IP Library Granted Patent US 7,317,017
Granted Patent B2
US 7,317,017 · App. 11/189,202 · Granted Jan 8, 2008

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Quick Facts
Patent No.
US 7,317,017
App. No.
11/189,202
Granted
Jan 8, 2008
Kind
B2
Abstract

Disclosed are novel A 2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Claims (24)

1. A compound of the Formula I or Formula II:

wherein:

R 1 and R 2 are independently chosen from hydrogen or loweralkyl;

R 3 hydrogen,;

X is five or six membered monocyclic arylene or heteroarylene that is attached to the purine ring at a carbon atom;

Y is a covalent bond or alkylene in which one carbon atom can be optionally replaced by —O—, —S—, or —NH—; and

Z is optionally substituted monocyclic aryl or optionally substituted monocyclic heteroaryl.

2. The compound of claim 1 , wherein,

X is phenylene or pyrazolene,

Y is lower alkylene in which one carbon atom can be optionally replaced by —O—, —S—, or —NH—, and

Z is optionally substituted phenyl, optionally substituted oxadiazolyl, optionally substituted isoxazolyl, or optionally substituted pyridyl.

3. The compound of claim 2 , wherein R 1 is lower alkyl and R 2 is hydrogen.

4. The compound of claim 2 , wherein X is optionally substituted 1,4-pyrazolene.

5. The compound of claim 2 , wherein Z is optionally substituted phenyl.

6. The compound of claim 2 , wherein Z is optionally substituted oxadiazolyl.

7. The compound of claim 2 , wherein Z is optionally substituted pyridyl.

8. The compound of claim 2 , wherein Z is optionally substituted isoxazolyl.

9. The compound of claim 2 , wherein R 1 is hydrogen and R 2 is lower alkyl.

10. The compound of claim 2 , wherein R 1 and R 2 are independently lower alkyl.

11. The compound of claim 2 , wherein X is phenylene.

12. The compound of claim 2 , wherein Y is methylene.

13. The compound of claim 2 , wherein Y is —O—CH 2 —.

14. The compound of claim 1 , wherein Y is a covalent bond.

15. A pharmaceutical composition comprising a therapeuticially effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2011
From: KALLA, RAO; PERRY, THAO; ELZEIN, ELFATIH; VARKHEDKAR, VAIBHAV; LI, XIAOFEN; IBRAHIM, PRABHA; PALLE, VENKATA; XIAO, DENGMING; ZABLOCKI, JEFF
To: CV THERAPEUTICS, INC.
Reel/Frame 027102/0294 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 18, 2011
From: GILEAD PALO ALTO, INC.
To: GILEAD SCIENCES, INC.
Reel/Frame 027077/0319 →
MERGER Recorded Apr 5, 2010
From: APEX MERGER SUB, INC.; CV THERAPEUTICS, INC.
To: GILEAD PALO ALTO, INC.
Reel/Frame 024185/0118 →