IP Library Granted Patent US 8,822,480
Granted Patent B2
US 8,822,480 · App. 13/003,681 · Granted Sep 2, 2014

Bicyclic heterocycle derivatives and use thereof as GPR119 modulators

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Quick Facts
Patent No.
US 8,822,480
App. No.
13/003,681
Granted
Sep 2, 2014
Kind
B2
Abstract

The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.

Claims (48)

1. A compound having the formula

or a pharmaceutically acceptable salt thereof, wherein:

A is O;

B is:

J and M are each —N— and L is —CH;

Q is a bond;

X—Y is CH 2 —CH 2 or CH═CH;

W is —C(O)O—, —C(O)— or —S(O) 2 —;

R 3 is alkyl, haloalkyl or cycloalkyl, wherein the cycloalkyl group can be optionally substituted with up to 4 substituents, each independently selected from alkyl and halo; and

R 8 is (i) phenyl optionally substituted with up to 2 groups independently selected from halo, —CN and —S(O) 2 -alkyl, or (ii) a heteroaryl optionally substituted with up to 2 groups independently selected from alkyl and heteroaryl.

2. The compound of claim 1 , where W is —C(O)O—.

3. The compound of claim 1 where R 8 is phenyl, optionally substituted with up to 2 groups each independently selected from halo, —CN, and —S(O) 2 -alkyl.

4. The compound of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

5. A composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

6. A method for treating type 2 diabetes in a patient, the method comprising administering to the patient an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

7. A compound having the formula

or a pharmaceutically acceptable salt thereof, wherein:

A is O;

B is:

J and M are each —N— and L is —CH;

Q is a bond;

X—Y is CH 2 —CH 2 or CH═CH;

W is —C(O)O—, —C(O)— or —S(O) 2 —;

R 3 is alkyl, haloalkyl or cycloalkyl, wherein the cycloalkyl group can be optionally substituted with up to 4 substituents, each independently selected from alkyl and halo; and

R 8 is (i) phenyl optionally substituted with up to 2 groups independently selected from halo, —CN and —S(O) 2 -alkyl, or (ii) a heteroaryl optionally substituted with up to 2 groups independently selected from alkyl and heteroaryl.

8. The compound of claim 7 , where W is —C(O)O—.

9. The compound of claim 7 , where W is —S(O) 2 —.

10. The compound of claim 7 where R 8 is phenyl, optionally substituted with up to 2 groups each independently selected from halo, —CN, and —S(O) 2 -alkyl.

11. The compound of claim 7 where R 8 is pyridyl, optionally substituted with up to 2 groups each independently selected from alkyl and heteroaryl.

12. The compound of claim 7 having the structure:

or a pharmaceutically acceptable salt thereof.

13. A composition comprising the compound of claim 7 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

14. A method for treating type 2 diabetes in a patient, the method comprising administering to the patient an effective amount of the compound of claim 7 , or a pharmaceutically acceptable salt thereof.

15. A compound having the formula

or a pharmaceutically acceptable salt thereof, wherein:

A is O;

B is:

J and M are each —N— and L is —CH;

Q is a bond;

X—Y is CH 2 —CH 2 or CH═CH;

W is —C(O)O—, —C(O)— or —S(O) 2 —;

R 3 is alkyl, haloalkyl or cycloalkyl, wherein the cycloalkyl group can be optionally substituted with up to 4 substituents, each independently selected from alkyl and halo; and

R 8 is (i) phenyl optionally substituted with up to 2 groups independently selected from halo, —CN and —S(O) 2 -alkyl, or (ii) a heteroaryl optionally substituted with up to 2 groups independently selected from alkyl and heteroaryl.

16. The compound of claim 15 , where W is —C(O)O—.

17. The compound of claim 15 where R 8 is phenyl, optionally substituted with up to 2 groups each independently selected from halo, —CN, and —S(O) 2 -alkyl.

18. A composition comprising the compound of claim 15 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

19. A method for treating type 2 diabetes in a patient, the method comprising administering to the patient an effective amount of the compound of claim 15 , or a pharmaceutically acceptable salt thereof.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →