IP Library › Granted Patent US 7,067,540

Granted Patent B2

US 7,067,540 · App. 10/367,987 · Granted Jun 27, 2006

Substituted pyridinones

Assignee: Pharmacia Corporation

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Quick Facts

Patent No.: US 7,067,540
App. No.: 10/367,987
Granted: Jun 27, 2006
Kind: B2

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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.

Claims (688)

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein

R 1 is halogen substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, —(C 1 -C 6 )alkyl-N(R)—CO 2 R 30 , haloalkyl, heteroaryl, heteroarylalkyl, —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-NRC(O)NR 16 R 17 , haloalkoxy, alkyl, CN, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxycarbonyl, phenyl, —SO 2 -phenyl wherein the phenyl and —SO 2 -phenyl groups are optionally substituted with 1, 2, or 3 groups that are independently halogen or NO 2 , or —OC(O)NR 6 R 7 , wherein

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 and the nitrogen to which they are attached form a morpholinyl ring;

R 6 and R 7 are independently at each occurrence H, alkyl, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkanoyl, arylalkyl, arylalkoxy, alkoxycarbonyl, —SO 2 -alkyl, OH, alkoxy, alkoxyalkyl, arylalkoxycarbonyl, —(C 1 -C 4 )alkyl-CO 2 -alkyl, heteroarylalkyl, or arylalkanoyl, wherein each is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, OH, SH, heterocycloalkyl, heterocycloalkylalkyl, C 3 -C 7 cycloalkyl, alkoxy, NH 2 , NH(alkyl), N(alkyl)(alkyl), —O-alkanoyl, alkyl, haloalkyl, carboxaldehyde, or haloalkoxy; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, pyrrolidinyl, thiomorpholinyl, thiomorpholinyl S-oxide, thiomorpholinyl S,S-dioxide, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, alkoxycarbonyl, C 1 -C 4 alkoxy, hydroxyl, hydroxyalkyl, dihydroxyalkyl, or halogen;

R 30 is C 1 -C 6 alkyl optionally substituted with 1 or 2 groups that are independently OH, SH, halogen, amino, monoalkylamino, dialkylamino or C 3 -C 6 cycloalkyl;

R 3 is H, 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 , NR 6 R 7 —(C 1 -C 6 )alkyl, 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, 3, 4, or 5 groups that are independently, halogen, alkoxy, alkyl, haloalkyl, or haloalkoxy,

wherein n is 0, 1, 2, 3, 4, 5, or 6; or

R 4 is alkyl unsubstituted or substituted with one or two groups that are independently CO 2 R, —CO 2 —(C 1 -C 6 )alkyl, —C(O)NR 6 R 7 , —C(O)R 6 , —N(R 30 )C(O)NR 16 R 17 , —N(R 30 )C(O)—(C 1 -C 6 )alkoxy, or —NR 6 R 7 , arylalkoxy, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, dihydroxyalkyl, haloalkyl, R 6 R 7 N—(C 1 -C 6 alkyl)-, —NR 6 R 7 , alkoxy, carboxaldehyde, —C(O)NR 6 R 7 , CO 2 R, alkoxyalkyl, or alkoxyalkoxy, wherein the heteroaryl or aryl portions of is the above are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, —CO 2 —(C 1 -C 6 )alkyl, —CONR 6 R 7 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 )alkyl-, nitro, haloalkyl, or haloalkoxy; and

R 5 is H, aryl, arylalkyl, arylthioalkyl, alkyl optionally substituted with 1, 2, or 3 groups that are independently arylalkoxycarbonyl, —NR 8 R 9 , halogen, —C(O)NR 8 R 9 , alkoxycarbonyl, C 3 -C 7 cycloalkyl, or alkanoyl, alkoxy, alkoxyalkyl optionally substituted with one trimethylsilyl group, amino, alkoxycarbonyl, hydroxyalkyl, dihydroxyalkyl, alkynyl, —SO 2 -alkyl, alkoxy optionally substituted with one trimethylsilyl group, heterocycloalkylalkyl, cycloalkyl, cycloalkylalkyl, -alkyl-S-aryl, -alkyl-SO 2 -aryl, heteroarylalkyl, heterocycloalkyl, heteroaryl, or alkenyl optionally substituted with alkoxycarbonyl, wherein

each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, hydroxyalkyl, dihydroxyalkyl, arylalkoxy, thioalkoxy, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 R, CN, OH, hydroxyalkyl, dihydroxyalkyl, amidinooxime, —NR 6 R 7 , —NR 8 R 9 , R 6 R 7 N—(C 1 -C 6 alkyl)-, carboxaldehyde, SO 2 alkyl, —SO 2 H, —SO 2 NR 6 R 7 , alkanoyl wherein the alkyl portion is optionally substituted with OH, halogen or alkoxy, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , amidino, haloalkyl, —(C 1 -C 4 alkyl)-NR 15 C(O)NR 16 R 17 , —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 , —O—CH 2 —O, —O—CH 2 CH 2 —O—, or haloalkoxy; wherein

R 15 is H or C 1 -C 6 alkyl; and

R 18 is C 1 -C 6 alkyl optionally substituted with —O—(C 2 -C 6 alkanoyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl; amino C 1 -C 6 alkyl, mono or dialkylamino C 1 -C 6 alkyl.

2. A compound according to claim 1 , of the formula:

or a pharmaceutically acceptable salt thereof, wherein

R 1 halogen,

R 2 is alkoxy substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, —NR 6 R 7 , haloalkyl, haloalkoxy, alkyl, heteroaryl, heteroarylalkyl, —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-NRC(O)NR 16 R 17 , CN, hydroxyalkyl, dihydroxyalkyl, —OC(O)NR 6 R 7 , or —(C 1 -C 6 )alkyl-N(R)—CO 2 R 30 , wherein

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 and the nitrogen to which they are attached form a morpholinyl ring;

R 6 and R 7 are independently at each occurrence H, alkyl, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, alkanoyl, arylalkyl, arylalkoxy, arylalkoxycarbonyl, or arylalkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, alkoxy, alkyl, OH, SH, carboxaldehyde, haloalkyl, or haloalkoxy; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, thiomorpholinyl S-oxide, thiomorpholinyl S,S-dioxide, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, dihydroxyalkyl, or halogen;

R 30 is C 1 -C 6 alkyl optionally substituted with 1 or 2 groups that are independently OH, SH, halogen, amino, monoalkylamino, dialkylamino or C 3 -C 6 cycloalkyl;

R 4 is alkyl substituted with one or two groups that are independently CO 2 R, —CO 2 alkyl, —C(O)NR 6 R 7 , —C(O)R 6 , —N(R 30 )C(O)NR 16 R 17 , —N(R 30 )C(O)—(C 1 -C 6 )alkoxy, or —NR 6 R 7 , arylalkoxy, heteroaryl, arylalkyl, hydroxyalkyl, dihydroxyalkyl, haloalkyl, —NR 6 R 7 , —C(O)NR 6 R 7 , alkoxy, alkoxyalkyl, or alkoxyalkoxy, wherein

the heteroaryl or aryl portions of the above are unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, hydroxy, alkoxy, alkyl, —CO 2 —(C 1 -C 6 )alkyl, —CONR 6 R 7 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 )alkyl-, nitro, haloalkyl, or haloalkoxy; and

R 5 is H, arylalkyl, alkyl optionally substituted with 1, 2, or 3 groups that are independently arylalkoxycarbonyl, —NR 8 R 9 , halogen, —C(O)NR 8 R 9 , alkoxycarbonyl, or alkanoyl, alkoxyalkyl optionally substituted with one trimethylsilyl group, alkoxycarbonyl, amino, hydroxyalkyl, dihydroxyalkyl, alkenyl optionally substituted with alkoxycarbonyl, alkynyl, —SO 2 -alkyl, aryl, alkoxy optionally substituted with one trimethylsilyl group, 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, hydroxyalkyl, dihydroxyalkyl, thioalkoxy, —SO 2 alkyl, alkoxycarbonyl, arylalkoxycarbonyl, CO 2 R, CN, OH, amidinooxime, NR 8 R 9 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , amidino, hydroxyalkyl, dihydroxyalkyl, carboxaldehyde, —NR 6 R 7 , haloalkyl, —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-CO 2 R, —(C 1 -C 4 alkyl)-C 1 -C 6 alkoxycarbonyl, —(C 1 -C 4 alkyl)-CN, —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 , —O—CH 2 —O—, —O—CH 2 CH 2 —O—, phenyl or haloalkoxy;

R 8 is hydrogen, alkyl, alkanoyl, arylalkyl and arylalkanoyl;

R 9 is alkyl, alkanoyl, arylalkyl, heteroaryl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, and arylalkanoyl.

