IP Library Granted Patent US 8,524,720
Granted Patent B2
US 8,524,720 · App. 12/651,639 · Granted Sep 3, 2013

Substituted N-(pyrazol-5-yl)-pyrrolo[3,2-D]pyrimidin-4-amine useful as protein kinase inhibitors

Inventors: David Bebbington (Newbury, GB); Hayley Binch (Encinitas, CA); Ronald Knegtel (Abindgon, GB); Julian M.C. Golec (Woolstone, GB); Sanjay Patel (Abingdon, GB); Jean-Damien Charrier (Grove, GB); David Kay (Purton, GB); Robert Davies (Watertown, MA); Pan Li (Lexington, MA); Marion Wannamaker (Bolton, MA); Cornelia Forster (Pelham, MA); Albert Pierce (Cambridge, MA)
Assignee: Vertex Pharmaceuticals Incorporated
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Quick Facts
Patent No.
US 8,524,720
App. No.
12/651,639
Granted
Sep 3, 2013
Kind
B2
Abstract

This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x and R y are independently selected from T-R 3 , or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R 2 , R 2′ , T, and R 3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Claims (9)

1. A compound of formula IV-34;

2. A composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

3. The composition according to claim 2 further comprising a second therapeutic agent.

4. A method of inhibiting Glycogen Synthase Kinase-3 or Aurora activity in a biological sample comprising contacting said biological sample with the compound according to claim 1 .

5. A method of enhancing glycogen synthesis in a patient in need thereof, which method comprises the step of administering to a patient a therapeutically effective amount of the composition according to claim 2 .

6. A method of lowering blood levels of glucose in a patient in need thereof, which method comprises the step of administering to a patient a therapeutically effective amount of the composition according to claim 2 .

7. A method of treating colon, ovarian, or breast cancer in a patient in need thereof, comprising the step of administering to said patient a therapeutically effective amount of the composition according to claim 2 .

8. A method of treating diabetes in a patient in need thereof, comprising the step of administering to said patient a therapeutically effective amount of the composition according to claim 2 .

9. A method of treating schizophrenia in a patient in need thereof, comprising the step of administering to said patient a therapeutically effective amount of the composition according to claim 2 .

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Oct 14, 2016
From: MACQUARIE US TRADING LLC
To: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 040357/0001 →
SECURITY INTEREST Recorded Jul 10, 2014
From: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: MACQUARIE US TRADING LLC
Reel/Frame 033292/0311 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 12, 2013
From: BEBBINGTON, DAVID; BINCH, HAYLEY; KNEGTEL, RONALD; GOLEC, JULIAN; PATEL, SANJAY; CHARRIER, JEAN-DAMIEN; KAY, DAVID; DAVIES, ROBERT; LI, PAN; WANNAMAKER, MARION; FORSTER, CORNELIA; PIERCE, ALBERT
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 030202/0490 →
Continuity (7)
Division 11369220 · Mar 6, 2006
Division 10624800 · Jul 22, 2003
Division 09952671 · Sep 14, 2001
Provisional Application 60232795 · Sep 15, 2000
Provisional Application 60257887 · Dec 21, 2000
Provisional Application 60286949 · Apr 27, 2001
Related Publication 20100256170A1 · Oct 7, 2010