Diaryl Substituted Pyridinones

Abstract

Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , and R 5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

1 . A compound of the formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, arylalkoxy, arylalkyl, CN, alkanoyl, alkoxy, alkoxyalkyl, or arylalkanoyl, 
 wherein the aryl portion of arylalkoxy, arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is arylalkoxy, aryloxy, OH, halogen, arylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n aryl, —OC(O)N(alkyl) (CH 2 ) n aryl, alkyl, alkoxyalkoxy, dialkylamino, heteroaryl, heterocycloalkyl, or CO 2 H, wherein  
 n is 0 1, 2, 3, 4, 5 or 6;  
 the aryl portion of arylalkoxy, aryloxy, arylthioalkoxy, —OC(O)NH(CH 2 ) n aryl, and —OC(O)N(alkyl) (CH 2 ) n aryl or the heteroaryl and heterocycloalkyl groups is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 , NR 6 R 7 alkyl, —OC(O)NR 6 R 7,  wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy;  
 R 3  is halogen, alkoxycarbonyl, arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N alkyl) (CH 2 ) n aryl, aryloxy, arylthio, thioalkoxy, arylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein the aryl portion of arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, and arylthioalkoxy, is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy,  
 
 wherein n is 0, 1, 2, 3, 4, 5, or 6; or  
 R 2 , R 3  and the carbons to which they are attached form an aryl, heterocycloalkyl or a heteroaryl ring, which is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, alkoxy, halogen, arylalkyl, arylalkoxy, heteroarylalkyl, heterocycloalkylalkyl, CN, NO 2 , haloalkyl, or haloalkoxy;  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein the aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is arylalkyl, alkyl, aryl, alkoxy, heterocycloalkylalkyl, heteroarylalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7,  amidino, haloalkyl, or haloalkoxy.  
 
     
     
         2 . A compound or salt of the formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is alkanoyl, halogen, arylalkanoyl, arylalkyl, alkoxyalkyl, hydroxyalkyl, or carboxaldehyde, wherein 
 the aryl portion of arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 the alkyl portion of the hydroxyalkyl, arylalkyl, alkanoyl, alkoxyalkyl and arylalkanoyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is arylalkoxy, aryloxy, OH, halogen, arylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n aryl, —OC(O)N(alkyl) (CH 2 ) n aryl, alkyl, alkoxyalkoxy, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 the aryl portion of. arylalkoxy, aryloxy, arylthioalkoxy, —OC(O)NH(CH 2 ) n aryl, and —OC(O)N(alkyl) (CH 2 ) n aryl or the heteroaryl and heterocycloalkyl groups is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 , NR 6 R 7 alkyl, —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion. of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy;  
 R 3  is halogen, arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, aryloxy, arylthio, thioalkoxy, arylthioalkoxy, or alkenyl, NR 6 R 7  or—alkyl, wherein  
 
 the aryl portion of arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, and arylthioalkoxy, is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3, 4, 5, or 6; or  
 R 2 , R 3  and the carbons to which they are attached form an aryl, heterocycloalkyl or a heteroaryl ring, which is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, alkoxy, halogen, arylalkyl, arylalkoxy, heteroarylalkyl, heterocycloalkylalkyl, CN, NO 21  haloalkyl, or haloalkoxy;  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 The aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is arylalkyl, alkyl, aryl, alkoxy, heterocycloalkylalkyl, heteroarylalkyl, arylthioalkyl, heterocycloalkyl, or heteroaryl, wherein  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy.  
 
     
     
         3 . A compound or salt according to  claim 2  wherein  
       R 2  is arylalkoxy, aryloxy, OH, halogen, arylthioalkoxy, alkoxy, alkyl, alkoxyalkoxy, —OC(O)NH(CH 2 ) n phenyl —OC(O)N(alkyl)(CH 2 ) n phenyl, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, or thiazolyl, thiophenyl, wherein 
 n is 0, 1, 2, 3, 4, 5 or 6; and  
 the above are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, or thiophenyl.  
 
     
     
         4 . A compound or salt according to  claim 2  wherein  
       R 5  is phenyl(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, phenyl, naphthyl, (C 1 -C 6 )alkoxy, piperidinyl(C 1 -C 6 )alkyl, pyrrolyl(C 1 -C 6 )alkyl, pyrrolidinyl(C 1 -C 6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, pyrazolyl(C 1 -C 6 )alkyl, imidazolyl(C 1 -C 6 )alkyl, tetrahydropyridinyl(C 1 -C 6 )alkyl, thiophenyl(C 1 -C 6 )alkyl, arylthio(C 1 -C 6 )alkyl, pyridyl, or pyridyl(C 1 -C 6 )alkyl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently (C 1 -C 4 )alkyl, fluoro, chloro, bromo, (C 1 -C 4 )alkoxy, phenyl(C 1 -C 4 )alkoxy, thio (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkoxycarbonyl, phenyl(C 1 -C 4 )alkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, CF 3 , —CF 2 CF 3 , OCF 3  or OCF 2 CF 3 .  
     
     
         5 . A compound or salt according to  claim 2  wherein  
       R 1  is halogen, (C 1 -C 6 )alkanoyl, phenyl(C 1 -C 6 )alkanoyl, naphthyl(C 1 -C 6 )alkanoyl, naphthyl(C 1 -C,)alkyl, phenyl(C 1 -C 6 )alkyl, alkoxyalkyl, hydroxyalkyl, or carboxaldehyde, wherein 
 the phenyl and naphthyl portions of the above are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 the alkyl portion of the hydroxyalkyl, arylalkyl, alkanoyl, alkoxyalkyl and arylalkanoyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy.  
 
     
     
         6 . A compound or salt according to  claim 2  wherein  
       R 3  is halogen, phenylalkoxycarbonyl, phenyloxycarbonyl, phenyl(C 1 -C 6 )alkyl, —OC(O)NH(CH 2 ) n aryl, phenylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, phenyloxy, naphthyloxy, phenylthio, thioalkoxy, arylthioalkoxy, (C 2 -C 6 )alkenyl, NR 6 R 7  or alkyl, wherein 
 the phenyl, naphthyl, and aryl portions of arylalkoxycarbonyl 1 , aryloxycarbonyl, arylalkyl, —OC (O)NH (CH 2 ) n aryl, arylthioalkoxy, arylalkoxy, and—OC(O)N(alkyl) (CH 2 ) n aryl, are unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ; and 
 wherein n is 0, 1, 2, 3, 4, 5, or 6.  
 
 
     
     
         7 . A compound or salt according to  claim 2  wherein  
       R 4  is H, (C 1 -C 6 )alkyl, phenylalkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, (C 1 -C 6 )alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein 
 the phenyl portion of the above groups is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3,  or OCF 3 .  
 
