IP Library Granted Patent US 7,326,713
Granted Patent B2
US 7,326,713 · App. 11/092,809 · Granted Feb 5, 2008

Substituted tricyclic compound as protein kinase inhibitors

Assignees: Arizona board of Regents on Behalf of the University of Arizona; Montigen Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 7,326,713
App. No.
11/092,809
Granted
Feb 5, 2008
Kind
B2
Abstract

Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Claims (21)

1. A compound having the following structure:

or a stereoisomer, or pharmaceutically acceptable salt thereof, wherein:

X is NH, S or O;

Z is CH or N, with the proviso when X═NH then Z═CH;

R 1 and R 2 are the same or different and are independently hydrogen, hydroxyl, halo, —CN, —NO 2 , —NH 2 , —R, —OR, —SCH 3 , —CF 3 , —C(═O)OR or OC(═O)R, where R is alkyl or substituted alkyl;

R 3 is hydrogen, —NH 2 , alkyl, —CN, or —NO 2 ,

L 2 is selected from —NHCH 2 —, —NH—, —C(═S)NH—, —NHC(═S)—, —C(═S)NHCH 2 —, —NHC(═S)NH—, —NHC(═O)—, —NHC(═O)NH—; —S(═O) 2 —; and

Cycl 2 is

2. The compound of claim 1 , wherein L 2 is —C(═S)NHCH 2 —.

3. The compound of claim 1 , wherein R 1 and R 2 are selected from —R or —OR where R is alkyl or substituted alkyl, hydroxyl, halo, —CF 3 or —OC(═O)CH 3 , and R 3 is selected from hydrogen or —NH 2 .

4. The compound of claim 1 , wherein R 1 and R 2 are selected from —OCH 3 , —Cl, or —CF 3 , and R 3 is hydrogen.

5. A compound having the following structure:

or a stereoisomer, or pharmaceutically acceptable salt thereof, wherein:

R 1 and R 2 are the same or different and are independently hydrogen, hydroxyl, halo, —CN, —NO 2 , —NH 2 , —R, —OR, —SCH 3 , —CF 3 , —C(═O)OR or —OC(═O)R, where R is alkyl or substituted alkyl;

R 3 is hydrogen, —NH 2 , alkyl, —CN, or —NO 2 ; and

Cycl 2 is

6. The compound of claim 5 , wherein R 1 and R 2 are selected from —R or —OR where R is alkyl or substituted alkyl, hydroxyl, halo, —CF 3 , or —OC(═O)CH 3 , and R 3 is hydrogen.

7. The compound of claim 5 , wherein R 1 and R 2 are selected from —OCH 3 , —CF 3 or —Cl, and R 3 is hydrogen.

8. A compound having the following structure:

9. A compound having the following structure:

10. A composition comprising a compound of any one of claims 1 , 5 , 8 and 9 in combination with a pharmaceutically acceptable excipient.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 16, 2015
From: ASTEX PHARMACEUTICALS, INC.
To: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
Reel/Frame 036807/0313 →
MERGER/NAME CHANGE Recorded Dec 2, 2011
From: SUPERGEN, INC.
To: ASTEX PHARMACEUTICALS, INC.
Reel/Frame 027316/0285 →
CONFIRMATORY LICENSE Recorded Jul 24, 2008
From: UNIVERSITY OF ARIZONA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 021290/0474 →
MERGER Recorded Dec 7, 2007
From: MONTIGEN PHARMACEUTICALS, INC.
To: SUPERGEN, INC.
Reel/Frame 020212/0073 →
Continuity (5)
Continuation 1096531300 · Oct 14, 2004
Provisional Application 6060852900 · Sep 9, 2004
Provisional Application 6051148600 · Oct 14, 2003
Provisional Application 6051148900 · Oct 14, 2003
Related Publication 20050239793A1 · Oct 27, 2005