IP Library › Granted Patent US 7,659,274
Granted Patent B2
US 7,659,274 · App. 11/657,156 · Granted Feb 9, 2010

Unsaturated mTOR inhibitors

Assignee: OSI Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 7,659,274
App. No.
11/657,156
Granted
Feb 9, 2010
Kind
B2
Abstract

Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

Claims (16)

1. A compound represented by Formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

X 1 and X 2 are both CH;

X 4 , X 6 , and X 7 are all C;

X 3 and X 5 are both N;

R 3 is cycloC 3-10 alkyl or heterocyclyl, either of which is optionally substituted by —C(O)O(CH 2 ) aa hetaryl, —C(O)(CH 2 ) aa hetaryl, —C(O)O(CH 2 ) aa aryl, —C(O)(CH 2 ) aa aryl, or —C(O)OC 0-6 alkyl;

Q 1 is —A—(K) m

A is vinyl or acetylenyl

K is aryl or hetaryl, either optionally substituted by halogen;

m is 1;

aa is 0 or 1; and

provided that the compound is not

3-cyclobutyl-1-[(4-phenoxyphenyl)ethynyl]imidazo[1,5-a]pyrazin-8-amine, 3-cyclobutyl-1-[(1-methyl-1H-imidazol-5-yl)ethynyl]imidazo[1,5-a]pyrazin-8-amine, N-{3-[(8-amino-3-cyclobutylimidazo[1,5-a]pyrazin-1-yl)ethynyl]phenyl}-4-chlorobenzamide or 3-cyclobutyl-1-(pyridin-4-ylethynyl)imidazo[1,5-a]pyrazin-8-amine.

2. The compound according to claim 1 , selected from

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2007
From: CREW, ANDREW PHILIP; WERNER, DOUGLAS S.; TAVARES, PAULA A.R.
To: OSI PHARMACEUTICALS, INC.
Reel/Frame 019826/0173 →
Continuity (2)
Provisional Application 6076207600 · Jan 25, 2006
Related Publication 20070254883A1 · Nov 1, 2007