenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is phenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido;    R 2  is 3-thienyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido; or R 2  is 2,6-dichlorophenyl, B is cyclobutyl, A is single bond, Y 0  is 4-amidinobenzyl, R 1  is hydroxymethyl, and X O  is hydrido.    
     
     
         33 - 46 . (canceled)  
     
     
         47 . A composition for inhibiting thrombotic conditions in blood comprising a compound of any one of claims  9 ,  17 , and  25  and a pharmaceutically acceptable carrier.  
     
     
         48 . A method for inhibiting thrombotic conditions in blood comprising adding to blood a therapeutically effective amount of a composition of and  claim 47 .  
     
     
         49 . A method for inhibiting formation of blood platelet aggregates in blood comprising adding to blood a therapeutically effective amount of a composition of  claim 47 .  
     
     
         50 . A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a composition of  claim 47 .  
     
     
         51 . A method for treating or preventing venuous thromboembolism and pulmonary embolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         52 . A method for treating or preventing deep vein thrombosis in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         53 . A method for treating or preventing cardiogenic thromboembolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         54 . A method for treating or preventing thromboembolic stroke in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         55 . A method for treating or preventing thrombosis associated with cancer and cancer chemotherapy in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         56 . A method for treating or preventing unstable angina in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 47 .  
     
     
         57 . A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a compound of any one of claims  9 ,  17 , and  25  with a therapeutically effective amount of fibrinogen receptor antagonist.  
     
     
         58 . (canceled)