3. A compound according to claim 2 wherein

R 1 is halogen;

R 2 is C 1 -C 8 alkoxy substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, NR 6 R 7 , haloalkyl, haloalkoxy, hydroxyalkyl, dihydroxyalkyl, alkyl, phenyl, pyridyl, piperidinyl, piperazinyl, —(C 1 -C 6 )alkyl-N(R)—CO 2 R 30 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-NRC(O)NR 16 R 17 , or —OC(O)NR 6 R 7 , wherein

R 6 and R 7 are independently at each occurrence H, alkyl, (C 1 -C 4 )hydroxyalkyl, (C 1 -C 4 )dihydroxyalkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkoxy(C 1 -C 4 )alkyl, (C 1 -C 4 )alkanoyl, phenyl(C 1 -C 4 )alkyl, phenyl(C 1 -C 4 )alkoxy, phenyl(C 1 -C 4 )alkoxycarbonyl, or phenyl(C 1 -C 4 )alkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, OH, SH, C 3 -C 6 cycloalkyl, (C 1 -C 4 )alkoxy, (C 1 -C 4 )alkyl, CF 3 , carboxaldehyde, NH 2 , NH(C 1 -C 6 )alkyl, N(C 1 -C 6 )alkyl(C 1 -C 6 )alkyl, OCF 3 ; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, C 1 -C 4 alkoxycarbonyl, or halogen; and

R 4 is H, alkyl optionally substituted with one or two groups that are independently CO 2 R, —CO 2 alkyl, —C(O)NR 6 R 7 , —C(O)R 6 , —N(R 30 )C(O)NR 16 R 17 , —N(R 30 )C(O)—(C 1 -C 6 )alkoxy, or —NR 6 R 7 , —C(O)NR 6 R 7 , phenyl(C 1 -C 6 )alkoxy, phenyl(C 1 -C 6 )alkyl, hydroxyalkyl, dihydroxyalkyl, haloalkyl, 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, CF 3 , OCF 3 ;

R 5 is phenyl benzyl, phenylethyl optionally substituted with 1, 2, 3, 4, or 5 groups that are independently phenyl C 1 -C 4 alkoxycarbonyl, —NR 8 R 9 , halogen, —C(O)NR 8 R 9 , alkoxycarbonyl, or alkanoyl, phenyl, alkoxy, C 2 -C 6 alkynyl, C 2 -C 6 alkenyl optionally substituted with alkoxycarbonyl, indolyl, quinolinyl, isoquinolinyl, isoindolyl, dihydroindolyl, pyrazolyl, imidazolyl, dihydroisoindolyl, indolon-2-yl, indazolyl, benzimidazolyl, pyridyl, imidazolidine dione, pyrazolyl(C 1 -C 6 alkyl), imidazolyl(C 1 -C 6 alkyl), piperidinyl(C 1 -C 6 )alkyl, pyrrolidinyl(C 1 -C 6 )alkyl, imidazolidinyl(C 1 -C 6 )alkyl, tetrahydroisoquinolinyl(C 1 -C 6 )alkyl, 1H-indazolyl(C 1 -C 6 )alkyl, dihydroindolon-2-yl(C 1 -C 6 alkyl), indolinyl(C 1 -C 6 alkyl), dihydrobenzimidazolyl(C 1 -C 6 alkyl), or dihydrobenzoimidazolonyl(C 1 -C 6 alkyl), pyridyl(C 1 -C 6 )alkyl, pyridazinyl(C 1 -C 6 )alkyl, pyrimidinyl(C 1 -C 6 )alkyl, pyrazinyl(C 1 -C 6 )alkyl, tetrahydrofuryl(C 1 -C 6 )alkyl, naphthyl(C 1 -C 6 )alkyl, morpholinyl(C 1 -C 6 )alkyl, tetrahydrofuryl(C 1 -C 6 )alkyl, thienyl(C 1 -C 6 )alkyl, piperazinyl(C 1 -C 6 )alkyl, indolyl(C 1 -C 6 )alkyl, quinolinyl(C 1 -C 6 )alkyl, isoquinolinyl(C 1 -C 6 )alkyl, isoindolyl(C 1 -C 6 )alkyl, dihydroindolyl(C 1 -C 6 )alkyl, pyrazolyl(C 1 -C 4 )alkyl, imidazolyl(C 1 -C 4 )alkyl, dihydroisoindolyl(C 1 -C 6 )alkyl, indoon-2-yl(C 1 -C 6 )alkyl, indolon-2-yl(C 1 -C 6 )alkyl, or morpholinyl 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 6 alkyl, halogen, C 1 -C 6 alkoxy, phenyl C 1 -C 6 alkoxy, C 1 -C 6 thioalkoxy, C 1 -C 6 alkoxycarbonyl, CO 2 R, CN, —SO 2 (C 1 -C 6 )alkyl, amidinooxime, NR 8 R 9 , —NR 6 R 7 , NR 6 R 7 C 1 -C 6 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , amidino, C 1 -C 4 haloalkyl, hydroxy C 1 -C 6 alkyl, C 1 -C 6 dihydroxyalkyl, or C 1 -C 4 haloalkoxy; wherein

R 8 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 6 alkyl and phenyl C 1 -C 6 alkanoyl; and

R 9 is aminoalkyl, mono C 1 -C 6 alkylamino C 1 -C 6 alkyl, di C 1 -C 6 alkylamino C 1 -C 6 alkyl, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 6 alkyl, indazolyl, and phenyl C 1 -C 6 alkanoyl.

4. A compound according to claim 3 , wherein

R 1 is halogen;

R 2 is C 1 -C 8 alkoxy substituted with 1, 2, 3, 4, or 5 groups that are independently halogen, —(C 1 -C 6 )alkyl-N(R)—CO 2 R 30 , NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , (C 1 -C 4 )haloalkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-NRC(O)NR 16 R 17 , (C 1 -C 4 )haloalkoxy, hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, (C 1 -C 6 )alkyl, pyridyl, or R 6 R 7 N—(C 1 -C 6 alkyl)-.

5. A compound according to claim 4 , wherein

R 5 is phenyl, benzyl, or phenylethyl, wherein

each of the above is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, benzyloxy, hydroxyalkyl, dihydroxyalkyl, thioalkoxy, —CO 2 (C 1 -C 5 alkyl), CO 2 R, CN, amidinooxime, —NR 8 R 9 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , amidino, CF 3 , or OCF 3 ;

R 8 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 6 alkyl and phenyl C 1 -C 6 alkanoyl; and

R 9 is aminoalkyl, mono C 1 -C 6 alkylamino C 1 -C 6 alkyl, di C 1 -C 6 alkylamino C 1 -C 6 alkyl, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 4 alkyl, indazolyl, and phenyl C 1 -C 4 alkanoyl.

6. A compound according to claim 4 , wherein

R 5 is phenyl, benzyl, or phenylethyl, which is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently alkyl, halogen, alkoxy, benzyloxy, thioalkoxy, —CO 2 (C 1 -C 5 alkyl), CO 2 R, CN, amidinooxime, —NR 8 R 9 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —(C 1 -C 4 )—C(O)NR 6 R 7 , amidino, CF 3 , or OCF 3 ; wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 4 alkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkyl, C 1 -C 4 alkanoyl, phenyl C 1 -C 4 alkyl, phenyl C 1 -C 4 alkoxy, or phenyl C 1 -C 4 alkanoyl, wherein each is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, CF 3 , or OCF 3 ; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen;

R 8 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 6 alkyl and phenyl C 1 -C 6 alkanoyl; and

R 9 is aminoalkyl, mono C 1 -C 6 alkylamino C 1 -C 6 alkyl, di C 1 -C 6 alkylamino C 1 -C 6 alkyl, C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, phenyl C 1 -C 4 alkyl, indazolyl, and phenyl C 1 -C 4 alkanoyl.

