IP Library Granted Patent US 7,671,059
Granted Patent B2
US 7,671,059 · App. 11/541,462 · Granted Mar 2, 2010

2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-ones

Assignee: Novartis AG
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Quick Facts
Patent No.
US 7,671,059
App. No.
11/541,462
Granted
Mar 2, 2010
Kind
B2
Abstract

Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

Claims (458)

1. A compound of formula (I):

or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein

R a is selected from the group consisting of

(1) hydrogen,

(2) halogen,

(3) hydroxyl,

(4) C 1 -C 6 alkoxy,

(5) thiol,

(6) C 1 -C 6 alkyithiol,

(7) substituted or unsubstituted C 1 -C 6 alkyl,

(8) amino or substituted amino,

(9) substituted or unsubstituted aryl,

(10) substituted or unsubstituted heteroaryl, and

(11) substituted or unsubstituted heterocyclyl;

R is selected from the group consisting of

(1) hydrogen,

(2) substituted or unsubstituted C 1 -C 6 alkyl,

(3) substituted or unsubstituted C 2 -C 6 alkenyl,

(4) substituted or unsubstituted C 2 -C 6 alkynyl,

(5) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(6) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(7) substituted or unsubstituted aryl,

(8) substituted or unsubstituted heteroaryl, and

(9) substituted or unsubstituted heterocyclyl;

R b is selected from the group consisting of

(1) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(2) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(3) substituted or unsubstituted aryl,

(4) substituted or unsubstituted heteroaryl, and

(5) substituted or unsubstituted heterocyclyl; and

with the proviso that when R a is amino, then R b is not phenyl, 4-alkyl-phenyl, 4-alkoxy-phenyl, or 4-halo-phenyl.

2. A compound of claim 1 having formula (Ia)

wherein R, R a , and R b are previously defined for formula (I).

3. A compound of claim 1 having formula (II):

or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein

n is 0 or 1,

wherein R a is selected from the group consisting of

(1) hydrogen,

(2) halogen,

(3) hydroxyl,

(4) C 1 -C 6 alkoxy,

(5) thiol,

(6) C 1 -C 6 alkyithiol,

(7) substituted or unsubstituted C 1 -C 6 alkyl,

(8) amino or substituted amino,

(9) substituted or unsubstituted aryl,

(10) substituted or unsubstituted heteroaryl, and

(11) substituted or unsubstituted heterocyclyl;

wherein R is selected from the group consisting of

(1) hydrogen,

(2) substituted or unsubstituted C 1 -C 6 alkyl,

(3) substituted or unsubstituted C 2 -C 6 alkenyl,

(4) substituted or unsubstituted C 2 -C 6 alkynyl,

(5) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(6) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(7) substituted or unsubstituted aryl,

(8) substituted or unsubstituted heteroaryl, and

(9) substituted or unsubstituted heterocyclyl,

wherein when n is 1, X is C, Y is at each position independently selected from CQ 1 and N, and Z is selected from CR 2 and N with the proviso that no more than 3 Y and Z groups are N, and wherein when n is 0, X is C or N, Y is at each position independently selected from CQ 1 , N, NQ 2 , O, and S with the proviso that no more than 4 X and Y groups are N and NQ 2 and no more than 1 Y group is S or O;

wherein Q 1 is at each position independently selected from the group consisting of

(1) hydrogen,

(2) halogen,

(3) substituted or unsubstituted C 1 -C 6 alkyl,

(4) substituted or unsubstituted C 2 -C 6 alkenyl,

(5) substituted or unsubstituted C 2 -C 6 alkynyl,

(6) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(7) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(8) substituted or unsubstituted aryl,

(9) substituted or unsubstituted heteroaryl,

(10) substituted or unsubstituted heterocyclyl,

(11) substituted or unsubstituted amino,

(12) —OR 3 or —SR 3

(13) —C(O)R 3 , —CO 2 R 3 , —C(O)N(R 3 ) 2 , —S(O)R 3 , —SO 2 R 3 , or —SO 2 N(R 3 ) 2 ,

(14) —OC(O)R 3 , —N(R 3 )C(O)R 3 , or —N(R 3 )SO 2 R 3 ,

(15) —CN, and

(16) —NO 2 ;

wherein Q 2 is at each position independently selected from the group consisting of

