P2X7 modulators

Patent metadata

Field	Value
Publication number	US-10150766-B2
Application number	US-201515540658-A
Country	US
Kind code	B2
Filing date	Aug 25, 2015
Priority date	Sep 12, 2014
Publication date	Dec 11, 2018
Grant date	Dec 11, 2018

Abstract

The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

First claim

What is claimed:

1. A compound of Formula (I)

or enantiomers or diastereomers thereof;
or pharmaceutically acceptable salts thereof;
wherein:
R a is

R 1 , R 2 , R 3 , and R 4 are each independently selected from the group consisting of: H, halo, C 1 -C 3 alkyl and C 1 -C 3 perhaloalkyl;
R 5 is C 1 -C 3 perhaloalkyl or C 1 -C 3 alkyl;

R b is selected from the group consisting of:

Wherein:
R 6 , R 8 , R 9 , R 10 , R 12 , R 13 are independently H or C 1 -C 3 alkyl,
R 7 is H, halo or C 1 -C 3 perhaloalkyl,
R 11 is H, halo or OH;
R 14 is H or halo; and

R c is selected from the group consisting of: H, NH 2 , C 1 -C 4 alkyl.

2. A compound as in claim 1 wherein, R a is

and R 1 is halo or C 1 -C 3 perhaloalkyl.

3. A compound as in claim 1 wherein, R a is

and R 1 is halo.

4. A compound as in claim 1 wherein wherein is R a is

and R 2 is C 1 -C 3 perhaloalkyl.

5. A compound as in claim 1 wherein, R a is

and R 3 is halo.

6. A compound as in claim 1 wherein, R a is

and R 1 is independently selected from the group consisting of: halo, C 1 -C 3 alkyl and C 1 -C 3 perhaloalkyl, R 2 is independently selected from the group consisting of: halo, C 1 -C 3 alkyl and C 1 -C 3 perhaloalkyl and R 3 is H or halo.

7. A compound as in claim 1 wherein, R a is

and R 1 is independently selected from the group consisting of: halo and C 1 -C 3 perhaloalkyl and R 2 is independently selected from the group consisting of: halo and C 1 -C 3 perhaloalkyl, and R 3 is H.

8. A compound as in claim 1 wherein, R a is

and R 1 is halo and R 2 is C 1 -C 3 perhaloalkyl.

9. A compound as in claim 1 wherein, R a is

and R 1 and R 2 are halo and R 3 is H.

10. A compound as in claim 1 wherein, R a is

and R 1 , R 2 and R 3 are halo.

11. A compound as in claim 1 wherein, R a is

and R 4 is independently selected from the group consisting of: halo, C 1 -C 3 alkyl and C 1 -C 3 perhaloalkyl.

12. A compound as in claim 1 wherein, R a is

and R 4 is halo or C 1 -C 3 perhaloalkyl.

13. A compound as in claim 1 wherein, R a is

and R 4 is halo.

14. A compound as in claim 1 wherein, R a is

and R 5 is C 1 -C 3 alkyl or C 1 -C 3 perhaloalkyl.

15. A compound as in claim 1 wherein, R a is

and R 5 is C 1 -C 3 perhaloalkyl.

16. A compound as in claim 1 wherein, R a is

and R 4 is independently selected from the group consisting of: halo, C 1 -C 3 alkyl and C 1 -C 3 perhaloalkyl and R 5 is C 1 -C 3 alkyl or C 1 -C 3 perhaloalkyl.

17. A compound as in claim 1 wherein, R a is

and R 4 is independently selected from the group consisting of: halo and C 1 -C 3 perhaloalkyl and R 5 is C 1 -C 3 perhaloalkyl.

18. A compound as in claim 1 wherein, R a is

and R 4 is halo and R 5 is C 1 -C 3 perhaloalkyl.

19. A compound as in claim 1 wherein, R b is selected from the group consisting of:

20. A compound as in claim 1 wherein, R b is selected from the group consisting of:

21. A compound as in claim 1 wherein, R b is selected from the group consisting of:

22. A compound as in claim 1 wherein, R b is selected from the group consisting of:

23. A compound as in claim 1 wherein, R b is

24. A compound as in claim 1 wherein, R b is

25. A compound as in claim 1 wherein, R b is

26. A compound as in claim 1 wherein R c is selected from the group consisting of: H, NH 2 , and 01-C 4 alkyl.

27. A compound as in claim 1 wherein R c is H or C 1 -C 4 alkyl.

28. A compound as in claim 1 wherein R c is C 1 -C 4 alkyl.

29. A compound as in claim 1 wherein, R a is

R 4 is halo, R 5 is C 1 -C 3 perhaloalkyl, R c is C 1 -C 4 alkyl, R 6 is H, and R b is

30. A compound as in claim 1 wherein, R a is

R 4 is halo, R 5 is C 1 -C 3 perhaloalkyl, R c is C 1 -C 4 alkyl, R 6 is CH 3 , R b is

31. A compound as in claim 1 wherein,

Assignees

• Jansssen Pharmaceutica NV
• Janssen Pharmaceutica Nv

Inventors

• Letavic Michael A
• Rech Jason C
• Wall Jessica L

Classifications

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/12

  Antihypertensives · CPC title