     
     
         8 . A compound or salt according to  claim 2  wherein  
       R 1  is halogen, (C 1 -C 6 )alkanoyl, phenyl(C 1 -C 6 )alkanoyl, naphthyl(C 1 -C 6 )alkanoyl, naphthyl(C 1 -C,)alkyl, phenyl(C 1 -C 6 )alkyl, alkoxyalkyl, hydroxyalkyl, or carboxaldehyde, wherein 
 the phenyl and napthyl portions of the above are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 the alkyl portion of the above groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy.  
 R 2  is phenylalkoxy, aryloxy, OH, halogen, phenylthioalkoxy, alkoxy, alkyl, alkoxyalkoxy, —OC (O)NH (CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, or thiophenyl, wherein  
 n is 0, 1, 2, 3, or 4, and  
 the above groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, halo(C 1 -C 4 )alkyl, thiophenyl;  
 R 3  is halogen, phenylalkoxycarbonyl, phenyloxycarbonyl, phenyl(C 1 -C 6 )alkyl, phenylalkoxy, phenyloxy, phenylthio, thioalkoxy, arylthioalkoxy, (C 2 -C 6 )alkenyl, NR 6 R 7  or alkyl, wherein  
 the phenyl, naphthyl, and aryl portions of arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl arylthioalkoxy, arylalkoxy, and—OC(O)N(alkyl) (CH 2 ) n aryl, are unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 , wherein n is 0, 1, 2, 3, 4, 5, or 6; or R 4  is H, (C 1 -C 6 )alkyl, phenylalkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, or alkoxyalkoxy, wherein the phenyl portion of the above groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3 , or OCF 3 .  
 R 5  is phenyl(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, phenyl, naphthyl, pyridyl, (C 1 -C 6 )alkoxy, piperidinyl(C 1 -C 6 )alkyl, pyrrolyl(C 1 -C 6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, pyrazolyl(C 1 -C 6 )alkyl, imidazolyl(C 1 -C 6 )alkyl, tetrahydropyridinyl(C 1 -C 6 )alkyl, thiophenyl(C 1 -C 6 )alkyl, phenylthio(C 1 -C 6 )alkyl, or pyridyl(C 1 -C 6 )alkyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C-C 1 -   4 )alkyl, fluoro, chloro, bromo, (C 1 -C 4 )alkoxy, phenyl(C 1 -C 4 )alkoxy, thio (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkoxycarbonyl, phenyl(C 1 -C 4 )alkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, CF 3 , —CF 2 CF 3 , OCF 3  or OCF 2 CF 3 .  
 
     
     
         9 . A compound or salt according to  claim 8  wherein  
       R 1  is halogen, (Cl-C 4 )alkanoyl, phenyl(C 1 -C 4 )alkanoyl, benzyl, phenethyl, phenpropyl, hydroxyalkyl, or carboxaldehyde, wherein 
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro/CN, CF 3 , OCF 3  or CO 2 H;  
 the alkyl portion of the above groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy;  
 R 2  is benzyloxy, phenethyloxy, phenpropyloxy, phenbutyloxy, phenyloxy, OH, halogen, phenylthioalkoxy, alkoxy, alkyl, alkoxyalkoxy, wherein  
 n is 0, 1, 2, 3, or 4, and the above groups are unsubstituted or substituted with 1, 2, or 3, groups that are independently halogen, halo(C 1 -C 4 )alkyl, or thiophenyl;  
 R 3  is halogen, phenylalkoxycarbonyl, phenyloxycarbonyl, phenyl(C 1 -C 6 )alkyl, phenylalkoxy, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, (C 2 -C 6 )alkenyl, NR 6 R 7  or alkyl, wherein  
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, (C 1 -C 4 )alkyl, CF 3 , or OCF 3 ,  
 R 4  is H, (C 1 -C   6 )alkyl, phenylalkoxy, benzyl, phenethyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, or alkoxyalkoxy, wherein  
 the phenyl portion of the above groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, (C 1 -C 4 )alkoxy 1  (C 1 -C 4 )alkyl, nitro, CF 3 , or OCF 3 .  
 R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, (C 1 -C 6 )alkyl, phenyl, or pyridyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 4 )alkyl, fluoro, chloro, bromo, (C 1 -C 4 )alkoxy, phenyl(C 1 -C 4 )alkoxy, thio (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , amidino, CF 3 , or OCF 3 .  
 
     
     
         10 . A compound or salt according to  claim 9  wherein  
       R 1  is bromo, phenyl(C 1 -C   4 )alkanoyl, benzyl, phenethyl, phenpropyl, hydroxyalkyl, or carboxaldehyde, wherein 
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H; R 2  is benzyloxy, phenethyloxy, phenpropyloxy, phenbutyloxy, phenyloxy, OH, halogen, ro phenylthioalkoxy, wherein  
 n is 0, 1, 2, 3, or 4, and  
 the above groups are unsubstituted or substituted with 1, 2, or 3, groups that are independently halogen, halo(C 1 -C 4 )alkyl, or thiophenyl;  
 R 3  is bromo, phenylalkoxycarbonyl, phenyloxycarbonyl, phenyl(C 1 -C   6 )alkyl, phenylalkoxy, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, (C 2 -C 6 )alkenyl, NR 6 R 7  or alkyl, wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, (C 1 -C 4 )alkyl, CF 3 , or OCF 3 ,  
 R 4  is H, (C 1 -C 6 )alkyl, phenylalkoxy, benzyl, or phenethyl, wherein the phenyl portion of the above groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl, nitro, CF 3 , or OCF 3 .  
 R 5  is benzyl, phenethyl, phenpropyl, (C 1 -C 6 )alkyl, phenyl, or pyridyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 4 )alkyl, fluoro, chloro, bromo, (C 1 -C 4 )alkoxy, CO 2 H, CN, amidinooxime, amidino, CF 3 , or OCF 3 .  
 
     
     
         11 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, arylalkoxy, arylalkyl, CN, alkanoyl, alkoxy, alkoxyalkyl, or arylalkanoyl, 
 wherein the aryl portion of arylalkoxy, arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4,or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is H, arylthio, —OC(O)NH(CH 2 ) n aryl, arylalkyl, —OC(O)N(alkyl) (CH 2 ) n aryl, or arylthioalkoxy, wherein n is 1, 2, 3, 4, or 5;  
 R 3  is halogen, alkoxycarbonyl, arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, aryloxy, arylthio, thioalkoxy, arylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein  
 the aryl portion of arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, and arylthioalkoxy, is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3, 4, S, or 6; or  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 The aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is arylalkyl, alkyl, aryl, alkoxy, heterocycloalkylalkyl, heteroarylalkyl, arylthioalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy.  
 
     
     
         12 . A compound or salt according to  claim 11  wherein  
       R 1  is H, F, Cl, Br, (C 1 -C 6 )alkyl, carboxaldehyde, hydroxy(C 1 -C 6 )alkyl, phenyl(C 1 -C   6 )alkoxy, phenyl(C 1 -C 6 )alkyl, CN, or phenyl(C 1 -C 6 )alkanoyl 
 wherein the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy.  
 
     
     
         13 . A compound or salt according to  claim 11  wherein  
       R 2  is H, phenylthio, —OC(O)NH(CH 2 ) n aryl, phenylalkyl, —OC(O)N(alkyl) (CH 2 ) n aryl, or phenylthio(C 1 -C 6 )alkoxy, wherein 
 n is 1, 2, 3, or 4.  
 
     
     
         14 . A compound or salt according to  claim 11  wherein  
       R 3  is halogen, alkoxycarbonyl, phenylalkoxycarbonyl, phenyloxycarbonyl, phenylalkyl, —OC(O)NH(CH 2 ) n phenyl, phenylalkoxy, —OC(O)N(alkyl) (CH 2 ) n phenyl, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl, halo(C 1 -C 4 )alkyl, or halo(C 1 -C 4 )alkoxy, wherein n is 0, 1, 2, 3, or 4.  
 
     
     
         15 . A compound or salt according to  claim 11  wherein  
       R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein 
 the phenyl portion of phenylalkoxy, phenylalkyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy.  
 
     
     
         16 . A compound or salt according to  claim 11  wherein  
       R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, alkyl, phenyl, alkoxy, pyridyl(C 1 -C 6 )alkyl, phenyl(C 1 -C 6 ) thioalkyl, pyrrolyl, pyrrolyl(C 1 -C 6 )alkyl, or pyridyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 6 )alkyl, halogen, (C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkoxy, (C 1 -C 6 ) thioalkoxy, alkoxycarbonyl, CO 2 H, CN, amidinooxime, amidino, CF 3 , or OCF 3 .  
     