(1) hydrogen,

(3) substituted or unsubstituted C 1 -C 6 alkyl,

(4) substituted or unsubstituted C 2 -C 6 alkenyl,

(5) substituted or unsubstituted C 2 -C 6 alkynyl,

(6) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(7) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(8) substituted or unsubstituted aryl,

(9) substituted or unsubstituted heteroaryl, and

(10) substituted or unsubstituted heterocyclyl;

wherein R 2 is selected from the group consisting of

(1) hydrogen,

(2) halogen,

(3) substituted or unsubstituted C 1 -C 3 alkyl, and

(4) —OR 3 , or —NHR 3 ; —SR 3 ,

wherein R 3 is at each position independently selected from the group consisting of

(1) hydrogen,

(2) substituted or unsubstituted C 1 -C 6 alkyl,

(3) substituted or unsubstituted C 2 -C 6 alkenyl,

(4) substituted or unsubstituted C 2 -C 6 alkynyl,

(5) substituted or unsubstituted C 3 -C 7 cycloalkyl,

(6) substituted or unsubstituted C 5 -C 7 cycloalkenyl,

(7) substituted or unsubstituted aryl,

(8) substituted or unsubstituted heteroaryl, and

(9) substituted or unsubstituted heterocyclyl,

with the proviso that when R a is amino, then X, Y, Z, and n together do not form a phenyl, 4-alkyl-phenyl, 4-alkoxy-phenyl, or 4-halo-phenyl group.

4. A compound of claim 3 having formula (IIa):

or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein R a , R, X, Y, Z, and n are previously defined for formula (II).

5. A compound of claim 4 having formula (III):

or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein

R a is selected from the group consisting of

(1) hydrogen,

(2) halogen,

(3) hydroxyl,

(4) C 1 -C 6 alkoxy,

(5) thiol,

(6) C 1 -C 6 alkylthiol,

(7) substituted or unsubstituted C 1 -C 6 alkyl,

(8) amino or substituted amino

(9) substituted or unsubstituted aryl,

(10) substituted or unsubstituted heteroaryl, and

(11) substituted or unsubstituted heterocyclyl;

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

R 5 is hydrogen, alkyl, alkoxy, or halo;

each of R 6 , R 7 , R 8 , and R 9 are independently selected from the group consisting of hydrogen, alkyl, alkoxy, halo, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; or

a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof, and with the proviso that when R a is amino and R 6 , R 7 , R 8 and R 9 are hydrogen, then R 5 is not hydrogen, alkyl, alkoxy, or halo.

6. A compound of claim 5 wherein R a is hydrogen.

7. A compound of claim 5 wherein R a is substituted or unsubstituted C 1 -C 6 alkyl.

8. A compound of claim 7 wherein R a is methyl.

9. A compound of claim 5 , wherein R 4 is selected from the group consisting of hydrogen, benzyl, 1-(4-methoxyphenyl)ethyl, methyl, 3-aminopropyl, and 2-methyl-2-morpholinopropyl.

10. A compound of claim 9 , wherein R 4 is hydrogen.

11. A compound of claim 5 , wherein R 5 is hydrogen or fluoro.

12. A compound of claim 5 , wherein R 7 , R 8 , and R 9 are each hydrogen.

13. A compound of claim 5 , wherein R 6 is selected from the group consisting of substituted aryl and substituted heteroaryl.

14. A compound of claim 13 , wherein said aryl and heteroaryl is selected from the group consisting of furanyl, pyrrolyl, phenyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyrazolyl, imidazolyl, triazolyl, indolyl, oxadiazole, thiadiazole, quinolinyl, isoquinolinyl, isoxazolyl, oxazolyl, thiazolyl, and thienyl.

