IP Library Granted Patent US 8,815,876
Granted Patent B2
US 8,815,876 · App. 13/003,716 · Granted Aug 26, 2014

Bicyclic heterocycle derivatives and methods of use thereof

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,815,876
App. No.
13/003,716
Granted
Aug 26, 2014
Kind
B2
Abstract

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

Claims (29)

1. A compound having the formula:

or a pharmaceutically acceptable salt thereof,

wherein:

A is —O— or —N(R 12 )—;

W is —C(O)O—, —C(O)— or —S(O) 2 —;

—X—Y is CH 2 —CH 2 or CH═CH;

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

each occurrence of R 7 is independently H or alkyl;

R 8 is aryl or heteroaryl, optionally substituted with R 9 ;

R 9 represents from 1-4 optional substituents, which can be the same or different, selected from alkyl, alkenyl, alkynyl, halo, haloalkyl, —CN, —NO 2 , —O-(alkylene) t -R 13 , —S-(alkylene) t -R 13 , —N(R 13 )-(alkylene) t -R 13 , -(alkylene) t -R 13 , —C(O)-(alkylene) t -R 13 , —C(O)O-(alkylene) t -R 13 , —N(R 7 )C(O)-(alkylene) t -R 13 , —C(O)N(R 7 )-(alkylene) t -R 13 , —OC(O)-(alkylene) t -R 13 , —N(R 7 )C(O)N(R 7 )-(alkylene) t -R 13 , —N(R 7 )C(O)O-(alkylene) t -R 13 , —S(O)-(alkylene) t -R 13 or —S(O) 2 (alkylene) t -R 13 ;

R 12 is H, alkyl or aryl;

each occurrence of R 13 is independently H, haloalkyl, aryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl or heteroaryl; and

each occurrence of t is independently 0 or 1.

2. The compound of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

3. A composition comprising one or more compounds of claim 1 or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

4. A method for treating type II diabetes in a patient, the method comprising administering to the patient an effective amount of one or more compounds of claim 1 , or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 where A is —NH—.

6. The compound of claim 1 where A is —O—.

7. The compound of claim 5 where W is —C(O)O—.

8. The compound of claim 5 where W is —S(O) 2 —.

9. The compound of claim 1 where R 8 is phenyl, optionally substituted with R 9 .

10. The compound of claim 1 where R 8 is pyridyl, optionally substituted with R 9 .

11. The compound of claim 9 where R 3 is cyclopropyl or cyclobutyl, optionally substituted with up to 4 substituents each independently selected from the group consisting of: alkyl and halo.

12. The compound of claim 9 where R 3 is isopropyl or t-butyl.

13. The compound of claim 1 where R 9 is independently selected from alkyl, halo, —CN, cycloalkyl, alkynyl, heteroaryl, —S(O) 2 -alkyl, or S(O) 2 -cycloalkyl.

14. The compound of claim 1 where R 9 is independently selected from methyl, F, Cl, —CN, , or —S(O) 2 CH 3 .

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

16. The compound of claim 1 where R 8 is heteroaryl, which is substituted with 1 or 2 groups, each independently selected from alkyl or heteroayl.

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 →