7. A compound according to claim 6 , wherein

R 5 is phenyl, benzyl or phenethyl, wherein each is optionally substituted with 1, 2, 3, 4, or 5 groups that are independently C 1 -C 6 alkyl, —NR 6 R 7 , —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 8 R 9 , halogen, C 1 -C 6 alkoxy, CO 2 R, —(C 1 -C 4 alkyl)-CO 2 R, C 1 -C 6 thioalkoxy, amidinooxime, C 1 -C 6 alkoxycarbonyl, —(C 1 -C 4 alkyl)-C 1 -C 6 alkoxycarbonyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, —(C 1 -C 4 alkyl)-CN, CN, phenyl C 1 -C 6 alkoxy, OH, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, R 6 R 7 N—(C 1 -C 6 alkyl)-, —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 , amidinooxime, —SO 2 (C 1 -C 6 alkyl), —O—CH 2 —O—, —O—CH 2 CH 2 —O—, phenyl C 1 -C 4 alkoxy, or phenyl; wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 4 alkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, C 1 -C 4 alkanoyl, or C 1 -C 4 alkoxy, each of which is optionally substituted with 1, 2, or 3 groups that are independently halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, OH, CF 3 , or OCF 3 .

8. A compound according to claim 7 , wherein

R 5 is phenyl, benzyl or phenethyl, each of which is unsubstituted or substituted with 1, 2, 3, 4, or 5 groups that are independently CN, halogen, C 1 -C 4 alkoxy, CF 3 , OCF 3 , C 1 -C 4 alkyl, —NR 8 R 9 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, or —C(O)NR 6 R 7 , wherein

9. A compound according to claim 4 , wherein

the R 5 group is of the formula:

wherein

Z 1 and Z 2 are independently H, halogen, C 1 -C 4 alkyl, or CO 2 R; and

Z is —C(O)NR 6 R 7 , —(C 1 -C 4 )alkyl-C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —NR 8 R 9 , C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkyl, CO 2 R, or halogen; wherein

R 6 and R 7 at each occurrence are independently H, OH, C 1 -C 6 alkyl, amino C 1 -C 4 alkyl, NH(C 1 -C 6 alkyl)alkyl, N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl)C 1 -C 6 alkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, or —SO 2 (C 1 -C 6 alkyl) each of which is optionally substituted with 1, 2, or 3 groups that are independently halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, OH, CF 3 , or OCF 3 ;

R 6 , R 7 , and the nitrogen to which they are attached form a piperidinyl, pyrrolidinyl, piperazinyl, or a morpholinyl, thiomorpholinyl, ring optionally substituted with 1 or 2 groups that are independently alkyl, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen; and

R 18 is C 1 -C 6 alkyl optionally substituted with —O—(C 2 -C 6 alkanoyl, C 1 -C 6 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl; amino C 1 -C 6 alkyl, mono or dialkylamino C 1 -C 6 alkyl.

10. A compound according to claim 4 , wherein

R 5 is phenyl, which is optionally substituted with 1, 2, 3, 4, or 5 groups that are independently C 1 -C 4 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , NR 6 R 7 (C 1 -C 6 alkyl), C 1 -C 6 hydroxyalkyl, dihydroxyalkyl, halogen, C 1 -C 4 alkoxy, CO 2 R, OH, C 1 -C 6 alkoxycarbonyl, CF 3 , —(C 1 -C 4 alkyl)-NR 15 C(O)NR 16 R 17 , —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 ; wherein

R 15 is H or C 1 -C 6 alkyl;

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 , and the nitrogen to which they are attached form a morpholinyl ring; and

11. A compound according to claim 10 , wherein

R 5 is of the formula:

Z 1 is H, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

Z 2 is C 1 -C 4 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , NR 6 R 7 (C 1 -C 6 alkyl), C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, halogen, C 1 -C 4 alkoxy, CO 2 R, OH, C 1 -C 6 alkoxycarbonyl, or C 1 -C 4 haloalkyl;

Z 3 is H, C 1 -C 4 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , NR 6 R 7 (C 1 -C 6 alkyl), C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, halogen, C 1 -C 4 alkoxy, CO 2 R, OH, C 1 -C 6 alkoxycarbonyl, or C 1 -C 4 haloalkyl;

wherein

R 6 and R 7 at each occurrence are independently H, OH, C 1 -C 6 alkyl, amino C 1 -C 4 alkyl, NH(C 1 -C 6 alkyl)alkyl, N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl)C 1 -C 6 alkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, —SO 2 (C 1 -C 6 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1 -C 6 alkyl), —SO 2 N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), or C 1 -C 6 alkanoyl, each of which is optionally substituted with 1, 2, or 3 groups that are independently halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, OH, CF 3 , or OCF 3 .

12. A compound according to claim 11 , wherein

R 5 is of the formula:

wherein

Z 1 is H, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

R 6 and R 7 at each occurrence are independently H, OH, C 1 -C 6 alkyl, amino C 1 -C 4 alkyl, NH(C 1 -C 6 alkyl)alkyl, N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl)C 1 -C 6 alkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, —SO 2 (C 1 -C 6 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1 -C 6 alkyl), —SO 2 N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), or C 1 -C 6 alkanoyl, each of which is optionally substituted with 1, 2, or 3 groups that are independently halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, OH, CF 3 , or OCF 3 .

13. A compound according to claim 11 , wherein

R 5 is of the formula:

wherein

Z 1 is H, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

R 6 and R 7 at each occurrence are independently H, OH, C 1 -C 6 alkyl, amino C 1 -C 4 alkyl, NH(C 1 -C 6 alkyl)alkyl, N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl)C 1 -C 6 alkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, —SO 2 (C 1 -C 6 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1 -C 6 alkyl), —SO 2 N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), or C 1 -C 6 alkanoyl, each of which is optionally substituted with 1, 2, or 3 groups that are independently halogen, OH, SH, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, OH, CF 3 , or OCF 3 .

14. A compound according to claim 10 , wherein

R 5 is either

wherein

Z 1 is H, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

Z 2 is C 1 -C 4 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , NR 6 R 7 (C 1 -C 6 alkyl), C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, halogen, C 1 -C 4 alkoxy, CO 2 R, C 1 -C 6 alkoxycarbonyl, —(C 1 -C 4 alkyl)-NR 15 C(O)NR 16 R 17 , or —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 ;

Z 3 is H, C 1 -C 4 alkyl, —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , NR 6 R 7 (C 1 -C 6 alkyl), C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, halogen, C 1 -C 4 alkoxy, CO 2 R, C 1 -C 6 alkoxycarbonyl, —(C 1 -C 4 alkyl)-NR 15 C(O)NR 16 R 17 , or —(C 1 -C 4 alkyl)-NR 15 C(O)R 18 ;

R 6 , R 7 , and the nitrogen to which they are attached form a piperidinyl, pyrrolidinyl, piperazinyl, or a morpholinyl ring optionally substituted with 1 or 2 groups that are independently alkyl, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen;

R 1 is H or C 1 -C 6 alkyl;

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 , and the nitrogen to which they are attached form a morpholinyl ring;

15. A compound according to claim 14 , wherein

R 5 is of the formula:

Z 1 is H, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

R 15 is H or C 1 -C 6 alkyl;

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 , and the nitrogen to which they are attached form a morpholinyl ring;

16. A compound according to claim 14 , wherein

R 5 is of the formula:

wherein

Z 1 is H, halogen, C 1 -C 4 alkyl C 1 -C 4 haloalkyl, C 1 -C 4 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, or C 1 -C 4 alkoxy; and

R 6 , R 7 , and the nitrogen to which they are attached form a piperidinyl, pyrrolidinyl, piperazinyl, or a morpholinyl ring, each of which is optionally substituted with 1 or 2 groups that are independently alkyl, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen;

R 15 is H or C 1 -C 6 alkyl;

R 16 and R 17 are independently H or C 1 -C 6 alkyl; or

R 16 , R 17 , and the nitrogen to which they are attached form a morpholinyl ring;

17. A compound according to claim 12 , wherein

Y 2 , Y 4 , and Y are independently halogen; and

Y 1 and Y 3 are both hydrogen.

18. A compound according to claim 17 , wherein

R 5 is

X 1 and X 2 are independently H, methyl, NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, or —(C 1 -C 4 alkyl)-morpholinyl; and

X a and X e are independently halogen, NH 2 , NH(C 1 -C 6 alkyl), N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), methyl, or hydrogen.