15. A compound of claim 14 , wherein R 6 is selected from the group consisting of (2-hydroxy-ethylamino)-pyrazin-2-yl, 1H-pyrazol-4-yl, 1-methyl-1H-pyrazol-4-yl, 1-methyl-1H-pyrazol-4-yl, 2-(5-methyl-pyridin-2-yl)-phenyl, 2,3-difluoro-phenyl, 2,3-dimethoxy-phenyl, 2,4-difluoro-phenyl, 2,4-dimethoxy-phenyl, 2,4-dimethoxy-pyrimidin-5-yl, 2,5-difluoro-phenyl, 2,6-difluoro-phenyl, 2,6-dimethyl-pyridin-3-yl, 2-acetamidophenyl, 2-aminocarbonylphenyl, 2-amino-pyrimidin-5-yl, 2-chloro-4-methoxy-pyrimidin-5-yl, 2-chloro-5-fluoro-pyridin-3-yl, 2-chloro-phenyl, 2-chloro-pyridin-3-yl, 2-chloro-pyridin-4-yl, 2-difluoro-3-methoxyphenyl, 2-ethyl-phenyl, 2-ethoxy-thiazol-4-yl, 2-fluoro-3-methoxy-phenyl, 2-fluoro-3-methylphenyl, 2-fluoro-4-methyl-phenyl, 2-fluoro-5-methoxy-phenyl, 2-fluoro-5-methylphenyl, 2-fluorophenyl, 2-fluoro-pyridin-3-yl, 2-hydroxymethyl-3-methoxyphenyl, 2-hydroxymethylphenyl, 2-isoquinolin-4-yl, 2-methoxy-5-trifluoromethyl-phenyl, 2-methoxy-phenyl, 2-methoxy-pyridin-3-yl, 2-methoxy-pyrimidin-4-yl, 2-methoxy-thiazol-4-yl, 2-methyl-phenyl, 2-methyl-pyridin-3-yl, 2-oxo-1,2-dihydro-pyridin-3-yl, 2-phenoxyphenyl, 2-pyridin-3-yl, 2-pyrimidin-5-yl, 2-trifluoromethoxyphenyl, 2-trifluoromethoxy-phenyl, 3,4-dimethoxy-phenyl, 3,5-dimethyl-isoxazol-4-yl, 3,6-dimethyl-pyrazin-2-yl, 3-acetamidophenyl, 3-aminocarbonylphenyl, 3-bromo-phenyl, 3-chloro-pyrazin-2-yl, 3-cyanophenyl, 3-dimethylaminophenyl, 3-ethoxy-phenyl, 3-ethyl-4-methyl-phenyl, 3-ethynyl-phenyl, 3-fluoro-6-methoxy-pyridin-2-yl, 3-fluorophenyl, 3-fluoro-pyrazin-2-yl, 3-methanesulfonamidophenyl, 3-methoxycarbonylphenyl, 3-methoxyphenyl, 3-methoxy-pyrazin-2-yl, 3-methyl-3H-imidazo[4,5-b]pyrazin-5-yl, 3-methylphenyl, 3-methyl-pyridin-2-yl, 3-trifluoromethoxyphenyl, 3-trifluoromethylphenyl, 4,5-dimethoxy-pyrimidin-2-yl, 4-amino-5-fluoro-pyrimidin-2-yl, 4-chloro-2,5-dimethoxy-phenyl, 4-chloro-2-fluoro-phenyl, 4-chloro-2-methoxy-5-methyl-phenyl, 4-chloro-pyridin-3-yl, 4-difluoro-2-methyl-phenyl, 4-ethoxy-5-fluoro-pyrimidin-2-yl, 4-ethoxy-pyrimidin-2-yl, 4-ethoxy-pyrimidin-5-yl, 4-ethyl-1H-pyrazol-3-yl, 4-fluoro-2-methoxy-phenyl, 4-fluoro-2-methyl-phenyl, 4-fluorophenyl, 4-methoxy-5-methyl-pyrimidin-2-yl, 4-methoxy-pyridin-3-yl, 4-methoxy-pyrimidin-2-yl, 4-methoxy-pyrimidin-5-yl, 4-methyl-phenyl, 4-methyl-pyridin-2-yl, 4-methyl-pyridin-3-yl, 4-pyrrolidin-1-yl-pyrimidin-2-yl, 5,6-dimethoxy-pyrazin-2-yl, 5-acetyl-thiophen-2-yl, 5-amino-6-ethoxy-pyrazin-2-yl, 5-amino-6-methoxy-3-methyl-pyrazin-2-yl, 5-amino-6-methoxy-pyridin-2-yl, 5-chloro-4methoxy-pyrimidin-2-yl, 5-chloro-6-methoxy-pyrazin-2-yl, 5-dimethylamino-6-methoxy-pyrazin-2-yl, 5-fluoro-2-methoxyphenyl, 5-fluoro-4-methoxy-pyrimidin-2-yl, 5-fluoro-6-methoxy-pyrazin-2-yl, 5-fluoro-pyridin-2-yl, 5-methoxy-pyridin-3-yl, 5-methoxy-thiophen-2-yl, 5-trifluoromethyl-pyrimidin-2-yl, 6-acetyl-pyridin-2-yl, 6-chloro-pyrazin-2-yl, 6-ethoxy-pyrazin-2-yl, 6-ethoxy-pyridin-2-yl, 6-fluoro-pyridin-2-yl, 6-fluoro-pyridin-3-yl, 6-hydroxy-pyridin-2-yl, 6-methoxy-5-methylamino-pyrazin-2-yl, 6-methoxy-5-methyl-pyrazin-2-yl, 6-methoxy-pyrazin-2-yl, 6-methoxy-pyridin-2-yl, 6-methoxy-pyridin-3-yl, 6-methylamino-pyrazin-2-yl, 6-methyl-pyridin-2-yl, 5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl, and 6-trifluoromethyl-pyridin-2-yl.