     
         17 . A compound or salt according to  claim 11  wherein  
       R 1  is H, Cl, Br, (C 1 -C 6 )alky, carboxaldehyde, hydroxy(C 1 -C 6 )alkyl, 
 wherein the alkyl portion of above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy  
 R 2  is H, phenylthio, —OC(O)NH(CH 2 ) n aryl, phenylalkyl, —OC(O)N(alkyl) (CH 2 ) n aryl, or phenylthio(C 1 -C 6 )alkoxy, wherein n is 1, 2, 3, or 4  
 R 3  is bromo, alkoxycarbonyl, phenylalkoxycarbonyl, phenyloxycarbonyl, phenylalkyl, phenylalkoxy, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein  
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl, halo(C 1 -C 4 )alkyl, or halo(C 1 -C 4 )alkoxy,  
 wherein n is 0, 1, 2, 3, or 4;  
 R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or wherein  
 the phenyl portion of phenylalkoxy, phenylalkyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy  
 R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, alkyl, phenyl, phenyl(CI-C 6 )thioalkyl, pyrrolyl, or pyridyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 5 )alkyl, halogen, (C 1 -C 6 )alkoxy, benzyloxy, (C 1 -C 6 )thioalkoxy, alkoxycarbonyl, CO 2 H, CN, amidinooxime, amidino, CF 3 , or OCF 3 .  
 
     
     
         18 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, arylalkoxy, arylalkyl, CN, alkanoyl, alkoxy, alkoxyalkyl, or arylalkanoyl, 
 wherein the aryl portion of arylalkoxy, arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is arylalkoxy, aryloxy, OH, halogen, arylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n aryl, —OC(O)N(alkyl) (CH 2 ) n aryl, alkyl, alkoxyalkoxy, dialkylamino, or CO 2 H, wherein  
 N is 0, 1, 2, 3, 4, 5 or 6;  
 the aryl portion of arylalkoxy, aryloxy, arylthioalkoxy, OC(O)NH(CH 2 ) n aryl, and —OC(O)N(alkyl) (CH 2 ) n aryl or the heteroaryl and heterocycloalkyl groups is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 , NR 6 R 7 alkyl, —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy;  
 R 3  is halogen, alkoxycarbonyl, arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, aryloxy, arylthio, thioalkoxy, arylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein  
 
 the aryl portion of arylalkoxycarbonyl, aryloxycarbonyl, arylalkyl, —OC(O)NH(CH 2 ) n aryl, arylalkoxy, —OC(O)N(alkyl) (CH 2 ) n aryl, and arylthioalkoxy, is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3, 4, 5, or 6; or  
 R 2 , R 3  and the carbons to which they are attached form an aryl, heterocycloalkyl or a heteroaryl ring, which is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, alkoxy, halogen, arylalkyl, arylalkoxy, heteroarylalkyl, heterocycloalkylalkyl, CN, NO 2 , haloalkyl, or haloalkoxy;  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 The aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is aryl, heterocycloalkylalkyl, heteroarylalkyl, arylthioalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy.  
 
     
     
         19 . A compound or salt according to  claim 18  wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, phenylalkoxy, phenylalkyl, CN, alkanoyl, alkoxy, alkoxyalkyl, or phenylalkanoyl, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is phenylalkoxy, phenyloxy, OH, halogen, phenylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, alkyl, alkoxyalkoxy, dialkylamino, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 the above aryl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, pyridyl, thiophenyl, NR 6 R 7 , NR 6 R 7 alkyl, or —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, phenylalkyl, phenylalkoxy, or phenylalkanoyl, wherein the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy.  
 
 
     
     
         20 . A compound or salt according to  claim 18  wherein  
       R 3  is halogen, alkoxycarbonyl, phenylalkoxycarbonyl, phenyloxycarbonyl, phenylalkyl, —OC(O)NH(CH 2 ) n phenyl, phenylalkoxy, —OC(O)N(alkyl) (CH 2 ) n ,phenyl, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3, 4, 5, or 6; or  
 R 2 , R 3  and the carbons to which they are attached form an phenyl, piperidinyl, pyrrolyl, pyrrolinyl or a pyridyl ring, each of which is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, alkoxy, halogen, phenylalkyl, phenylalkoxy, CN, NO 2 , haloalkyl, or haloalkoxy; R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is phenyl, naphthyl, pyrrolylalkyl, piperidinylalkyl pyridinylalkyl, pyrimidinylalkyl, phenylthioalkyl, pyrrolyl, piperidinyl, pyridyl, or thiophenylalkyl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, phenylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy.  
 
     
     
         21 . A compound or salt according to  claim 18  wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, benzyloxy, phenethyloxy, phenpropyloxy, benzyl, phenethyl, phenpropyl, CN, alkanoyl, alkoxy, or phenylC(O)—, phenylCH 2 C(O)—, or phenylCH 2 CH 2 C(O), 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 wherein the above alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that,-are independently halogen, methoxy, or ethoxy;  
 R 2  is benzyloxy, phenethyloxy, phenpropyloxy, phenyloxy, OH, halogen, phenylthioalkoxy, alkyl, alkoxy, —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, dialkylamino, or CO 2 H, wherein  
 n is 0, 1, 2, 3, or 4;  
 the above aryl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, CF 3 , pyridyl, thiophenyl, NR 6 R 7 , or NR 6 R 7 alkyl, wherein R 6  and R 7  are independently at each occurrence H, alkyl, alkanoyl, benzyl, or phenylC(O)—, wherein the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ;  
 R 3  is halogen, alkoxycarbonyl, phenylalkoxycarbonyl, phenyloxycarbonyl, phenylalkyl, —OC(O)NH(CH 2 ) n phenyl, phenylalkoxy, —OC(O)N(alkyl) (CH 2 ) n phenyl, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein  
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3,or 4;  
 R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is phenyl, naphthyl, pyrrolylalkyl, piperidinylalkyl pyridinylalkyl, pyrimidinylalkyl, phenylthioalkyl, pyrrolyl, piperidinyl, pyridyl, or thiophenylalkyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, phenylalkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 6 R 7 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy.  
 
     
     
         22 . A compound or salt according to  claim 21  wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, benzyloxy, phenethyloxy, benzyl, phenethyl, CN, (C 1 -C 6 )alkanoyl, alkoxy, or phenylC(O)—, or phenylCH 2 C(O)—, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 R 2  is benzyloxy, phenethyloxy, phenpropyloxy, phenyloxy, OH, halogen, phenyl(C 1 -C 4 ) thioalkoxy, —OC(O)NH(CH 2 ) n ,phenyl, OC(O)N(alkyl) (CH 2 ) n phenyl, or dialkylamino, wherein  
 n is 0, 1, 2, 3, or 4;  
 the above aryl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, CF 3 , NR 6 R 7 , or NR 6 R 7 alkyl, wherein 
 R 6  and R 7  are independently at each occurrence H, (C 1 -C 6 )alkyl, acetyl, benzyl, or phenylC(O)—, wherein the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ;  
 R 3  is halogen, alkoxycarbonyl, phenylalkoxycarbonyl, phenyloxycarbonyl, phenylalkyl, phenylalkoxy, phenyloxy, phenylthio, thioalkoxy, phenylthioalkoxy, alkenyl, NR 6 R 7  or alkyl, wherein  
 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy, 
 wherein n is 0, 1, 2, 3,or 4;  
 R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 the phenyl portion of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is phenyl, phenyl(C 1 -C 4 )thioalkyl, pyridyl, or thiophenyl(C 1 -C 4 )alkyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 4 )alkyl, fluoro, chloro, bromo, (C 1 -C 4 )alkoxy, CN, amidinooxime, amidino, CF 3 , or OCF 3 .  
 
     
     
         23 . A compound or salt according to  claim 22  wherein  
       R 5  is substituted with at least one group selected from fluoro, chloro, bromo, and methyl.  
     