19. A compound according to claim 18 , wherein

one of X b and X c is hydrogen and the other is —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , —SO 2 NR 6 R 7 , or halogen; where

R 6 and R 7 are independently at each occurrence H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl, C 1 -C 6 alkoxycarbonyl, OH, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, —(C 1 -C 4 )alkyl-CO 2 -alkyl, pyridyl C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, benzyl, phenyl C 1 -C 6 alkoxy, or phenyl C 1 -C 6 alkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, piperidinyl C 1 -C 6 alkyl, morpholinyl C 1 -C 6 alkyl, piperazinyl C 1 -C 6 alkyl, OH, SH, NH 2 , NH(alkyl), N(alkyl)(alkyl), —O—C 1 -C 4 alkanoyl, C 1 -C 4 alkyl, CF 3 , or OCF 3 ; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen.

20. A compound according to claim 19 , wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl, C 1 -C 6 alkoxycarbonyl, OH, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, —(C 1 -C 4 )alkyl-CO 2 -alkyl, pyridyl C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, benzyl, phenyl C 1 -C 6 alkoxy, or phenyl C 1 -C 6 alkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, piperidinyl C 1 -C 6 alkyl, morpholinyl C 1 -C 6 alkyl, piperazinyl C 1 -C 6 alkyl, OH, NH 2 , NH(alkyl), N(alkyl)(alkyl), —O—C 1 -C 4 alkanoyl, C 1 -C 4 alkyl, CF 3 , or OCF 3 .

21. A compound according to claim 20 , wherein

X a is hydrogen, methyl, fluorine, or chlorine;

X c and X d are both hydrogen;

X b is —NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 ; wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 6 alkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 4 dihydroxyalkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl, or C 1 -C 6 alkanoyl, wherein each of the above is optionally substituted with 1, 2, or 3 groups that are independently OH, SH, halogen, or C 3 -C 6 cycloalkyl.

22. A compound according to claim 17 , wherein

R 5 is

X a is H, fluoro, chloro, or methyl;

X e is hydrogen, halogen, or methyl; and

X b is H;

X d is H or halogen.

23. A compound according to claim 22 , wherein

X c is —SO 2 NR 6 R 7 , or halogen; wherein

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen; or

X c is fluoro, chloro, —NH 2 , —NH(C 1 -C 6 alkyl), —N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1 -C 6 alkyl), —SO 2 N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), or piperazinyl, wherein the piperazinyl group is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen.

24. A compound according to claim 22 , wherein

X c is —C(O)NR 6 R 7 , —(C 1 -C 6 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , or R 6 R 7 N—(C 1 -C 6 alkyl)-; wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl, C 1 -C 6 alkoxycarbonyl, OH, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, C 1 -C 6 dihydroxyalkyl, —(C 1 -C 4 )alkyl-CO 2 -alkyl, pyridyl C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, benzyl, phenyl C 1 -C 6 alkoxy, or phenyl C 1 -C 6 alkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, piperidinyl C 1 -C 6 alkyl, morpholinyl C 1 -C 6 alkyl, piperazinyl C 1 -C 6 alkyl, OH, —NH 2 , —NH(alkyl), —N(alkyl)(alkyl), —O—C 1 -C 4 alkanoyl, C 1 -C 4 alkyl, CF 3 , or OCF 3 ; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, thiomorpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen.

25. A compound according to claim 24 , wherein R 6 is hydrogen; and R 7 is C 1 -C 6 alkyl or C 1 -C 6 alkanoyl, each of which is optionally substituted with 1, 2, or 3 groups that are independently NH 2 , NH(C 1 -C 6 alkyl), N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), OH, SH, cyclopropyl, or C 1 -C 4 alkoxy.

26. A compound according to claim 25 , wherein X c is —C(O)NR 6 R 7 .

27. A compound according to claim 25 , wherein X c is NR 6 R 7 , or R 6 R 7 N—(C 1 -C 6 alkyl)-.

28. A compound according to claim 1 , wherein

X a is hydrogen;

two of X b , X c , and X d are hydrogen and the other is —C(O)NR 6 R 7 , —(C 1 -C 6 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)- or —CO 2 —(C 1 -C 6 )alkyl; wherein

R 6 and R 7 are independently at each occurrence H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy C 1 -C 6 alkyl, C 1 -C 6 alkoxycarbonyl, OH, C 1 -C 6 hydroxyalkyl, C 1 -C 6 dihydroxyalkyl, —(C 1 -C 4 )alkyl-CO 2 -alkyl, pyridyl C 1 -C 6 alkyl, C 1 -C 6 alkanoyl, benzyl, phenyl C 1 -C 6 alkoxy, or phenyl C 1 -C 6 alkanoyl, wherein each of the above is unsubstituted or substituted with 1, 2, or 3 groups that are independently, halogen, C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, piperidinyl C 1 -C 6 alkyl, morpholinyl C 1 -C 6 alkyl, piperazinyl C 1 -C 6 alkyl, OH, NH 2 , NH(alkyl), N(alkyl)(alkyl), —O—C 1 -C 4 alkanoyl, C 1 -C 4 alkyl, CF 3 , or OCF 3 ; or

R 6 , R 7 , and the nitrogen to which they are attached form a morpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl ring which is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen; and

X e is hydrogen, methyl, C 1 -C 2 alkoxy, or halogen.

29. A compound according to claim 28 , wherein

X b is —C(O)NR 6 R 7 , —(C 1 -C 6 alkyl)-C(O)NR 6 R 7 , —NR 6 R 7 , or R 6 R 7 N—(C 1 -C 6 alkyl)- wherein

R 6 is hydrogen or C 1 -C 4 alkyl;

R 7 is OH, C 1 -C 6 alkyl or C 1 -C 6 alkanoyl, wherein the alkyl and alkanoyl groups substituted with 1, 2, or 3 groups that are independently NH 2 , NH(C 1 -C 6 alkyl), N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), C 3 -C 6 cycloalkyl, OH, or C 1 -C 4 alkoxy.

30. A compound according to claim 1 , wherein

X a is halogen or methyl;

X b is H, —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , or —CO 2 —(C 1 -C 6 )alkyl;

X c is —NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, —C(O)NR 6 R 7 , halogen, —CO 2 —(C 1 -C 6 )alkyl, NH 2 , NH(C 1 -C 6 alkyl), N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1 -C 6 alkyl), —SO 2 N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), or piperazinyl, wherein the piperazinyl group is optionally substituted with 1 or 2 groups that are independently C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, hydroxy C 1 -C 4 alkyl, C 1 -C 4 dihydroxyalkyl, or halogen;

X d is hydrogen;

X e is H, methyl, NH 2 , NH(C 1 -C 6 alkyl) or N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl).

31. A compound according to claim 38 , wherein X 1 , X 2 , X a , X b , X c , X d , and X e are independently selected from H, OH, halogen, CF 3 , alkyl, OCF 3 , pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, thienyl, furyl, pyrrolyl, piperidinyl, piperazinyl, or C 3 -C 7 cycloalkyl, wherein each of the above is optionally substituted with —NR 6 R 7 , —C(O)NR 6 R 7 , —(C 1 -C 4 alkyl)-C(O)NR 6 R 7 , R 6 R 7 N—(C 1 -C 6 alkyl)-, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, or halogen.

32. A compound which is

(−)-3-[3-bromo-4[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide

or a pharmaceutically acceptable salt thereof.

33. A compound which is

(+)-3-[3-bromo-4[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide

or a pharmaceutically acceptable salt thereof.