16. A compound of claim 5 having formula (IIIa):

or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein R a , R 4 , X, Y, Z, and n are as previously defined for formula (III) and with the proviso that when R a is amino and R 6 , R 7 , R 8 , and R 9 are hydrogen, then R 5 is not hydrogen, alkyl, alkoxy, or halo.

17. A compound of claim 5 having formula (IV):

or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein

R 4 is hydrogen or substituted or unsubstituted C 1 -C 6 alkyl,

R 5 is hydrogen or halo,

R 6a is selected from the group consisting of hydrogen, halo, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl.

18. A compound of claim 17 having formula (IVa):

or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein

R 4 , R 5 , and R 6a are as previously defined for formula (IV).

19. A compound of claim 3 having formula (V):

wherein R 10 and R 11 are independently Q 1 , and R a , R, Q 1 , and Q 2 are as previously defined for formula (II).

20. A compound of claim 19 having formula (Va):

wherein R 10 and R 11 are independently Q 1 , and R a , R, Q 1 , and Q 2 are as previously defined for formula (V).

21. A compound of claim 1 selected from the group consisting of

(R)-2-Amino-7-[2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(S)-2-Amino-6-benzyl-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-6-[(S)-1-(4-methoxy-phenyl)-ethyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4,6-dimethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4,6-dimethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

2-Amino-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4,6-dimethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,2′-difluoro-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5-fluoro-2′-trifluoromethoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(2-chloro-pyridin-3-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(6-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-isoquinolin-4-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,3′-difluoro-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(4-chloro-pyridin-3-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,2′-difluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,4′-difluoro-2′-methyl-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyridol[4,3-d]pyrimidin-5-one;

2-Amino-7-(5-fluoro-2′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-pyrimidin-5-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5-fluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(3-amino-propyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,2′-difluoro-4′-methyl-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(1-methyl-1H-pyrazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(1H-pyrazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-4-methyl-7-(5,2′,3′-trifluoro-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-6-(2-methyl-2-morpholin-4-yl-propyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(3′-dimethylamino-5-fluoro-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(2,4-dimethoxy-pyrimidin-5-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(5-methoxy-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-pyrimidin-5-yl-phenyl)-4-methyl-6-(2-methyl-2-morpholin-4-yl-propyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-6-(2-methyl-2-morpholin-4-yl-propyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5-fluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-6-(2-methyl-2-morpholin-4-yl-propyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-methoxy-5-methyl-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-furan-3-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4-ethoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-methoxy-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-pyrrolidin-1-yl-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-((R)-2-Amino-4-methyl-5-oxo-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-7-yl)-5-fluoro-benzonitrile;

