IP Library Granted Patent US 6,960,584
Granted Patent B2
US 6,960,584 · App. 10/473,763 · Granted Nov 1, 2005

Inhibitors of Akt activity

Assignee: Merck & Co., Inc.
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 6,960,584
App. No.
10/473,763
Granted
Nov 1, 2005
Kind
B2
Abstract

The present invention is directed to compounds comprising a triazolo[4,3-b]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Claims (24)

1. A compound of the formula A:

wherein

R 1 represents phenyl, furyl, thienyl or pyridinyl, any of which groups may be optionally substituted with one, two or three substituents, independently selected from:

a) halogen;

b) C 1-4 alkyl;

c) C 1-4 alkoxy;

d) cyano;

e) di(C 1-4 alkyl)amino;

f) hydroxy;

R 2 represents amino-C 1-6 alkyl, C 1-4 alkylamino-(C 1-6 )alkyl, di(C 1-4 alkyl)amino-(C 1-6 )alkyl, or C 1-4 alkoxy-(C 1-6 )alkyl; and

R 3 is selected from: C 3-7 cycloalkyl and aryl;

or a pharmaceutically acceptable salt or stereoisomer thereof.

2. The compound according to claim 1 of the formula A-I:

wherein

R 2 is as defined in claim 1 ;

R 3 is selected from: C 3-7 cycloalkyl and phenyl,

m is 0, 1, 2 or 3; and

R 5 independently represents halogen, C 1-4 alkyl or C 1-6 alkoxy;

or a pharmaceutically acceptable salt or stereoisomer thereof.

3. A pharmaceutical composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound of claim 1 .

4. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a composition of claim 3 .

5. A method for treating ovarian, pancreatic and breast cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound selected from 6-(2-hydroxyethyl)oxy-3,7-diphenyl-[1,2,4]triazolo[4,3-b]pyridazine, 6-(4-hydroxybutyl)oxy-3,7-diphenyl-[1,2,4]triazolo[4,3-b]pyridazine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

6. A pharmaceutical composition made by combining the compound of claim 1 and a pharmaceutically acceptable carrier.

7. A process for making a pharmaceutical composition comprising combining a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 20, 2005
From: CARLING, WILLIAM ROBERT; PINEIRO, JOSE LUIS CASTRO; MOORE, KEVIN WILLIAM
To: MERCK SHARP & DOHME LTD.
Reel/Frame 016548/0997 →
Continuity (2)
Provisional Application 6028280600 · Apr 10, 2001
Related Publication 20040116432A1 · Jun 17, 2004