34. A compound of claim 1 which is

3-Chloro-4-(2,4-difluorobenzyloxy)-6-methyl-1-(1H-pyrazol-4-ylmethyl-1H-pyridin-2-one;

2-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzonitrile;

3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzonitrile;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzonitrile;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzamide;

Methyl 4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzate;

Methyl 3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzate;

3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzamide;

2-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-methyl}benzamide;

1-[2-(aminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-1(2H)-yl-one;

3-bromo-1-[3-(bromomethyl)benzyl]-4[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-bromo-1-[4-(bromomethyl)benzyl]-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(aminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-(aminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((morpholin-4-yl)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((dimethylamino)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((isopropylamino)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((piperidin-1-yl)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((2-hydroxyethyl)amino)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((bis(2-hydroxyethyl)amino)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-((piperazin-1-yl)methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzoic acid;

1-[3-((1-oxoethyl)aminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-(carbomethoxyaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-(methylsulfonylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-(glycolylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[3-(aminocarbonylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(isopropylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(morpholin-4-ylmethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(dimethylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(piperidin-1-ylmethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4([bis(2-hydroxyethyl)amino]methyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-((2-etholyl)aminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-piperazin-1-ylmethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(methoxycarbonylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(acetylaminomethylbenzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(methylsulfonylaminomethyl)benzyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-[4-(carbamylaminomethyl)benzyl]-3-bromo-4-[(2,4-diflorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

4-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzoyl)piperazine-1-carboxamide;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-2-methoxyacetamide;

methyl 2-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzylcarbamoyl)acetate;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-hydroxy-2-methylpropanamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-1-hydroxycyclopropanecarboxamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-aminoacetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-hydroxyacetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-(1-oxoethylamino)acetamide;

1-{4-[(4-acetylpiperazin-1-yl)carbonyl]benzyl}-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(4-{[4-(methylsulfonyl)piperazin-1-yl]carbonyl}benzyl)pyridin-2(1H)-one;

3-Bromo-4-[(2,4-diflurorbenzyl)oxy]-1-[3-(hydroxymethyl)phenyl]-6-methylpyridin-2(1H)-one;

Methyl-4-[3-bromo-4-[(difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1-(2H)-yl]benzoate;

or pharmaceutically acceptable salts thereof.

35. A comyound of claim 1 which is

4-[3-bromo-4-[(difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzoic acid;

4-(Benzyloxy)-1-(3-fluorobenzyl)-3-(trifluoromethyl)pyridin-2(1H)-one;

4-{[3-bromo-4-[(2,4-difluorobenzyloxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzoic acid;

3-Bromo-4-[(2,4-diflurobenzyl)oxy]-1-[4-(hydroxymethyl)benzyl]-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-diflurobenzyl)oxy]-1-[4-(1-hydroxy-1-methylethyl)benzyl]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-diflurobenzyl)oxy]-6-methyl-1-{4-[(methylamino)methyl]benzyl}pyridin-2(1H)-one;

4-[(2,4-diflurobenzyl)oxy]-1-(4-methoxybenzyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-diflurobenzyl)oxy]-1-(4-methoxybenzyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-diflurobenzyl)oxy]-1-(4-hydroxybenzyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1{4-[(4-hydroxy-4-methylpiperidin-1-yl)carbonyl]benzyl}-6-methylpyridin-2(1H)-one;

4-{[3-bromo-4-[(2,4-difluorobenzyloxy]-6-methyl-2-oxypyridin-1(2H)-yl]methyl}-N-(2-hydroxy-2-methylpropyl)benzamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1{4-[(4-hydroxypiperidin-1-yl)carbonyl]benzyl}-6-methylpyridin-2(1H)-one;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)benzamide;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((aminoethyl)aminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((aminopropyl)aminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-(hydroxyaminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((aminomethyl)aminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-(dimethylaminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-(diethanol-2-ylaminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-(isoyropylaminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((dimethylaminoethyl)aminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((methoxyethyl)aminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((ethanol-2-yl)methylaminocarbonyl)benzyl]pyridin-2(1H)-one;

3-bromo-4-(2,4-difluorophenoxy)-6-methyl-1-[4-((methoxyethyl)methylaminocarbonyl)benzyl]pyridin-2(1H)-one;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-(2-hydroxyethyl)benzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-aminoethyl)benzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(3-aminopropyl)benzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-hydroxybenzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-methylbenzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,N-dimethylbenzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,N-bis(2-hydroxyethyl)benzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-isopropylbenzamide;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzamide;

Methyl-4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzoate;

3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-methylbenzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N-(2-aminoethyl)benzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N-(3-aminopropyl)benzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N-hydroxybenzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N,N-dimethylbenzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N-(2-hydroxyethyl)benzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N,N-bis(2-hydroxyethyl)benzamide;

3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)-N-isopropylbenzamide;

N-(3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)methyl}benzyl]-2-methoxyacetamide;

N-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-aminoacetamide;

N-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-(1-oxoethylamino)acetamide;

N-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-3-oxobutanamide;

N-(3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-2-hydroxy-2-methylpropanamide;

N-(3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-1-hydroxycyclopropanecarboxamide;

N′-(3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-N,N-dimethylurea;

1-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-3-methylurea;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzoic acid;

Ethyl 3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzoate;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-methylbenzamide;

or pharmaceutically acceptable salts thereof.

36. A compound of claim 1 which is

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-aminoethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(3-aminopropyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-hydroxybenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,N-dimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-hydroxyethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-isopropylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-(dimethylamino)ethyl)-benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-(dimethylamino)ethyl)-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-hydroxyethyl)-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)-N-methylbenzamide; 3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzamide;

3-[3-chloro-4-[(2,4-difluorobenzy)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzoic acid;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-[3-(hydroxymethyl)phenyl]-6-methylpyridin-2(1H)-one;

1-[3-(aminomethyl)phenyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

N-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzyl}methanesulfonamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)benzyl)acetamide;

methyl 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)benzylcarbamate;

N-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzyl}-2-methoxyacetamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)benzyl)-2-aminoacetamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)benzyl)-2-hydroxyacetamide;

N′-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzyl}-N,N-dimethylurea;

1-(3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)benzyl)-3-methylurea;

N-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzyl}urea;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{3-[(dimethylamino)methyl]phenyl}-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyloxy]-6-methyl-1-(2-morpholin-4-ylethyl)pyridin-2(1H)-one;

3-bromo-1-(4-bromo-2,6-difluorophenyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(2,4,6-trifluorophenyl)pyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(2,4,6-trifluorophenyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-1-(2,4,6-trifluorophenyl)pyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-1-(2,4,6-trifluorophenyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluoro-4-morpholin-4-ylphenyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[2,6-difluoro-4-(4-methylpiperazin-1-yl)phenyl]-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-[2,6-difluoro-4-(4-methylpiperazin-1-yl)phenyl]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[4-(dimethylamino)-2,6-difluorophenyl]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{2,6-difluoro-4-[(2-hydroxyethyl)(methyl)amino]phenyl}-6-methylpyridin-2(1H)-one;

3-bromo-1-(3,5-dibromo-2,6-difluoro-4-hydroxyobenyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

2-{4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3,5-difluorophenoxyl}acetamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[2,6-difluoro-4-(2-hydroxyethoxy)phenyl]-6-methypyridin-2(1H)-one;

3-bromo-1-(2,6-difluorophenyl)-4-{[4-fluoro-2-(hydroxymethyl)benzyl]oxy}-6-methylpyridin-2(1H)-one;

3-chloro-1-(2,6-difluorophenyl)-4-{[4-fluoro-2-(hydroxymethyl)benzyl]oxy}-6-methylpyridin-2(1H)-one;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-2-methyl)-N-(2-morpholin-4-ylethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)-2-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,N,2-trimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-hydroxyethyl)-2-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,2-dimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-hydroxyethyl)-N,2-dimethylbenzamide;

4-(2,4-difluorobenzyloxy)-1-(3-(4-methylpiperazin-1-yl)carbonyl-2-methylphenyl)-3-bromo-6-methylpyridin-2(1H)-one;

4-(2,4-difluorobenzyloxy)-1-(3-(morpholin-4-yl)carbonyl-2-methylphenyl)-3-bromo-6-methylpyridin-2(1H)-one;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)-N,2-dimethylbenzamide;

or pharmaceutically acceptable salts thereof.