(R)-2-Amino-7-[2-(4,5-dimethoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-chloro-4-methoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,5′-difluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,4′-difluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-3′,4′-dimethoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-3′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-4′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,4′-difluoro-2′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(4-fluoro-2-pyridin-3-yl-phenyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2,4-dimethoxy-pyrimidin-5-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-fluoro-4-methoxy-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(5-methoxy-thiophen-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4-ethoxy-5-fluoro-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-2′,3′-dimethoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyridin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-phenyl]-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(2-methoxy-thiazol-4-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(2-methoxy-thiazol-4-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-(6-methoxy-pyrazin-2-yl)-thiazol-4-yl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5-fluoro-2′-trifluoromethyl-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(4-fluoro-2-pyridin-4-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-(5,3′-difluoro-4′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-4-methyl-7-phenyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-6-(2-amino-ethyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(4-fluoro-phenyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(S)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-methyl-7-phenyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-6-Allyl-2-amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-ethyl-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-ethyl-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-ethyl-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-ethyl-7-(5-fluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-ethyl-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2,4-dimethoxy-pyrimidin-5-yl)-4-fluoro-phenyl]-6-ethyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[2-(5-chloro-4-hydroxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-6-(2-hydroxy-ethyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-6-(2,4-dimethoxy-benzyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(3-chloro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(3-chloro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(3-chloro-benzyl)-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2,4-dimethoxy-benzyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2,4-dimethoxy-benzyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-6-pyridin-4-ylmethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-pyridin-4-ylmethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-6-pyridin-4-ylmethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2-fluoro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-6-(2-fluoro-benzyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2-chloro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-6-(2-chloro-benzyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-(3-trifluoromethyl-benzyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-6-(3-trifluoromethyl-benzyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2-fluoro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(2-chloro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-(tetrahydro-pyran-4-ylmethyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-6-(tetrahydro-pyran-4-ylmethyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-(2-methyl-2-morpholin-4-yl-propyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-(5-fluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-4-methyl-7-(5,2′,3′-trifluoro-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-(5,3′-difluoro-4′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[2-(2,4-dimethoxy-pyrimidin-5-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-(5,2′-difluoro-4′-methyl-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-benzyl-7-(5,2′-difluoro-3′-methoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-Amino-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-methoxy-pyridin-3-yl)-phenyl]-4-methyl-6-(3-methyl-butyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-pyridin-3-yl)-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-methoxy-pyridin-3-yl)-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(4-fluoro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(4-fluoro-benzyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-6-(4-fluoro-benzyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-6-isobutyl-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-6-pyridin-3-ylmethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

{3-[(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-5-oxo-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-propyl}-carbamic acid tert-butyl ester;

(R)-2-Amino-6-(3-amino-propyl)-7-(2-bromo-4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

{3-[(R)-2-Amino-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-5-oxo-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-propyl}-carbamic acid tert-butyl ester;

(R)-2-Amino-6-(3-amino-propyl)-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(3-{(R)-2-Amino-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-5-oxo-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-propyl)-carbamic acid tert-butyl ester;

(R)-2-Amino-6-(3-amino-propyl)-7-[4-fluoro-2-(2-fluoro-pyridin-3-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-6-(3-amino-propyl)-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-(6-methoxy-pyridin-2-yl)-thiazol-4-yl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-bromo-thiazol-4-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4-ethoxy-5-fluoro-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,5′-difluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,4′-difluoro-2′-methoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-3′,4′-dimethoxy-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-3′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-2′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-4′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5,4′-difluoro-2′-methyl-biphenyl-2-yl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4,5-dimethoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-(6-methoxy-pyrazin-2-yl)-thiazol-4-yl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyridin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5,6-dimethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(4-fluoro-2-pyridin-3-yl-phenyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2,4-dimethoxy-pyrimidin-5-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4-ethoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-methoxy-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-phenyl]-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[2-(2-methoxy-thiazol-4-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-chloro-4-methoxy-pyrimidin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-fluoro-4-methoxy-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(4-pyrrolidin-1-yl-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyridin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(5-methoxy-thiophen-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-fluoro-2′,3′-dimethoxy-biphenyl-2-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-4-ethyl-7-[4-fluoro-2-(2-methoxy-thiazol-4-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

