US 7,612,080 B2 · GTPase inhibitors and use thereof for controlling platelet hyperactivity

Abstract

The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac GTPase, and methods of treating pathological conditions associated or related to a Rho family GTPase, including Rac. The preferred embodiments also relate to methods of using such compounds, or derivatives thereof, e.g., in therapeutics, diagnostics, and as research tools.

Claims9

Dependent claims

A method for treating platelet hyperreactivity in a subject, comprising administering to the subject in need thereof an effective amount of at least one compound having the formula (IIa):

wherein:
R1 to R2 are independently selected from the group consisting of H, —X-Alk, —X-Alk-X′, and —X—Y—X′;
wherein
X is —CR7R8;
X′ is —CHR7R8;
Alk is a C2-C18 substituted or unsubstituted hydrocarbon chain;
Y is a C2-C8 substituted or unsubstituted alkylene chain;
R6 is H or (C1-C4) alkyl;
and
R7 and R8 are independently selected from the group consisting of H and (C1-C4) alkyl;
or a salt of a compound of formula (IIa), wherein the platelet hyperreactivity is a condition selected from the group consisting of arterial thrombosis, stroke, atherosclerosis, Kawasaki syndrome, and moyamoya.

8 more elements

Dependencies are inferred from the claim text.

Facts

Application

11/283,556Filed 18 Nov 2005 · us provisional application

Priority

19 Nov 2004

Published

US 2006/0135542 A122 Jun 2006

Granted

3 Nov 2009

Term ends

Not estimatedThe source records don’t support an estimate.

Classification5 codes

A61K 31/506
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: not condensed and containing further heterocyclic rings
A61P 7/02
Drugs for disorders of the blood or the extracellular fluid: antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/00
Drugs for disorders of the cardiovascular system
A61K
Medicines and medical preparations

GTPase inhibitors and use thereof for controlling platelet hyperactivity

Life of this patent

GTPase inhibitors and use thereof for controlling platelet hyperactivity

Life of this patent

Abstract

Claims9