IP Library Granted Patent US 8,329,697
Granted Patent B2
US 8,329,697 · App. 12/811,911 · Granted Dec 11, 2012

Imidizo[1,2-A]pyrazines useful as AHCY hydrolase inhibitors

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Quick Facts
Patent No.
US 8,329,697
App. No.
12/811,911
Granted
Dec 11, 2012
Kind
B2
Abstract

The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.

Claims (36)

1. A compound of formula (I):

or a pharmaceutically acceptable salt thereof, wherein

X—Y is selected from the group consisting of

(1) CH 2 —CR 1 R 2 ,

(2) CH═CR 1 ;

R 1 is selected from the group consisting of

(1) hydrogen,

(2) hydroxy,

(3) —C 1-6 alkyl, wherein said alkyl is optionally substituted with

(a) halogen, or

(b) hydroxy; and

R 2 is selected from the group consisting of

(1) hydrogen,

(2) hydroxy,

(3) —C 1-6 alkyl, wherein said alkyl is optionally substituted with

(a) halogen, or

(b) hydroxy.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein X—Y is CH 2 —CR 1 R 2 , and R 1 is selected from the group consisting of

(1) hydrogen, and

(2) —C 1-3 alkyl, wherein said alkyl is optionally substituted with

(a) halogen, or

(b) hydroxy.

3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein X—Y is CH 2 —CR 1 R 2 , and R 1 is selected from the group consisting of

(1) hydrogen, and

(2) —CH 2 OH.

4. The A compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein X—Y is CH═CR 1 , and R 1 is selected from the group consisting of

(1) hydrogen, and

(2) —C 1-3 alkyl, wherein said alkyl is optionally substituted with

(a) halogen, or

(b) hydroxy.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein CH═CR 1 , and R 1 is selected from the group consisting of

(1) hydrogen, and

(2) —CH 2 OH.

6. The compound of claim 1 , which is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

7. The pharmaceutical composition comprising a compound of any of claims 1 - 6 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (3)
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 7, 2010
From: GARBACCIO, ROBERT M.; CONVERSO, ANTONELLA; FRALEY, MARK E.; HARTINGH, TIMOTHY J.
To: MERCK SHARP & DOHME CORP
Reel/Frame 024645/0598 →