2-((R)-2-Amino-4-methyl-5-oxo-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-7-yl)-5-fluoro-benzonitrile;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(4-methoxy-5-methyl-pyrimidin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(5-oxo-4,5-dihydro-[1,3,4]oxadiazol-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(5-methoxy-[1,3,4]oxadiazol-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(S)-2-Amino-7-[5-(6-methoxy-pyrazin-2-yl)-thiazol-4-yl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-thiazol-5-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-ethyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-methoxy-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-phenyl)-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2-ethoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2-ethoxy-thiazol-4-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(S)-2-Amino-7-[5-(6-methoxy-pyridin-2-yl)-thiazol-4-yl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(S)-2-Amino-7-[5-(6-methoxy-pyrazin-2-yl)-thiazol-4-yl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethyl-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-methoxy-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-methoxy-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-methoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-ethoxy-pyrazin-2-yl)-4-methoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-methoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-methoxy-2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(2-ethoxy-thiazol-4-yl)-4-methoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(6-methoxy-5-methylamino-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-5-methylamino-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-methoxy-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-methoxy-2-(6-methoxy-pyrazin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-dimethylamino-6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-dimethylamino-6-methoxy-pyrazin-2-yl)-4-fluoro-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(5-bromo-2-methoxy-pyridin-4-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(6,6′-dimethoxy-[2,3′]bipyridinyl-4′-yl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-methoxy-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[5-methoxy-2-(6-methoxy-pyridin-2-yl)-phenyl]-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-ethoxy-pyrazin-2-yl)-4-ethoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[2-(5-amino-6-methoxy-pyrazin-2-yl)-4-ethoxy-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-ethoxy-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-ethoxy-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-(cyclopentyloxy)-4-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-(cyclopentyloxy)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(4-fluoro-2-isopropoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-5-fluoro-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(6-methoxypyridin-2-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-5-fluoro-2-(6-methoxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(6-methoxypyrazin-2-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-((R)-5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl)-4-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-5-fluoro-2-(2-methoxythiazol-4-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(5-amino-6-methoxypyrazin-2-yl)-5-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(2-methoxythiazol-4-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(5-amino-6-methoxypyrazin-2-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-(cyclopentyloxy)-4-fluorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-((R)-5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl)phenyl)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-((R)-5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-((R)-5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl)-4-fluorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-2-(5-amino-6-methoxypyrazin-2-yl)-4-fluoro-5-methoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4-fluoro-5-methoxy-2-(6-methoxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(4-fluoro-5-methoxy-2-((S)-6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-4-fluoro-5-methoxy-2-(2-methoxythiazol-4-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-2-(5-amino-6-methoxypyrazin-2-yl)-4-isopropoxy-5-methoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4-isopropoxy-5-methoxy-2-(6-methoxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(4-isopropoxy-5-methoxy-2-((S)-6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-4-isopropoxy-5-methoxy-2-(2-methoxythiazol-4-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4,5-dimethoxy-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4,5-dimethoxy-2-(6-methoxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-bromo-4,5-dimethoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-4,5-dimethoxy-2-(2-methoxythiazol-4-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-2-(5-amino-6-ethoxypyrazin-2-yl)-4,5-dimethoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-bromo-4-ethoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4-fluoro-2-(6-hydroxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((R)-4-fluoro-2-(6-hydroxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-(2-bromo-4,5-diethoxyphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one; and

(R)-2-Amino-7-((R)-4-fluoro-2-(2-hydroxythiazol-4-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one

or a stereolsomer, tautomer, or pharmaceutically acceptable salt thereof.

22. A composition comprising a pharmaceutically acceptable carrier and a compound of claim 1 .

23. A compound selected from the group consisting of

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-((R)-2-(5-amino-6-methoxypyrazin-2-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4-fluoro-2-(6-hydroxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one; and

(R)-2-Amino-7-((R)-4-fluoro-2-(6-hydroxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one,

or a pharmaceutically acceptable salt thereof.

24. A composition comprising a pharmaceutically acceptable carrier and a compound selected from the group consisting of

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyrazin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-(2-bromo-4-fluoro-phenyl)-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-[4-fluoro-2-(2-methoxy-thiazol-4-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one;

(R)-2-Amino-7-((R)-2-(5-amino-6-methoxypyrazin-2-yl)-4-methylphenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one;

(R)-2-Amino-7-((S)-4-fluoro-2-(6-hydroxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one; and

(R)-2-Amino-7-((R)-4-fluoro-2-(6-hydroxypyrazin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one,

or a pharmaceutically acceptable salt thereof.

25. A compound that is (R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one or a pharmaceutically acceptable salt thereof.