37. A compound of claim 1 which is

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-2-methylbenzamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[3-(hydroxymethyl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

3-[3-chloro-4-[(2,4-difluorobenzyhoxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-(2-methoxyethyl)-2-methylbenzamide;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,2-dimethylbenzamide;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-(2-hydroxyethyl)-2-methylbenzamide;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-2-methylbenzamide;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-dimethylphenyl)-6-methylpyridin-2(1H)-one;

3-Bromo-1-(2,6-dimethylphenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-Bromo-1-(2,6-dimethylphenyl)-6-methyl-4-[(2,4,6-trifluorobenzyl)oxy]pyridin-2(1H)-one;

3-Bromo-4-[(2,6-difluorobenzyl)oxy]-1-(2,6-dimethylphenyl)-6-methylpyridin-2(1H)-one;

3-Bromo-1-(2,6-dichlorophenyl)-4-[(4-fluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-Bromo-1-(2,6-dichlorophenyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-Bromo-1-(2,6-dichloroyhenyl)-4-[(2,6-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-methoxy-6-methylphenyl)-6-methylpyridin-2(1H)-one;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3,5-dichlorobenzenesulfonamide;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-5-iodo-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-[2-(dimethylamino)-4,6-difluorophenyl]-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-{2,4-difluoro-6-[(2-hydroxyethyl)(methyl)amino]phenyl}-6-methylpyridin-2(1H)-one;

2-({[3-Bromo-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzonitrile;

4-{[2-(Aminomethyl)-4-fluorobenzyl]oxy}-3-bromo-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one trifluoroacetate;

N-[2-({[3-bromo-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzyl]urea;

Methyl 2-({[3-bromo-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

N-[2-({[3-bromo-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzyl]-2-hydroxyacetamide;

Ethyl 2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

Isobutyl 2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

Cycloyronylmethyl 2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one trifluoroacetate;

1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one hydrochloride;

1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one trifluoroacetate;

1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one hydrochloride;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(1H-indazol-5-ylmethyl)-6-methylpyridin-2(1H)-one trifluoroacetate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-{[2-(methylthio)pyrimidin-4-yl]methyl}pyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-{[2-(methylsulfonyl)pyrimidin-4-yl]methyl}pyridin-2(1H)-one;

4-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrimidine-2-carbonitrile trifluoroacetate;

4-{[2-(Aminomethyl)-4-fluorobenzyl]oxy}-3-bromo-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-[(2-methoxypyrimidin-4-yl)methyl]-6-methylpyridin-2(1H)-one trifluoroacetate;

Methyl 4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrimidine-2-carboxylate trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-[(2-hydroxypyrimidin-4-yl)methyl]-6-methylpyridin-2(1H)-one trifluoroacetate;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrimidine-2-carboxamide trifluoroacetate;

Methyl (4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrimidin-2-yl)methylcarbamate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-[(5-methylpyrazin-2-yl)methyl]pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyrazin-2-ylmethyl)pyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-{[5-(hydroxymethyl)pyrazin-2-yl]methyl}-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-{5-[(dimethylamino)methyl]pyrazin-2-yl}methyl)-6-methylpyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-[(5-{[(2-hydroxyethyl)-(methyl)amino]methyl}pyrazin-2-yl)methyl]-6-methylpyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-({5-[(4-methylpiperazin-1-yl)carbonyl]pyrazin-2-yl}methyl)pyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-({5-[(4-methylpiperazin-1-yl)carbonyl]pyrazin-2-yl}methyl)pyridin-2(1H)-one;

5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)-N-methylpyrazine-2-carboxamide;

5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2,3-dihydroxypropyl)pyrazine-2-carboxamide;

5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)pyrazine-2-carboxamide;

or pharmaceutically acceptable salts thereof.

38. A compound of claim 1 which is

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-{[5-(methoxymethyl)pyrazin-2-yl]methyl}-6-methylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-({5-[(2-methoxyethoxy)methyl]pyrazin-2-yl}methyl)-6-methylpyridin-2(1H)-one;

(5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrazin-2-yl)methyl carbamate;

1-benzyl-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one;

3-bromo-1-(4-fluorobenzyl)-4-[(4-fluorobenzyl)amino]-6-methylpyridin-2(1H)-one;

3-bromo-1-(cyclpyropylmethyl)-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;

4-(4-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-4-yl)methyl)pyridin-2(1H)-one;

4-(2,4,6-trifluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-4-yl)methyl)pyridin-2(1H)-one;

4-(2,6-difluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-4-yl)methyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

4-(4-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-yl)methyl)pyridin-2(1H)-one;

4-(2,4,6-trifluorobenzyloxy)-3-bromo-6-methyl-1-(pyridin-3-yl)methyl)pyridin-2(1H)-one;

4-(2-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-yl)methyl)pyridin-2(1H)-one;

4-(2,4,5-trifluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-ylmethyl)pyridin-2(1H)-one;

4-(4-chloro-2-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-yl)methyl)pyridin-2(1H)-one;

4-(2-chloro-4-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-yl)methyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-2-ylmethyl)pyridin-2(1H)-one;

4-(2,6-difluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-3-yl)methyl)pyridin-2(1H)-one;

4-(4-fluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-2-yl)methyl)pyridin-2(1H)-one;

4-(2,4,6-trifluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-2-yl)methyl)pyridin-2(1H)-one;

4-(2,4,5-trifluorobenzyloxy)-3-bromo-6-methyl-1-((pyridin-2-yl)methyl)pyridin-2(1H)-one;

3-bromo-4-[2-(4-fluorophenyl)ethyl]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[2-(4-fluorophenyl)ethyl]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

1-[(4-amino-2-methylpyrimidin-5-ylmethyl]-3-bromo-6-methyl-4-[(2,4,6-trifluorobenzyl)oxy]pyridin-2(1H)-one trifluoroacetate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-{[2-methyl-4-(methylamino)pyrimidin-5-yl]methyl}pyridin-2(1H)-one trifluoroacetate;

ethyl N-(5-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-2-methylpyrimidin-4-yl)glycinate trifluoroacetate;

N-(5-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-2-methylpyrimidin-4-yl)-2-hydroxyacetamide trifluoroacetate;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-({5-[(4-hydroxypiperidin-1-yl)carbonyl]pyrazin-2-yl}methyl)-6-methylpyridin-2(1H)-one;

5-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(3-hydroxy-2,2-dimethylpropyl)pyrazine-2-carboxamide;

5-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2,2,2-trifluoroethyl-pyrazine-2-carboxamide;

1-allyl-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-allyl-3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

Methyl (2E)-4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]but-2-enoate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-prop-2-ynylpyridin-2(1H)-one;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-[(dimethylamino)methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-(hydroxymethyl)pyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-(hydroxymethyl)pyridin-2(1H)-one;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-oxo-1,6-dihydropyridine-2-carbaldehyde;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-[(dimethylamino)methyl]pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-(morpholin-4-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-{[(2-methoxyethyl)amino]methyl}pyridin-2(1H)-one;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-oxo-1,6-dihydropyridine-2-carboxylic acid;

Methyl 4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3-methylbenzoate;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-3-methylbenzoic acid;

4-(2,4-difluorobenzyloxy)-3-bromo-1-(4-(hydroxymethyl)-2-methylphenyl)-6-methylpyridin-2(1H)-one;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)-3-methylbenzamide;

4-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,3-dimethylbenzamide;

or pharmaceutically acceptable salts thereof.

39. A compound of claim 1 which is

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(2-methyl-4-vinylphenyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[4-(1,2-dihydroxyethyl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

methyl 3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-chlorobenzoate;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-chlorobenzoic acid;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-(hydroxymethyl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-[5-(hydroxymethyl)-2-methylphenyl]-6-methypyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{5-[(dimethylamino)methyl]-2-methylphenyl}-6-methylpyridin-2(1H)-one hydrochloride;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{5-[(ispropylamino)methyl]-2-methylphenyl}-6-methylpyridin-2(1H)-one hydrochloride;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N-(2-methoxyethyl)-4-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,N,4-trimethylbenzamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-(1-hydroxy-1-methylethyl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

methyl 3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-methylbenzoate;

methyl 4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3-chlorobenzoate;

3-bromo-4-[(2,4-difluorobenzyl)amino]-6-methyl-1-(pyridin-4-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)amino]-6-methyl-1-(pyridin-3-ylmethyl)pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)amino]-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)amino]-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one;

3-{[3-chloro-4-[(2,4-difluorobenzyl)amino]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzonitrile;

4-{[3-chloro-4-[(2,4-difluorobenzyl)amino]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzonitrile;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[2-fluoro-5-(hydroxymethyl)phenyl]-6-methylpyridin-2(1H)-one;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzoic acid;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluoro-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N,N-dimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2-hydroxyethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2-methoxyethyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2-hydroxyethyl)-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(3-hydroxyoropyl)benzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2,3-dihydroxypropyl)benzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzoic acid;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-methoxybenzoic acid;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-methoxy-N-methylbenzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-methoxy-N,N-dimethylbenzamide;

1-[(5-aminomethyl)-2-fluorophenyl]-3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one hydrochloride;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluoro-N-[2-hydroxy-1-(hydroxymethyl)ethyl]benzamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluorobenzyl)acetamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluorobenzyl)-2-methoxyacetamide;

N-(3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluorobenzyl)-methylsulfonamine;

1-(3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluorobenzyl)urea;

2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzonitrile;

4-{[2-(aminomethyl)-4-fluorobenzyl]oxy}-3-chloro-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one trifluoroacetate;

methyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

N-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-2,2,2-trifluoroacetamide;

isopropyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-ethylurea;

tetrahydrofuran-3-yl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

propyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

allyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

prop-2-ynyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

or pharmaceutically acceptable salts thereof.

