IP Library Granted Patent US 6,960,603
Granted Patent B2
US 6,960,603 · App. 10/646,256 · Granted Nov 1, 2005

Prenylation inhibitors and methods of their synthesis and use

Assignee: PPD Discovery, Inc.
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Quick Facts
Patent No.
US 6,960,603
App. No.
10/646,256
Granted
Nov 1, 2005
Kind
B2
Abstract

The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.

Claims (19)

1. A compound of the formula:

wherein

R1 is a halogenated phenyl;

R2 is bicyclo[2.2.1]heptane, cyclopropane or cyclohexane; and,

R3 is NH2, OH or 2-amino-3-phenylpropanamide.

2. The compound of claim 1 , wherein R1 is 3,4-dichlorophenyl.

3. The compound of claim 1 , wherein R1 is 3-chlorophenyl.

4. The compound of claim 1 , wherein R3 is OH.

5. The compound of claim 1 , wherein R3 is 2-amino-3-phenylpropanamide.

6. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically-acceptable salt thereof, and a pharmaceutically-acceptable carrier.

7. A method of treating colon cancer comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula:

wherein

R1 is a halogenated phenyl;

R2 is bicyclo[2.2.1]heptane, cyclopropane or cyclohexane; and,

R3 is NH2, OH or 2-amino-3-phenylpropanamide.

8. The method of claim 7 , wherein R1 is 3,4-dichlorophenyl.

9. The method of claim 7 , wherein R1 is 3-chlorophenyl.

10. The method of claim 7 , wherein R3 is OH.

11. The method of claim 7 , wherein R3 is 2-amino-3-phenylpropanamide.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded Sep 2, 2015
From: CREDIT SUISSE AG, CAYMAN ISLANDS BRANCH, AS ADMINISTRATIVE AGENT
To: PHARMACEUTICAL PRODUCT DEVELOPMENT, LLC; PPD DEVELOPMENT, L.P.; PHARMACO INVESTEMENTS, INC.; X-CHEM, INC.
Reel/Frame 036481/0051 →
SECURITY AGREEMENT Recorded Dec 6, 2011
From: PHARMACEUTICAL PRODUCT DEVELOPMENT, INC.; PPD DEVELOPMENT, LP; PHARMACO INVESTMENTS INC. AND DUKE UNIVERSITY; PHARMACO INVESTMENTS INC.
To: CREDIT SUISSE AG, CAYMAN ISLANDS BRANCH, AS ADMINISTRATIVE AGENT
Reel/Frame 027334/0106 →
MERGER Recorded Feb 3, 2009
From: PPD DISCOVERY, INC.
To: PHARMACEUTICAL PRODUCT DEVELOPMENT, INC.
Reel/Frame 022191/0690 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 20, 2007
From: PHARMACEUTICAL PRODUCT DEVELOPMENT, INC.
To: PHARMACO INVESTMENTS, INC.
Reel/Frame 018907/0953 →
Continuity (3)
Division 1033628500 · Jan 3, 2003
Continuation In Part 1021962800 · Aug 14, 2002
Related Publication 20040053970A1 · Mar 18, 2004