26. A composition comprising a pharmaceutically acceptable carrier and (R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one or a pharmaceutically acceptable salt thereof.

Assignments (10)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 26, 2022
From: NOVARTIS AG
To: VERNALIS (R&D) LIMITED
Reel/Frame 058771/0965 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 24, 2022
From: VERNALIS (R&D) LIMITED
To: VERNALIS DEVELOPMENT LIMITED
Reel/Frame 058822/0570 →
CHANGE OF NAME Recorded Jan 24, 2022
From: VERNALIS DEVELOPMENT LIMITED
To: LIGAND UK DEVELOPMENT LIMITED
Reel/Frame 058738/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 15, 2008
From: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
To: NOVARTIS AG
Reel/Frame 020952/0946 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2008
From: POON, DANIEL; BARSANTI, PAUL A; LIN, XIAODONG; COSTALES, ABRAN; RICO, ALICE; BRAMMEIER, NATHAN; PICK, TERESA; RENHOWE, PAUL A
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 020929/0969 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: MACHAJEWSKI, TIMOTHY D.; SHAFER, CYNTHIA M.; MCBRIDE, CHRISTOPHER; ANTONIOS-MCCREA, WILLIAM R.; DOUGHAN, BRANDON M.; LEVINE, BARRY H.; XIA, YI; MCKEENA, MAUREEN; WANG, X. MICHAEL; MENDENHALL, KRIS G.; ZHOU, YASHEEN; GONG, BAOQING; GU, DAN; DOLAN, JOHN; TULINSKY, JOHN; BRINNER, KRISTIN; GAO, ZHENHAI
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 019016/0669 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: MACHAJEWSKI, TIMOTHY D.; SHAFER, CYNTHIA M.; MCBRIDE, CHRISTOPHER; ANTONIOS-MCCREA, WILLIAM R.; DOUGHAN, BRANDON M.; LEVINE, BARRY H.; XIA, YI; MCKEENA, MAUREEN; WANG, X. MICHAEL; MENDENHALL, KRIS G.; ZHOU, YASHEEN; GONG, BAOQING; GU, DAN; DOLAN, JOHN; TULINSKY, JOHN; BRINNER, KRISTIN; GAO, ZHENHAI
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 018965/0454 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: MACHAJEWSKI, TIMOTHY D.; SHAFER, CYNTHIA M.; MCBRIDE, CHRISTOPHER; ANTONIOS-MCCREA, WILLIAM R.; DOUGHAN, BRANDON M.; LEVINE, BARRY H.; XIA, YI; MCKEENA, MAUREEN; WANG, X. MICHAEL; MENDENHALL, KRIS G.; ZHOU, YASHEEN; GONG, BAOQING; GU, DAN; DOLAN, JOHN; TULINSKY, JOHN; BRINNER, KRISTIN; GAO, ZHENHAI
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 018973/0032 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: MACHAJEWSKI, TIMOTHY D.; SHAFER, CYNTHIA M.; MCBRIDE, CHRISTOPHER; ANTONIOS-MCCREA, WILLIAM R.; DOUGHAN, BRANDON M.; LEVINE, BARRY H.; XIA, YI; MCKEENA, MAUREEN; WANG, X. MICHAEL; MENDENHALL, KRIS G.; ZHOU, YASHEEN; GONG, BAOQING; GU, DAN; DOLAN, JOHN; TULINSKY, JOHN; BRINNER, KRISTIN; GAO, ZHENHAI
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 018973/0069 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: MACHAJEWSKI, TIMOTHY D.; SHAFER, CYNTHIA M.; MCBRIDE, CHRISTOPHER; ANTONIOS-MCCREA, WILLIAM R.; DOUGHAN, BRANDON M.; LEVINE, BARRY H.; XIA, YI; MCKEENA, MAUREEN; WANG, X. MICHAEL; MENDENHALL, KRIS G.; ZHOU, YASHEEN; GONG, BAOQING; GU, DAN; DOLAN, JOHN; TULINSKY, JOHN; BRINNER, KRISTIN; GAO, ZHENHAI
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 018982/0045 →
Continuity (3)
Provisional Application 6072279600 · Sep 30, 2005
Provisional Application 6083688600 · Aug 9, 2006
Related Publication 20070123546A1 · May 31, 2007