40. A compound of claim 1 which is

t-butyl 2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-tert-butylurea;

N-(2-((3-chloro-1-(2,6-difluoroyhenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-2-(propylsulfonyl)acetamide;

N-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-2-(ethylsulfonyl)acetamide;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-isopropylurea

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-methylurea;

3-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-1-tert-butyl-1-methylurea;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-cyclpyropylurea;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-(2,2,2-trifluoroethyl)urea;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-(cyclopropylmethyl)urea;

1-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-3-neopentylurea;

3-(2-((3-chloro-1-(2,6-difluorophenyl)-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzyl)-1,1-dimethylurea;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{[5-(1-hydroxy-1-methylethyl)pyridin-2-yl]methyl}-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{[5-(hydroxymethyl)pyridin-2-yl]methyl}-6-methylpyridin-2(1H)-one;

6-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)-N-methylnicotinamide;

6-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)nicotinamide;

6-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N,N-dimethylnicotinamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-[2-(trifluoromethyl)phenyl]pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-methyl-5-vinylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-5-(1,2-dihydroxyethyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-5-(hydroxymethyl)-6-methylpyridin-2(1H)-one;

4-(benzyloxy)-3-bromo-1-(2,6-difluorophenyl)-6-methylpyridin-2(1H)-one;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-2-methyl-6-oxo-1,6-dihydropyridin-3-yl]methyl carbamate;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-2-methyl-6-oxo-1,6-dihydropyridine-3-carbaldehyde;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluoropbenyl)-2-methyl-6-oxo-1,6-dihydropyridine-3-carbaldehyde oxime;

5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-2-methyl-6-oxo-1,6-dihydropyridine-3-carbonitrile;

4-(benzyloxy)-3-bromo-1-(2,6-difluorophenyl)-5-iodo-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyloxy]-1-(2,6-difluorophenyl)-6-methyl-5-oxiran-2-ylpyridin-2(1H)-one;

4-(benzylamino)-3-bromo-1-(2,6-difluorophenyl)-5-iodo-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluorophenyl)-6-methyl-5-[(E)-2-phenylethenyl]pyridin-2(1H)-one;

ethyl 3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxo-2H-1,2′-bipyridine-5′-carboxylate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-5′-(1-hydroxy-1-methylethyl)-6-methyl-2H-1,2-bipyridin-2-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2-furylmethyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-(thien-2-ylmethy)pyridin-2(1H)-one;

3-bromo-1-(2,6-difluorophenyl)-4-(2-furylmethoxy)-6-methylpyridin-2(1H)-one;

3-bromo-1-[2-fluoro-6-(3-furylmethoxy)phenyl]-4-(3-furylmethoxy)-6-methylpyridin-2(1H)-one;

3-bromo-1-[2-fluoro-6-(thien-3-ylmethoxy)phenyl]-6-methyl-4-(thien-3-ylmethoxy)pyridin-2(1H)-one;

methyl 2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-[(methylamino)carbonyl]benzoate;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-(1-hydroxy-1-methylethyl)-N-methylbenzamide;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3-chlorobenzamide;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-methylbenzamide;

3-[3-chloro-4-[(2,4-difluorobenzyloxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide;

N-{3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzyl}propanamide;

N-{3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzyl}dimethylurea;

N-{3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzyl}-2-hydroxyacetamide;

N-{3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzyl}-2-hydroxy-2-methylpropanamide;

N-{3-[3-chloro-4-[(2,4-difluorobenzy)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzyl}glycinamide hydrochloride;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorobenzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluoro-N-methylbenzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluoro-N,N-dimethylbenzamide;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{2-fluoro-5-[(4-methylpiperazin-1-yl)carbonyl]phenyl}-6-methylpyridin-2(1H)-one;

or pharmaceutically acceptable salts thereof.

41. A compound of claim 1 which is

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2-hydroxyethyl)-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-(2-hydroxy-2-methylpropyl)benzamide;

methyl 4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3-fluorobenzoate;

4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzoic acid;

4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzamide;

4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N,N-dimethylbenzamide;

4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxy-2-methylpropyl)benzamide;

N-{4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzyl}-2-hydroxyacetamide;

3-[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzamide;

1-(4-aminobenzyl)-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

1-(3-aminobenzyl)-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}phenyl)acetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)phenyl)-2-hydroxyacetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)phenyl)-(dimethylaminosulfonylcarbonyl)amine;

N-(3-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}phenyl)acetamide;

N-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)phenyl)-(dimethylaminosulfonylcarbonyl)amine;

N-(3-((4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)methyl)phenyl)-2-hydroxyacetamide;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-N′-methylurea;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-N′-(2-hydroxy-2-methylpropyl)urea;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)piperidine-1-carboxamide;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)morpholine-4-carboxamide;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)piperazine-1-carboxamide hydrochloride;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-N′-(2-hydroxyethyl)urea;

N′-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-N,N-dimethylurea;

N-(4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-4-hydroxypiperidine-1-carboxamide;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N,N-dimethylbenzenesulfonamide;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxyethyl)benzenesulfonamide;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxy-2-methyloropyl)benzenesulfonamide;

3-Chloro-4-(2,4-difluorobenzyloxy)-6-methyl-1-(1H-pyrazol-3-ylmethyl)-1H-pyridin-2-one;

3-Chloro-4-(2,4-difluorobenzyloxy)-6-methyl-1-(2,3-dihydro-1H-indol-5-ylmethyl)-1H-pyridin-2-one;

5-[3-Chloro-4-(2,4-difluorobenzyloxy)-6-methyl-2-oxo-2H-pyridin-1-ylmethyl]-1,3-dihydro-indol-2-one;

N-[(5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrazin-2-yl)methyl]-N-methylmethanesulfonamide;

Methyl (5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrazin-2-yl)methyl(methyl)carbamate;

N-[(5-{[3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}pyrazin-2-yl)methyl]-2-hydroxy-N,2-dimethylpropanamide;

5-{[3-Bromo-4-[(2,4-difluorobenzyhoxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N-(2-hydroxy-2-methylpropyl)pyrazine-2-carboxamide;

1-[(5-Aminopyrazin-2-yl)methyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-[(3-methyl-1,2,4-triazin-6-yl)methyl]pyridin-2(1H)-one trifluoroacetate;

3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-(1H-indazol-5-yl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(1H-indazol-6-yl)-6-methylpyridin-2(1H)-one;

methyl 2-{[(3-bromo-6-methyl-1-{2-methyl-5-[(methylamino)carbonyl]phenyl}-2-oxo-1,2-dihydropyridin-4-yl)oxy]methyl}-5-fluorobenzylcarbamate;

methyl 2-({[3-bromo-1-(5-{[(2-hydroxyethyl)amino]carbonyl}-2-methylphenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

methyl 2-({[3-bromo-1-(5-{[(2-hydroxy-2-methylpropyl)amino]carbonyl}-2-methylphenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

methyl 2-({[3-bromo-1-(5-{[(2-methoxyethyl)amino]carbonyl}-2-methylphenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

methyl 2-[({1-[5-(aminocarbonyl)-2-methylphenyl]-3-bromo-6-methyl-2-oxo-1,2-dihydropyridin-4-yl}oxy)methyl]-5-fluorobenzylcarbamate;

N-[2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzyl]-N′-phenylurea;

thien-3-ylmethyl 2-({[3-chloro-1-(2,6-difluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

ethyl 2-{[(3-bromo-6-methyl-1-{2-methyl-5-[(methylamino)carbonyl]phenyl}-2-oxo-1,2-dihydropyridin-4-yl)oxy]methyl}-5-fluorobenzylcarbamate;

3-[3-bromo-4-{[2-({[(cyclopropylamino)carbonyl]amino}methyl)-4-fluorobenzyl]oxy}-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide;

3-[3-bromo-4-{[2-({[(cyclopropylamino)carbonyl]amino}methyl)-4-fluorobenzyl]oxy}-6-methyl-2-oxopyridin-1(2H)-yl]-4-methylbenzoic acid;

methyl 3-[6-[(acetyloxy)methyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-2-oxopyridin-1(2H)-yl]-4-methylbenzoate;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-4-methylbenzoic acid;

or pharmaceutically acceptable salts thereof.

