IP Library Granted Patent US 7,589,097
Granted Patent B2
US 7,589,097 · App. 12/003,110 · Granted Sep 15, 2009

Triazol[4,5-d] pyramidine derivatives and their use as purinergic receptor antagonists

Assignee: Vernalis Research Limited
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Quick Facts
Patent No.
US 7,589,097
App. No.
12/003,110
Granted
Sep 15, 2009
Kind
B2
Abstract

The use of a compound of formula (I): wherein R 1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR 5 R 6 , NR 4 COR 5 , NR 4 CONR 5 R 6 , NR 4 CO 2 R 7 and NR 4 SO 2 R 7 ; R 2 is selected from aryl attached via an unsaturated carbon; R 3 is selected from H, alkyl, COR 5 , CO 2 R 7 , CONR 5 R 6 , CONR 4 NR 5 R 6 and SO 2 R 7 ; R 4 , R 5 and R 6 are independently selected from H, alkyl and aryl or where R 5 and R 6 are in an NR 5 R 6 group, R 5 and R 6 may be linked to form a heterocyclic group, or where R 4 , R 5 and R 6 are in a (CONR 4 NR 5 R 6 ) group, R 4 and R 5 may be linked to form a heterocyclic group; and R 7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A 2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.

Claims (10)

1. A method of treating a patient suffering from Parkinson's disease comprising administering to the patient an effective dose of a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof,

at least one additional drug useful in the treatment of Parkinson's disease and

at least one pharmaceutically acceptable carrier,

wherein

R 1 is selected from the group consisting of H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR 5 R 6 , NR 4 COR 5 , NR 4 CONR 5 R 6 , NR 4 CO 2 R 7 and NR 4 SO 2 R 7 ;

R 2 is an aryl attached via an unsaturated ring carbon of said aryl group;

R 3 is selected from the group consisting of H, alkyl, COR 5 , CO 2 R 7 , CONR 5 R 6 , CONR 4 NR 5 R 6 and SO 2 R 7 ;

R 4 , R 5 and R 6 are independently selected from the group consisting of H, alkyl and aryl, or where R 5 and R 6 are in an NR 5 R 6 group, R 5 and R 6 may be linked to form a heterocyclic group, or where R 4 , R 5 and R 6 are in a (CONR 4 NR 5 R 6 ) group, R 4 and R 5 may be linked to form a heterocyclic group; and

R 7 is selected from the group consisting of alkyl and aryl.

2. The method according to claim 1 , wherein the at least one additional drug is evodopa (L-DOPA) or a dopamine agonist.

Assignments (3)
CHANGE OF NAME Recorded Jan 24, 2022
From: VERNALIS DEVELOPMENT LIMITED
To: LIGAND UK DEVELOPMENT LIMITED
Reel/Frame 058738/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 24, 2022
From: VERNALIS (R&D) LIMITED
To: VERNALIS DEVELOPMENT LIMITED
Reel/Frame 058822/0570 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 13, 2014
From: VERNALIS RESEARCH LIMITED
To: VERNALIS (R&D) LIMITED
Reel/Frame 031949/0742 →
Priority Claims (1)
GB 0100624.6 · Jan 10, 2001 · national
Continuity (3)
Division 1150762500 · Aug 22, 2006
Continuation 1025094200
Related Publication 20080234296A1 · Sep 25, 2008