     
         24 . A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, solvent, adjuvant or excipient and a compound or salt according to  claim 2 .  
     
     
         25 . A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, solvent, adjuvant or excipient and a compound or salt according to  claim 11 .  
     
     
         26 . A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, solvent, adjuvant or excipient and a compound or salt according to  claim 18 .  
     
     
         27 . A compound of the formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, arylalkoxy, arylalkyl, alkenyl, alkynyl, arylalkynyl, CN, alkanoyl, alkoxy, alkoxyalkyl, haloalkyl, or arylalkanoyl, 
 wherein the aryl portion of arylalkoxy, arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is arylalkoxy, aryloxy, arylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n aryl, —OC(O)N(alkyl) (CH 2 ) n aryl, alkyl, alkoxyalkoxy, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 alkyl, —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy;  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 the aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is arylalkyl, alkyl, aryl, alkoxy, heterocycloalkylalkyl, heteroarylalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 H, CN, OH, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy; 
 wherein R 8  is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 wherein R 5  is alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 provided that when R 2  is benzyloxy, and R 5  is benzyl or methyl, R 1  is not hydrogen.  
 
 
     
     
         28 . A compound or salt according to  claim 27  wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, phenyl(C 1 -C 6 )alkoxy, phenyl(C-C 6 )alkyl, CN, phenyl(C 2 -C 6  alkynyl), C 2 -C 6  alkynyl, alkanoyl, alkoxy, alkoxyalkyl, haloalkyl, or phenyl(C 1 -C 6 )alkanoyl, 
 wherein the phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl.  
 
     
     
         29 . A compound or salt according to  claim 27  wherein  
       R 2  is phenyl(C 1 -C 6 )alkoxy, phenyloxy, phenylthioalkoxy, C 1 -C 8  alkoxy, alkyl, alkoxyalkoxy, —OC(O)NH (CH2) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein 
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 alkyl, —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy.  
 
 
     
     
         30 . A compound or salt according to  claim 27  wherein  
       R 4  is H, (C 1 -C 6 )alkyl, phenyl(C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, haloalkyl-, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein 
 the phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy.  
 
     
     
         31 . A compound or salt according to  claim 27  wherein 
 R 5  is phenyl(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, phenyl, alkoxy, heterocycloalkylalkyl, naphthyl(C 1 -C 6 )alkyl, heteroarylalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy; 
 wherein R 8  is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
   wherein R 9  is alkyl, alkanoyl, arylalkyl and arylalkanoyl;    provided that when R 2  is benzyloxy, and R 5  is benzyl or methyl, R, is not hydrogen.    
     
     
         32 . A compound or salt according to  claim 27  wherein  
       R 1  is H, halogen, alkyl, carboxaldehyde, hydroxyalkyl, phenyl(C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkyl, CN, alkanoyl, alkoxy, ethynyl, alkoxyalkyl, haloalkyl, or phenyl(C 1 -C 6 )alkanoyl, 
 wherein the phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 wherein the alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy;  
 R 2  is phenyl(C 1 -C 6 )alkoxy, phenyloxy, phenylthioalkoxy, C 1 -C 8  alkoxy, alkyl, alkoxyalkoxy, —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 alkyl, —OC(O)NR 6 R 7 , wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , OCF 3 ;  
 R 4  is H, (C 1 -C 6 )alkyl, phenyl(C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 
 the phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF3 , OCF 3 ; and  
 R 5  is phenyl(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, phenyl, alkoxy, piperidinylalkyl, thienylalkyl, naphthyl(C 1 -C 6 )alkyl, heteroarylalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, CF 3 , or OCF 3 ;  
 wherein R 8  is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 wherein R 9  is alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 provided that when R 2  is benzyloxy, and R 5  is benzyl or methyl, R 1  is not hydrogen.  
 
     
     
         33 . A compound or salt according to  claim 32  wherein  
       R 1  is H, halogen), alkyl, haloalkyl, carboxaldehyde, hydroxyalkyl, phenyl(C 1 -C 6 )alkoxy, benzyl, phenethyl, phenpropyl, CN, or phenyl(C 1 -C 6 )alkanoyl, 
 wherein the phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, nitro, CN, CF 3 , OCF 3  or CO 2 H;  
 R 2  is benzyloxy, phenyloxy, phenylthioalkoxy, C 1 -C 8 , —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, or NR 6 R 7 alkyl, wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of arylalkyl, arylalkoxy, or arylalkanoyl is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , OCF 3 ;  
 R 4  is H, (C 1 -C 6 )alkyl, phenyl(C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, wherein  
 
 the phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3 , OCF 3 ; and R 5  is phenyl(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, phenyl, piperidinylalkyl, thienylalkyl, heteroaryl, naphthyl(C 1 -C 6 )alkyl, heteroarylalkyl, or wherein  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, benzyloxy, thioalkoxy, —CO 2 CH 3 , —CO 2 CH 2 CH 3 , —CO2(C 3 -C 5  alkyl), CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, CF 3 , or OCF 3 ; 
 wherein R 8  is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 
 wherein R 9  is alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 provided that when R 2  is benzyloxy, and R 5  is benzyl or methyl, R 1  is not hydrogen.  
 
     
     
         34 . A compound or salt according to  claim 33  wherein  
       R 1  is H, halogen, alkyl or carboxaldehyde;  
       R 2  is benzyloxy, phenyloxy, phenylthioalkoxy, or pyridyl; wherein 
 each of the above is unsubstituted or substituted with 1, 2, or 3, groups that are independently halogen, haloalkyl, or alkyl.  
 
     
     
         35 . A compound or salt according to  claim 33  wherein  
       R 4  is H, (C 1 -C 4 )alkyl, phenyl(C 1 -C 6 )alkoxy, benzyl, phenyethyl, phenpropyl, hydroxy(C 1 -C 6 )alkyl, wherein 
 the phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3 , OCF 3 ; and  
 R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, (C 1 -C 6 )alkyl, phenyl, pyridyl, pyrimidyl, naphthyl(C 1 -C 6 )alkyl, thiophenyl(C 1 -C 6 )alkyl, or pyridyl(C 1 -C 6 )alkyl wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, halogen, alkoxy, benzyloxy, thioalkoxy, —CO 2 CH 3 , —CO 2 CH 2 CH 3 , —CO 2 (C 3 -C 5  alkyl), CF 3 , OCF 3 , CO 2 H, CN, amidinooxime;  
 provided that when R 2  is benzyloxy, and R 5  is benzyl or methyl, R 1  is not hydrogen.  
 
     
     
         36 . A compound or salt according to  claim 33  wherein  
       R 1  is bromo, iodo, or H; and  
       R 5  is benzyl, phenethyl, phenpropyl, phenyl, piperidinylalkyl, thienylalkyl, -CH 2 -pyridyl, or pyridyl, each of which is unsubstituted or substituted with 1, 2, or 3 groups that are independently C 1 -C 4  alkyl, halogen, CF 3 , OCF 3 , —CO 2 CH 3 , C 1 -C 4  alkoxy, —CO 2 CH 3 , —CO 2 CH 2 CH 3 , -QO2 (C 3 -C 5  alkyl), benzyloxy, and amidinooxime.  
     
     
         37 . A compound or salt according to  claim 36  wherein  
       R 2  is benzyloxy, or phenethyloxy; 
 each of the above is unsubstituted or substituted with 1, 2, or 3, groups that are independently fluoro, chloro, bromo, CF 3 , or (C 1 -C 4 )alkyl.  
 
