IP Library Granted Patent US 7,713,985
Granted Patent B2
US 7,713,985 · App. 11/767,624 · Granted May 11, 2010

Adenosine A

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Quick Facts
Patent No.
US 7,713,985
App. No.
11/767,624
Granted
May 11, 2010
Kind
B2
Abstract

Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X 1 and X 2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF 3 , —OCF 3 , alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R 1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

Claims (18)

1. A compound represented by the structural formula

or a pharmaceutically acceptable salt thereof, wherein:

X 1 is 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF 3 , —OCF 3 , alkoxy, —OH and —CN;

X 2 is 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF 3 , —OCF 3 , alkoxy, —OH and —CN;

n is 0, 1 or 2; and

R and R 1 are independently selected from the group consisting of H and alkyl.

2. A compound of claim 1 wherein n is 1.

3. A compound of claim 1 wherein R and R 1 are each H.

4. A compound of claim 1 wherein X 1 is 1 or 2 substituents independently selected from H, halo, alkyl, alkoxy and —CF 3 .

5. A compound of claim 4 wherein X 1 is 1 or 2 substituents independently selected from H, fluoro, chloro, methyl, methoxy and —CF 3 .

6. A compound of claim 1 wherein X 2 is 1, 2 or 3 substituents independently selected from H, halo, alkyl, alkoxy, —CF 3 , —OCF 3 and —CN.

7. A compound of claim 6 wherein X 2 is 1, 2 or 3 substituents independently selected from H, fluoro, chloro, methyl, methoxy, —CF 3 , —OCF 3 and —CN.

8. A compound of claim 1 wherein n is 1; R and R 1 are each H; X 1 is 1 or 2 substituents independently selected from H, halo, alkyl, alkoxy and —CF 3 ; and X 2 is 1, 2 or 3 substituents independently selected from H, halo, alkyl, alkoxy, —CF 3 , —OCF 3 and —CN.

9. A compound of claim 8 wherein X 1 is 1 or 2 substituents independently selected from H, fluoro, chloro, methyl, methoxy and —CF 3 , and X 2 is 1, 2 or 3 substituents independently selected from H, fluoro, chloro, methyl, methoxy, —CF 3 , —OCF 3 and —CN.

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

11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier.

12. A pharmaceutical composition comprising a therapeutically effective amount of a combination of a compound of claim 1 and one to three other agents useful in treating Parkinson's disease in a pharmaceutically acceptable carrier.

13. A kit comprising in separate containers in a single package pharmaceutical compositions for use in combination to treat Parkinson's disease wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, in separate containers, one or more pharmaceutical compositions each comprise an effective amount of an agent useful in the treatment of Parkinson's disease in a pharmaceutically acceptable carrier.

Assignments (3)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 26, 2008
From: CLASBY, MARTIN C.; CHACKALAMANNIL, SAMUEL; STAMFORD, ANDREW
To: SCHERING CORPORATION
Reel/Frame 021444/0271 →