42. A compound of claim 1 which is

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-4-methylbenzoic acid;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-(hydroxymethyl)-2-oxopyridin-1(2H)-yl]-4-methylbenzamide;

(5-bromo-4-[(2,4-difluorobenzyl)oxy]-1-{2-methyl-5-[(methylamino)carbonyl]phenyl}-6-oxo-1,6-dihydropyridin-2-yl)methyl acetate;

(2E)-4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-methylbut-2-enamide;

methyl 5-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-2-furoate;

3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-(hydroxymethyl)-N-methylbenzamide;

2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,N′-dimethylterephthalamide;

2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N-(4-methylterephthalamide;

methyl 4-(aminocarbonyl)-2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]benzoate;

2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N 1 ,N 1 ,N 4 -trimethylterephthalamide;

2-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-[(methylamino)carbonyl]benzyl carbamate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-(2,6-difluoro-4-vinylphenyl)-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[4-(1,2-dihydroxyethyl)-2,6-difluorophenyl]-6-methylpyridin-2(1H)-one;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3,5-difluorobenzaldehyde;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3,5-difluorobenzyl carbamate;

4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-1-((5-methylpyrazin-2-yl)methyl)pyridin-2(1H)-one;

4-(2,4-difluorobenzyloxy)-3-chloro-1-((5-(hydroxymethyl)pyrazin-2-yl)methyl)-6-methylpyridin-2(1H)-one;

4-(2,4-difluorobenzyloxy)-3-bromo-1-((1-(2-hydroxyacetyl)indolin-5-yl)methyl)-6-methylpyridin-2(1H)-one;

1-((1H-pyrazol-3-yl)methyl)-4-(2,4-difluorobenzyloxy)-3-bromo-6-methylpyridin-2(1H)-one;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluoro-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-chloro-N-methylbenzamide;

3-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-4-fluorobenzamide;

4-(4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)-N,3-dimethylbenzamide;

4-(2,4-difluorobenzyloxy)-3-chloro-1-(4-(1,2-dihydroxyethyl)-2-methylphenyl)-6-methylpyridin-2(1H)-one;

N-(4-((4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)methyl)phenyl)-2-hydroxyacetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-1-hydroxycyclopropanecarboxamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H)-yl)methyl)benzyl)-2-hydroxyacetamide;

N-(4-((4-(2,4-difluorobenzyloxy)-3-chloro-6-methyl-2-oxopyridin-1(2H))-ylmethyl)phenyl)acetamide;

ethyl 2-((3-bromo-1-(2,6-difluorophenyl-1,2-dihydro-6-methyl-2-oxopyridin-4-yloxy)methyl)-5-fluorobenzylcarbamate;

3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-(2-hydroxyethyl)-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide;

4-(2,4-difluorobenzyloxy)-3-bromo-1-(5-(2-hydroxyethyl)-2-methylphenyl)-6-methylpyridin-2(1H)-one;

5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-2-(2-hydroxyethyl)-N,4-dimethylbenzamide;

4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-1-(4-methyl-2-(methylsulfonyl)pyrimidin-5-yl)-pyridin-2(1H)-one;

5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylpyrimidine-2-carbonitrile;

4-(2,4-difluorobenzyloxy)-1-(2-(aminomethyl)-4-methylpyrimidin-5-yl)-3-bromo-6-methylpyridin-2(1H)-one;

4-(2,4-difluorobenzyloxy)-3-bromo-1-(2-((dimethylamino)methyl)-4-methylpyrimidin-5-yl)-6-methylpyridin-2(1H)-one;

N-((5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylpyrimidin-2-yl)methyl)-2-hydroxyacetamide;

5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylpyrimidine-2-carboxylic acid;

5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylpyrimidine-2-carboxamide;

5-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylpyrimidine-2-carboxamide;

N-(4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-2-hydroxyacetamide;

N-(4-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl)-1-hydroxycyclopropanecarboxamide;

4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}benzyl carbamate;

2-[4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}phenyl)amino]-1-methyl-2-oxoethyl acetate;

2-[4-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}phenyl)amino]-1,1-dimethyl-2-oxoethyl acetate;

{1-[3-(aminocarbonyl)phenyl]-5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxo-1,6-dihydropyridin-2-yl}methyl acetate;

or pharmaceutically acceptable salts thereof.

43. A compound of claim 1 which is

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-{[2-(methylthio)pyrimidin-5-yl]methyl}pyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-1-{[2-(methylsulfonyl)pyrimidin-5-yl]methyl}pyridin-2(1H)-one;

Ethyl 2-({[3-bromo-1-(5-{[(2-hydroxyethyl)amino]carbonyl}-2-methylphenyl)-6-methyl-2-oxo-1,2-dihydropyridin-4-yl]oxy}methyl)-5-fluorobenzylcarbamate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-(1H-imidazol-2-yl)-2-methylphenyl]-6-methylpyridin-2(1H)-one trifluoroacetate;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-(5-hydroxy-1H-pyrazol-3-yl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-(5-hydroxylsoxazol-3-yl)-2-methylphenyl]-6-methylpyridin-2(1H)-one;

5-{[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-2-furamide;

5-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-2-furamide;

1-[3,5-bis(hydroxymethyl)phenyl]-3-bromo-4-[(2,4-difluorobenzyloxy]-6-methylpyridin-2(1H)-one;

5-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]isophthalamide;

1-[3,5-bis(1-hydroxy-1-methylethyl)phenyl]-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[4-(hydroxymethyl)phenyl]-6-methylpyridin-2(1H)-one;

3-bromo-4-[(2,4-difluorobenzyl)oxy]-1-[4-(1-hydroxy-1-methylethyl)phenyl]-6-methylpyridin-2(1H)-one;

1-(5-amino-2-fluorophenyl)-3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methylpyridin-2(1H)-one hydrochloride;

N-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorophenyl}-2-hydroxyacetamide;

N-{3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-4-fluorophenyl}-2-hydroxy-2-methylpropanamide;

4-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-3-fluoro-N,N-dimethylbenzamide;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-[(1-glycoloyl-2,3-dihydro-1H-indol-5-yl)methyl]-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-{[1-(2-hydroxy-2-methylpropanoyl)-2,3-dihydro-1H-indol-5-yl]methyl}-6-methylpyridin-2(1H)-one;

3-chloro-4-[(2,4-difluorobenzyl)oxy]-1-{[1-(methoxyacetyl)-2,3-dihydro-1H-indol-5-yl]methyl}-6-methylpyridin-2(1H)-one;

5-{[3-chloro-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]methyl}-N,N-dimethylindoline-1-carboxamide;

or pharmaceutically acceptable salts thereof.

44. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

45. A pharmaceutical composition comprising a therapeutically effective amount of (−)-3-[3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl]-N,4-dimethylbenzamide, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (2)

CHANGE OF NAME Recorded Dec 6, 2012

From: PHARMACIA CORPORATION

To: PHARMACIA LLC

Reel/Frame 029416/0192 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 25, 2003

From: DEVADAS, BALEKUDRU; WALKER, JOHN; SELNESS, SHAUN R.; BOEHM, TERRI L.; DURLEY, RICHARD C.; DEVRAJ, RAJESH; HICKORY, BRIAN S.; RUCKER, PAUL V.; JEROME, KEVIN D.; MADSEN, HEATHER M.; ALVIRA, EDGARDO; PROMO, MICHELE A.; BLEVIS-BAL, RADHIKA M.; MARRUFO, LAURA D.; HITCHCOCK, JEFF; OWEN, THOMAS; NAING, WIN; XING, LI; SHIEH, HUEY S.; SAMBANDAM, ARUNA; LIU, SHUANG; SCOTT, IAN L.; MCGEE, KEVIN F.

To: PHARMACIA CORPORATION

Reel/Frame 014522/0250 →

Continuity (3)

Provisional Application 6035702900 · Feb 14, 2002

Provisional Application 6043691500 · Dec 30, 2002

Related Publication 20040058964A1 · Mar 25, 2004