     
     
         38 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein  
       R 1  is halogen, alkyl, carboxaldehyde, hydroxyalkyl, arylalkoxy, arylalkyl, CN, aryl, alkanoyl, alkoxy, alkoxyalkyl, haloalkyl, or arylalkanoyl, 
 wherein the aryl portion of arylalkoxy, arylalkyl, and arylalkanoyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the alkyl portion of the alkyl, hydroxyalkyl, arylalkoxy, arylalkyl, alkanoyl, alkoxy, alkoxyalkyl and arylalkanoyl groups is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, ethoxy or spirocyclopropyl;  
 R 2  is arylalkoxy, arylalkyl, OH, aryloxy, arylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n aryl, —OC(O)N(alkyl) (CH 2 ) n aryl, alkyl, alkoxyalkoxy, NR 6 R 7 , pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, amino, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, NR 6 R 7 alkyl, —SO 2 -phenyl wherein the phenyl is optionally substituted with 1 or 2 groups that are halogen or NO 2 ; or —OC(O)NR 6 R 71  wherein 
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy;  
 R 4  is H, alkyl, arylalkoxy, arylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein the aryl portion of arylalkoxy, arylalkyl is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is arylalkyl, alkyl, aryl, alkoxy, heterocycloalkylalkyl, heteroarylalkyl, heterocycloalkyl, or heteroaryl, wherein each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, OH, CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy;  
 wherein R 5  is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl; and  
 wherein R 9  is alkyl, alkanoyl, arylalkyl and arylalkanoyl;  
 provided that when R 2  is OH, R 4  is methyl and R 5  is phenyl, R 1  is not acetyl.  
 
 
     
     
         39 . A compound or salt according to  claim 38  wherein  
       R 1  is halogen, alkyl, carboxaldehyde, hydroxyalkyl, phenylalkoxy, phenylalkyl, CN, alkanoyl, phenyl, alkoxy, alkoxyalkyl, haloalkyl, or phenylalkanoyl, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the above alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy.  
 
     
     
         40 . A compound or salt according to  claim 38  wherein  
       R 2  is phenylalkoxy, OH, phenyloxy, phenylthioalkoxy, alkoxy, —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2  )phenyl, NR 6 R 7 , alkyl, dialkylamino, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, amino, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, phenyl(C 1 -C 6  alkyl), triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein 
 n is 0, 1, 2, 3, 4, 5 or 6;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, or NR 6 R 7 alkyl, wherein 
 R 6  and R 7  at each occurrence are independently H, alkyl, alkoxy, alkanoyl, phenylalkyl, phenylalkoxy, or phenylalkanoyl, wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy.  
 
 
     
     
         41 . A compound or salt according to  claim 38  wherein  
       R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein 
 the above phenyl groups are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy.  
 
     
     
         42 . A compound or salt according to  claim 38  wherein  
       R 5  is phenylalkyl, (C 1 -C 6 )alkyl, phenyl, naphthyl, alkoxy, piperidinyl, pyrolidinyl, imidazolidinyl, piperazinyl, tetrahydropyranyl, piperidinyl(C 1 -C 6 )alkyl, pyrolidinyl(C 1 -C 6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, piperazinyl(C 1 -C 6 )alkyl, tetrahydropyranyl(C 1 -C 6 )alkyl, pyridyl, pyrimidyl, pyridazyl, pyrazinyl, pyridyl(C 1 -C 6 )alkyl, pyrimidyl(C 1 -C 6 )alkyl, pyridazyl(C 1 -C 6 )alkyl, or pyrazinyl(C 1 -C 6 )alkyl wherein 
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, phenylalkoxycarbonyl, OH, CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy;  
 wherein R 8  and R 9  are independently hydrogen, alkyl, alkanoyl, phenylalkyl and phenylalkanoyl;  
 provided that when R 2  is OH, R 4  is methyl and R 5  is phenyl, R 1  is not acetyl.  
 
     
     
         43 . A compound or salt according to  claim 38  wherein  
       R 1  is halogen, alkyl, phenyl, carboxaldehyde, hydroxyalkyl, phenylalkoxy, phenylalkyl, CN, alkanoyl, alkoxy, alkoxyalkyl, haloalkyl, or phenylalkanoyl, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the above alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy,  
 R 2  is phenylalkoxy, OH, phenyloxy, phenylthio(C 1 -C 4 )alkoxy, alkoxy, phenethyl, —OC(O)NH(CH 2 ) n phenyl, —OC(O)N(alkyl) (CH 2 ) n phenyl, alkyl, alkoxyalkoxy, NR 6 R 7 , pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, tetrahydroquinolinyl, amino, tetrahydroisoquinolinyl, tetrazolyl, pyrazinyl, benzimidazolyl, triazinyl, tetrahydrofuryl, piperidinyl, hexahydropyrimidinyl, thiazolyl, thiophenyl, or CO 2 H, wherein  
 n is 0, 1, 2, or 3;  
 each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, haloalkyl, haloalkoxy, alkyl, thiophenyl, or pyridyl;  
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, benzyl, arylalkoxy, or arylalkanoyl, wherein the aryl portion of each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ;  
 R 4  is H, alkyl, phenylalkoxy, phenylalkyl, hydroxyalkyl, haloalkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein  
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, haloalkyl, or haloalkoxy; and  
 R 5  is benzyl, phenethyl, (C 1 -C 6 )alkyl, phenyl, naphthyl, alkoxy, piperidinyl, pyrolidinyl, imidazolidinyl, piperazinyl, piperidinyl(C 1 -C 6 )alkyl, pyrolidinyl(C 1 -C 6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, pyridyl, pyrimidyl, pyridazyl, pyrazinyl, pyridyl(C 1 -C 6 )alkyl, pyrimidyl(C 1 -C 6 )alkyl, pyridazyl(C 1 -C 6 )alkyl, or pyrazinyl(C 1 -C 6 )alkyl wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, halogen, alkoxy, phenylalkoxy, thioalkoxy, alkoxycarbonyl, phenylalkoxycarbonyl, OH, CO 2 H, CN, amidinooxime, NR 8 R 9 , NR 6 R 7 alkyl, —C(O)NR 6 R 7 , amidino, haloalkyl, or haloalkoxy; 
 wherein R 8  and R 9  are independently hydrogen, alkyl, alkanoyl, phenylalkyl and phenylalkanoyl;  
 provided that when R 2  is OH, R 4  is methyl and R 5  is phenyl, R 1  is not acetyl.  
 
 
     
     
         44 . A compound or salt according to  claim 43  wherein  
       R 1  is halogen, alkyl, carboxaldehyde, hydroxyalkyl, phenylalkoxy, phenyl, benzyl, phenethyl, phenpropyl, phenbutyl, CN, (C 2 -C 6 )alkanoyl, haloalkyl, or phenylCO—, phenylCH 2 CO—, phenylCH 2 CH 2 CO—, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 21 or 3 groups that are independently halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, nitro, CN, haloalkyl, haloalkoxy or CO 2 H;  
 wherein the above alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy,  
 R 2  is benzyloxy, phenethyloxy, phenpropyloxy, OH, phenyloxy, phenylthio(C 1 -C 4 )alkoxy, NR 6 R 7 , (C 1 -C 6 )alkyl, phenethyl, —OC(O)N(CH 3 )CH 2 phenyl, alkoxyalkoxy, pyridyl, pyrimidyl, pyridazyl, pyrazolyl, imidazolyl, pyrrolyl, pyrazinyl, piperidinyl, hexahydropyrimidinyl, benzimidazolyl, or thiophenyl, wherein  
 each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, CF 3 , OCF 3 , (C 1 -C 4 )alkyl, thiophenyl, or pyridyl;  
 R 6  and R 7  are independently at each occurrence H, alkyl, alkoxy, alkanoyl, phenylalkyl, phenylalkoxy, or phenylalkanoyl, wherein the phenyl portion of each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ;  
 R 4  is H, alkyl, benzyloxy, phenethyloxy, phenpropyloxy, benzyl, phenethyl, phenpropyl, hydroxyalkyl, halo (C 1 -C 4 )alkyl, NR 6 R 7 alkyl, alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3  or OCF 3 ; and  
 R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, (C 1 -C 6 )alkyl, phenyl, piperidinyl, pyrolidinyl, imidazolidinyl, piperazinyl, piperidinyl(C 1 -C 6 )alkyl, pyrolidinyl(C 1 -C   6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, pyridyl, pyrimidyl, pyridazyl, pyrazinyl, pyridyl(C 1 -C 6 )alkyl, pyrimidyl(C 1 -C 6 )alkyl, pyridazyl(C 1 -C 6 )alkyl, or pyrazinyl(C 1 -C 6 )alkyl wherein  
 each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, halogen, alkoxy, benzyloxy, thioalkoxy, —CO 2 CH 3 , —CO 2 CH 2 CH 3 , OH, CO 2 H, CN, —CO 2 (C 3 -C 5  alkyl), phenylalkoxycarbonyl, amidinooxime, amidino, CF 3 , CF 2 CF 3 , C 1 CH 2 , or OCF 3 ; provided that when R 2  is OH, R 4  is methyl and R 5  is phenyl, R 1  is not acetyl.  
 
     
     
         45 . A compound or salt according to  claim 44  wherein  
       R 1  is halogen, alkyl, carboxaldehyde, hydroxy(C 1 -C 4 )alkyl, phenylalkoxy, benzyl, phenethyl, —C(O)CH 3 , phenylCO—, or phenylCH2CO—, 
 wherein the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )alkoxy, nitro, CN, CF 3 , or OCF 3 ;  
 wherein the above alkyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, methoxy, or ethoxy;  
 R 2  is benzyloxy, phenethyloxy, phenpropyloxy, OH, phenyloxy, NR 6 R 7 , —S-benzyl, or (C 1 -C 6 )alkyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, CF 3 , OCF 3 , alkyl, thiophenyl, or pyridyl;  
 R 6  and R 7  are independently at each occurrence H, alkyl, alkanoyl, benzyl, benzyloxy, or phenylalkanoyl, wherein the phenyl portion of each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, CF 3 , or OCF 3 ;  
 R 4  is H, alkyl, benzyloxy, phenethyloxy, phenpropyloxy, benzyl, or hydroxyalkyl, wherein  
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, alkoxy, alkyl, nitro, CF 3  or OCF 3 ; and  
 R 5  is benzyl, phenethyl, phenpropyl, phenbutyl, (C 1 -C 6 )alkyl, phenyl, pyridyl, or pyridyl(C 1 -C 4 )alkyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, halogen, (C 1 -C 4 )alkoxy, phenyl(C 1 -C 4 )alkoxy, thio(C 1 -C 4 )alkoxy, alkoxycarbonyl, OH, CO 2 H, CN, amidinooxime, amidino, CF 3 , or OCF 3 .  
 
     
     
         46 . A compound or salt according to  claim 45  wherein  
       R 1  is halogen, alkyl, carboxaldehyde, or hydroxyalkyl;  
       R 2  is benzyloxy, phenethyloxy, phenpropyloxy, OH, phenyloxy, phenylthioalkoxy, or (C 1 -C 6 )alkyl, wherein 
 each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, CF 3 , OCF 3 , alkyl, thiophenyl, or pyridyl;  
 R 4  is H, (C 1 -C 4 )alkyl, benzyloxy, phenethyloxy, wherein  
 the above phenyl groups are unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, hydroxy, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl, nitro, CF 3  or OCF 3 ; and  
 R 5  is benzyl, phenethyl, (C 1 -C 6 )alkyl, phenyl, or pyridyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently (C 1 -C 4 )alkyl, halogen, OH, CO 2 H, CN, (C 1 -C 4 )alkoxy, benzyloxy, —CO 2 CH 3 , —CO2CH 2 CH 3 , —C 2 (C 3 -C 5  alkyl), amidino, thio(C 1 -C 4 )alkoxy, amidinooxime, CF 3 , or OCF 3 .  
 
     
     
         47 . A compound or salt according to  claim 46  wherein  
       R 1  is bromo; and  
       R 5  is benzyl, phenethyl, phenpropyl, phenyl, or pyridyl, each of which is unsubstituted or substituted with 1, 2, or 3 groups that are independently alkyl, OH, halogen, alkoxy, and amidinooxime.  
     
     
         48 . A compound or salt according to  claim 47  wherein  
       R 2  is benzyloxy, or phenethyloxy, each of which is unsubstituted or substituted with 1, 2, or 3 groups that are independently halogen, CF 3 , OCF 3 , or (C 1 -C 4 )alkyl.  
     
     
         49 . A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, solvent, adjuvant or excipient and a compound or salt according to  claim 27 .  
     
     
         50 . A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, solvent, adjuvant or excipient and a compound or salt according to  claim 38 .  
     
     
         51 . A method of treating a TNF mediated disorder, a p38 kinase mediated disorder, inflammation and/or arthritis in a subject, the method comprising treating a subject having or susceptible to such disorder or condition with a therapeutically-effective amount of a compound or salt of any of the preceding claims.  
     
     
         52 . A method according to  claim 51  for treating or preventing inflammation; arthritis, rheumatoid arthritis, spondylarthropathies, gouty arthritis, osteoarthritis, systemic lupus erthematosus, juvenile arthritis; neuroinflammation; pain, neuropathic pain; fever; pulmonary disorders, lung inflammation, adult respiratory distress syndrome, pulmonary sarcoisosis, asthma, silicosis, chronic pulmonary inflammatory disease; cardiovascular disease, arteriosclerosis, myocardial infarction, thrombosis, congestive heart failure, cardiac reperfusion injury; cardiomyopathy; reperfusion injury; renal reperfusion injury; ischemia including stroke and brain ischemia; brain trauma; brain edema; liver disease and nephritis; gastrointestinal conditions, inflammatory bowel disease, Crohn's disease, gastritis, irritable bowel syndrome, ulcerative colitis; ulceratiuve diseases, gastric ulcers; ophthalmic diseases, retinitis, retinopathies, uveitis, ocular photophobia, acute injury to the eye tissue; ophthalmological conditions, corneal graft rejection, ocular neovascularization, retinal neovascularization, neovascularization following injury or infection, diabetic retinopathy, retrolental fibroplasias, neovascular glaucoma; diabetes; diabetic nephropathy; skin-related conditions, psoriasis, eczema, burns, dermatitis, keloid formation, scar tissue formation, angiogenic disorders; viral and bacterial infections, sepsis, septic shock, gram negative sepsis, malaria, meningitis, opportunistic infections, cachexia secondary to infection or malignancy, cachexia secondary to acquired immune deficiency syndrome, (AIDS), AIDS, ARC (AIDS related complex), pneumonia, herpes virus; myalgias due to infection; influenza; endotoxic shock; toxic shock syndrome;’ autoimmune disease, graft vs. host reaction and allograft rejections; treatment of bone resorption diseases, osteoporosis; multiple sclerosis; disorders of the female reproductive system, endometriosis; hemaginomas, infantile hemagionmas, angiofibroma of the nasopharynx, avascular necrosis of bone; benign and malignant tumors/neoplasia, cancer, colorectal cancer, brain cancer, bone cancer, epithelial call-derived neoplasia (epithelial carcinoma), basal cell carcinoma, adenocarcinoma, gastrointestinal cancer, lip cancer, mouth cancer, esophageal cancer, small bowel cancer, stomach cancer, colon cancer, liver cancer, bladder cancer, pancreas cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, skin cancer, squamus cell and/or basal cell cancers, prostate cancer, renal cell carcinoma, and other known cancers that affect epithelial cells throughout the body; leukemia; lymphoma; systemic lupus erthrematosis (SLE); angiogenesis including neoplasia; metastasis; central nervous system disorders, central nervous system disorders having an inflammatory or apoptotic component, Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinal cord injury, and peripheral neuropathy.  
     
     
         52 . A method of treating a p38 kinase or TNF-alpha mediated disorder comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to  claim 1  and at least one pharmaceutically acceptable carrier, adjuvant, solvent or excipient.  
     
     
         53 . A compound according to  claim 27  or  claim 38 , which is 
 1-benzyl-4-(benzyloxy)-3-bromopyridin-2(1Hl)-one;    3-bromo-1-(4-fluorobenzyl)-4-((4-fluorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-dimethylphenyl)-6-methylpyridin-2(11H)-one;    4-(benzyloxy) n -3-bromo-1-(4-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(3-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    4-bromo-2-(2,6-dichlorophenyl)-5-[(2,4-difluorobenzyl)oxy]pyridazin-3(2H)-one;    3-bromo-1-(2,6-dichlorophenyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-4-[(3-methylbenzyl)oxy]pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(3-fluorobenzyl)pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-bromo-6-methylpyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-methoxy-6-methylphenyl)-6-methylpyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    3-bromo-1-(2,6-dichlorophenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2(11H)-one;    4-(benzyloxy)-3-bromo-1-(4-methylbenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(4-chlorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(3-methoxybenzyl)pyridin-2 (1H)-one;    4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1(2H)-yl]methyl}benzoic acid;    4-(benzyloxy)-3-bromo-1-(2-fluorobenzyl)pyridin-2 (1H)-one;    3-bromo-1-(2,6-dimethylphenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(methylthio)benzyl]pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-chloropyridin-2(1H)-one;    4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1(2H) -yl]methyl}-N′-hydroxybenzenecarboximidamide;    methyl 4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1 (2H) -yl]methyl}benzoate;    3-bromo-4-[(3-chlorobenzyl)oxy]-1-(3-fluorobenzyl)pyridin-2(1H) -one;    3-bromo-1-(3-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]pyridin-2(1H)-one;    4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1(2H)-yl]methyl}benzonitrile;    4-(benzyloxy)-3-bromo-1-(2,6-dichlorophenyl)-6-methylpyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(4-bromobenzyl)pyridin-2 (1H)-one;    4-{[3-bromo-4-[(4-fluorobenzyl)oxy]-2-oxopyridin-1(2H)-yl]methyl}benzonitrile;    1-(3-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]-3-iodopyridin-2(1H)-one;    4-bromo-2-(2,6-dichlorophenyl)-5-{[2-(hydroxymethyl)benzyl]oxy}pyridazin-3(21)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    3-bromo-1-(2,4-difluorobenzyl)-4-[(2,4-difluorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-6-methyl-1-(pyridin-2-ylmethyl)pyridin-2(1H)-one; or a pharmaceutically acceptable salt thereof.    
     
     
         54 . A compound according to any one of the preceding claims which is 
 2-benzyl-5-(2,6-dichlorophenyl)-3,4-dimethyl-1,5-dihydro-6H-pyrrolo[3,2-c]pyridin-6-one;    3-bromo-4-[(4-chlorobenzyl)oxy]-1-(4-fluorobenzyl)pyridin-2(1H)-one;    1-benzyl-3-bromo-4-[(4-chlorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-1-(4-chlorobenzyl)-4-[(4-chlorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-4-[(4-chlorobenzyl)oxy]-1-[2-(phenylthio)ethyl]pyridin-2(1H)-one;    3-bromo-4-[(4-chlorobenzyl)oxy]-1-(2-phenylethyl)pyridin-2(1H)-one;    3-bromo-4-hydroxy-1-(4-hydroxybenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(piperidin-3-ylmethyl)pyridin-2(1H)-one hydrochloride;    3-bromo-1-(4-methoxybenzyl)-4-phenoxypyridin-2(111)-one;    1-benzyl-2-oxo-4-phenoxy-1,2-dihydropyridine-3-carbaldehyde;    3-bromo-4-[(4-chlorobenzyl)oxy]-1-(4-methoxybenzyl)pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-1-(3-phenylpropyl)pyridin-2(1H)-one,    4-(benzyloxy)-1-[4-(benzyloxy)benzyl]-3-bromopyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[2-(trifluoromethyl)benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[3-(trifluoromethyl)benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(piperidin-4-ylmethyl)pyridin-2(1H)-one hydrochloride;    1-benzyl-4-(benzylthio)-3-bromopyridin-2(1H)-one;    1-benzyl-3-bromo-4-{[2-(trifluoromethyl)benzyl]oxy}pyridin-2(1H)-one;    1-benzyl-4-[(2,6-dichlorobenzyl)oxy]pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-(hydroxymethyl)pyridin-2(1H)-one;    1-benzyl-3-bromo-4-[(2,6-dichlorobenzyl)oxy]pyridin-2(1H)-one;    1-benzyl-4-[(3-chlorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    1-benzyl-3-bromo-4-[(3-chlorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    1-benzyl-3-bromo-4-[(2-chlorobenzyl)oxy]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-ethylpyridin-2(1H)-one;    4-(benzyloxy)-1-(4-bromobenzyl)pyridin-2(1H)-one;    3-bromo-1-(4-methylbenzyl)-4-[(4-methylbenzyl)oxy]pyridin-2(1H)-one;    methyl 4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1(2H)-yl]methyl }benzoate;    4-(benzyloxy)-3-bromo-1-(2-thien-3-ylethyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(2-thien-2-ylethyl)pyridin-2(1H)-one;    1-benzyl-4-[(3-chlorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-1-(4-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]pyridin-2(1H)-one;    4-(benzyloxy)-1-(3-fluorobenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-1-(2-fluorobenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-methylpyridin-2(1H)-one hydrobromide;    4-(benzyloxy)-3-bromo-1-methylpyridin-2(1H)-one;    3-bromo-1-(3-chlorobenzyl)-4-[(4-chlorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-1-(3-chlorobenzyl)-4-[(4-fluorobenzyl)oxy]pyridin-2(1H)-one;    4-(benzyloxy)-1-(4-chlorobenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(trifluoromethoxy)benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(4-tert-butylbenzyl)pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-6-methylpyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3,5-dibromo-6-methylpyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(trifluoromethyl)benzyl]pyridin-2(1H)-one;    1-benzyl-4-[(2-chlorobenzyl)oxy]pyridin-2(1H)-one;    1-(2-bromobenzyl)-3-[(2-bromobenzyl)oxy]pyridin-2(1H)-one;    methyl 5-chloro-1-(4-chlorobenzyl)-6-oxo-1,6-dihydropyridine-3-carboxylate;    3-benzyl-4-hydroxy-1-(2-phenylethyl)pyridin-2(1H)-one;    5-bromo-1-(2-chloro-6-fluorobenzyl)-3-methylpyridin-2(1H)-one;    1-(2-bromobenzyl)-3-[(2-bromobenzyl)oxy]pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-bromopyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-2-oxo-1,2-dihydropyridine-3-carbaldehyde;    1-benzyl-4-chloro-2-oxo-1,2-dihydropyridine-3-carbaldehyde;    1-benzyl-4-hydroxy-2-oxo-1,2-dihydropyridine-3-carbaldehyde;    1-benzyl-4-(benzyloxy)-3-methylpyridin-2(1H)-one;    4-(benzyloxy)-1-(4-fluorobenzyl)pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3,5-dibromopyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(methylthio)benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-(4-fluorobenzyl)pyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-chloropyridin-2(1H)-one;    3-bromo-1-(4-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]pyridin-2(1H)-one;    5-benzyl-1,2,7-trimethyl-3-(phenylthio)-1,5-dihydro-6H-pyrrolo[3,2-c]pyridin-6-one;    1-benzyl-3-bromo-2-oxo-1,2-dihydropyridin-4-yl methyl(phenyl)carbamate;    1-benzyl-3-bromo-4-(2-phenylethyl)pyridin-2(1H)-one;    1-benzyl-3-bromo-4-(3-phenylpropyl)pyridin-2(1H)-one;    1-benzyl-3-methyl-4-(2-phenylethyl)pyridin-2(1H)-one;    1-benzyl-3-methyl-4-(3-phenylpropyl)pyridin-2(1H)-one;    1-benzyl-4-(benzylthio)-3-methylpyridin-2(1H)-one;    1-benzyl-4-(benzylthio)-3-bromopyridin-2(1H)-one;    (product) 1-benzyl-2-oxo-1,2-dihydropyridin-4-yl methanesulfonate;    3-acetyl-4-hydroxy-6-methyl-1-[choro]phenylpyridin-2(1H)-one;    6-(benzyloxy)-1-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile;    3-benzoyl-6-(benzyloxy)-1-methylpyridin-2(1H)-one;    3-benzyl-6-(benzyloxy)-1-methylpyridin-2(1H)-one;    1-benzyl-4-hydroxypyridin-2(1H)-one;    1-benzyl-2-oxo-1,2-dihydropyridin-4-yl methanesulfonate;    1-benzyl-4-(benzylthio)pyridin-2(1H)-one    1-benzyl-4-(benzylthio)-3-bromopyridin-2(1H)-one;    1-benzyl-2-oxo-1,2-dihydropyridin-4-yl methanesulfonate;    4-amino-1-benzylpyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)pyridin-2(1H)-one;    1-benzyl-4-hydroxypyridin-2(1H)-one;    1-benzyl-2-oxo-1,2-dihydropyridin-4-yl methyl(phenyl)carbamate;    or a pharmaceutically acceptable thereof.    
     
     
         55 . A compound according to any one of the preceding claims that is 
 4-(benzyloxy)-1-(4-methylbenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-bromopyridin-2(1H)-one;    methyl 4-{[4-(benzyloxy)-2-oxopyridin-1(2H)-yl]methyl} benzoate;    methyl-4-{[4-(benzyloxy)-3-bromo-2-oxopyridin-1(2H)-yl]methyl} benzoate;    4-{[4-(benzyloxy)-2-oxopyridin-1(2H)-yl]methyl} benzonitrile;    4-(benzyloxy)-1-(4-tert-butylbenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-1-[4-(trifluoromethyl)benzyllpyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(trifluoromethyl) benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[3-(trifluoromethyl) benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[2-(trifluoromethyl) benzyl]pyridin-2(1H)-one;    4-(benzyloxy)-1-[4-(trifluoromethoxy)benzyl1pyridin-2(1H)-one;    4-(benzyloxy)-3-bromo-1-[4-(trifluoromethoxy) benzyl]pyridin-2(1H)-one;    1-benzyl-4-hydroxy-6-methylpyridin-2(1H)-one;    1-benzyl-6-methyl-2-oxo-1,2-dihydropyridin-4-yl 4-bromobenzenesulfonate;    1-benzyl-3-bromo-4-[(3-chlorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    1-benzyl-6-methyl-2-oxo-1,2-dihydropyridin-4-yl 4-bromobenzenesulfonate;    1-benzyl-3-bromo-4-[(3-chlorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    1-Benzyl-4-[2,6-(dichlorobenzyl)oxy]pyridin-2(1H)-one;    4-[(2,6-dichlororbenzyl)oxy]pyridine-1-oxide;    4-[(2,6-dichlorobenzyl)oxy]pyridine 1-oxide;    1-Benzyl-3-bromo-4-[2,6-(dichlorobenzyl)oxy]pyridin-2(1H)-one;    1-Benzyl-3-bromo-4-[(4-methylbenzyl)oxy]pyridin-2(1H)-one;    1-Benzyl-4-[benzylthio]-3-bromopyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-iodopyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-vinylpyridin-2(1H)-one;    1-benzyl-4-(benzyloxy)-3-ethylpyridin-2(1H)-one;    3-acetyl-4-(benzyloxy)-1-(2-chlorophenyl)-6-methylpyridin-2(1H)-one;    3-acetyl-1-(2-chlorophenyl)-4-hydroxy-6-methylpyridin-2(1H)-one;    1-benzyl-3-bromo-4-hydroxypyridin-2(1H)-one;    1-benzyl-3-bromo-2-oxo-1,2-dihydropyridin-4-yl trifluoromethanesulfonate;    1-benzyl-3-bromo-4-(phenylethynyl)pyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-6-methyl-4-(2-phenylethyl)pyridin-2(1H)-one;    1-(3-fluorobenzyl)-4-hydroxy-6-methylpyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-4-hydroxy-6-methylpyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl trifluoromethanesulfonate;    3-bromo-1-(3-fluorobenzyl)-6-methyl-4-(phenylethynyl)pyridin-2(1H)-one;    3-acetyl-1-(2,6-dichlorophenyl)-4-hydroxy-6-methylpyridin-2(1H)-one;    1-(2,6-dichlorophenyl)-4-hydroxy-6-methylpyridin-2(1H) one;    4-(benzyloxy)-1-(2,6-dichlorophenyl)-6-methylpyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-4-(2-phenylethyl)pyridin-2(1H)-one;    3-bromo 7 1-(3-fluorobenzyl)-4-hydroxypyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-2-oxo-1,2-dihydropyridin-4-yl trifluoromethanesulfonate;    3-bromo-1-(3-fluorobenzyl)-4-(phenylethynyl)pyridin-2(1H)-one;    4-(benzyloxy)-3-ethynyl-1-(3-fluorobenzyl)pyridin-2(1H)-one;    4-(benzyloxy)-1-(3-fluorobenzyl)-3-iodopyridin-2(1H)-one;    4-(benzyloxy)-1-(3-fluorobenzyl)-3-[(trimethylsilyl)ethynyl]pyridin-2(1H)-one;    4-(benzylamino)-3-bromo-1-(3-fluorobenzyl)pyridin-2(1H)-one;    1-(3-fluorobenzyl)-4-hydroxypyridin-2(1H)-one;    4-(benzylamino)-1-(3-fluorobenzyl)pyridin-2(1H)-one;    or a pharmaceutically acceptable salt thereof.    
     
     
         56 . A compound according to any one of the preceding claims which is 
 3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2 (1H)-one;    3-bromo-1-(2,6-dichlorophenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(3-methoxybenzyl)pyridin-2(1H)-one;    3-bromo-1-(2,6-dimethylphenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2 (1H) -one;    3-bromo-4-[(3-chlorobenzyl)oxy]-1-(3-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-1-(pyridin-4-ylmethyl)pyridin-2(1H) -one;    3-bromo-1-(3-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]pyridin-2(1H)-one;    4-{[3-bromo-4-[(4-fluorobenzyl)oxy]-2-oxopyridin-1(2H)-yl]methyl}benzonitrile;    1-(3-fluorobenzyl)-4-[(4-fluorobenzyl)oxy]-3-iodopyridin-2(1H)-one;    3-bromo-4-((4-fluorobenzyl)oxy]-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    3-bromo-1-(2,4-difluorobenzyl)-4-1(2,4-difluorobenzyl)oxy]pyridin-2(1H)-one;    3-bromo-4-[(4-fluorobenzyl)oxy]-6-methyl-1-(pyridin-2-ylmethyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(3-fluorobenzyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;    3-bromo-1-(2,6-dichlorophenyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;    3-bromo-1-(3-fluorobenzyl)-4-[(3-methylbenzyl)oxy]piperidin-2-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;    3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-methoxy-6-methylphenyl)-6-methylpyridin-2(1H)-one; or a pharmaceutically acceptable salt thereof.