Vernalis Research Limited

Vernalis &r&d) Ltd.

Roger John Gillespie

Joanne Lerpiniere

Suneel Gaur

Richard Simon Todd

Samantha Jane Bamford

Gemma Caroline Stratton

Claire Elizabeth Dawson

Scott Murray Weiss

Simon Edward Ward

Stefania Leonardi

Samantha Jayne Bamford

Robert Mark Pratt

Nathaniel Julius Thomas Monck

Lars Jacob Stray Knutsen

Paul Richard Giles

Andrew James Bird

Allan Michael Jordan

David Reginald Adams

Ian Anthony Cliffe

David Bebbington

David Reginald Adoms

Michael Fredrick Snape

Michael Frederick Snape

Steven Michael McAteer

Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning. 

Triazolo[4,5-d] pyramidine derivatives and their use as purine receptor antagonists

Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning. 

Triazolo[4,5-D] pyramidine derivatives and their use as purine receptor antagonists

Triazolo [4, 5-D] pyramidine derivatives and their use as purine receptor antagonists

Triazolo[4,5-D]pyramidine derivatives and their use as purine receptor antagonists

Compounds of formula (I); wherein Ris H or NHZ; Ris optionally substituted aryl or heteroaryl attached via a carbon atom; Ris H; optionally substituted C-Calkyl, C-Calkenyl, C-Calkynyl, or CCcycloalkyl, halogen; OH or OR, or Ris H, optionally substituted C-Calkyl, CCalkenyl, C-Calkynyl, C-Ccycloalkyl, aryl or heteroaryl, Ris H or optionally substituted C-Calkyl, C-Calkenyl, C-Calkynyl, or C-Ccycloalkyl; or Rand Rtogether form a 5 or 6-membered heterocyclic ring; and Ris optionally substituted C-Calkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease. 

Pyrimidine compounds as purine receptor antagonist

Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: Ris selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NRR, NRCOR, NRCONRR, NRCOR, and NRSOR; Ris a heteroaryl attached via an unsaturated ring carbon of said heteroaryl group; Ris selected from: H, alkyl, halogen, OR, SR, and NRR; Ris selected from: H, acyclic alkyl, CONRR, CONRNRR, COR, COR, and SOR; R, R, and Rare independently selected from: H, alkyl, and aryl, or where Rand Rare in an NRRgroup, Rand Rmay be linked to form a hetero cyclic group, or where R, Rand Rare in a (CONRNRR) group, Rand Rmay be linked to form a heterocyclic group; and Ris selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof.

Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists

Use of a compound of the formula (I) wherein Ris selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NRR, NRCOR, NRCORand NRSOR; Ris selected from aryl attached via an unsaturated carbon; Rand Rare independently selected from H, alkyl, halogen, alkoxy, alkylthio, CN and NRR; Ris selected from H, acyclic alkyl, COR, CONRR, CONRNRR, CORand SOR; R, Rand Rare independently selected from H, alkyl and aryl or where Rand Rare in an NRRgroup Rand Rmay be linked to form a hererocyclic group, or where R, Rand Rare in a (CONRNRR) group, Rand Rmay be linked to form a hererocyclic group; and Ris selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly Areceptors, 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 subect; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se. 

Pyrrolo [2,3-d] pyrimidine and their use as purinergic receptor antagonists

The use of a compound of formula (I): wherein

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

Use of a compound of formula (I) wherein Ris selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NRR, NRCOR, NRCONRR, NRCORand NRSOR; Ris selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; Ris selected from H, alkyl, COR, CONRR, CONRNRR, CORand SOR; R, Rand Rare independently selected from H, alkyl and aryl or where Rand Rare in an (NRR) group then Rand Rmay be linked to form a heterocyclic ring; Ris selected from alkyl and aryl; R, Rand Rare independently selected from H, alkyl and aryl, or Rand Rmay be linked to form a heterocyclic ring, or where R, Rand Rare in a (CONRNRR) group, Rand Rmay be linked to form a heterocyclic group; and R, 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 Areceptors, 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. 

Purine derivatives as purinergic receptor antagonists

Triazolo [4,5-d] pyrimidine derivatives and their use as purinergic receptor antagonists

A compound of formula (I), wherein X is S or O; Ris selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, COR, COR, CONRR, CONRNRR, NRR, NRCONRR, NRCOR, NRCOR, and NRSOR; Ris selected from aryl attached via an unsaturated carbon atom; Ris selected from H, alkyl, hydroxy, alkoxy, halogen, CN and NO; Ris selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, NO, COR, COR, CONRR, CONRNRR, NRR, NRCONRR, NRCOR, NRCORand NRSOR; R, Rand Rare independently selected from H, alkyl and aryl or where Rand Rare in an (NRR) group, Rand Rmay be linked to form a heterocyclic group, or where R, Rand Rare in a (CONRNRR) group, Rand Rmay be linked to form a heterocyclic group; and Ris selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, and the use thereof in therapy and in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly Areceptors, may be beneficial, particularly wherein said disorder is a movement disorder such a Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or wherein said medicament is for neuroprotection in a subject 

Thieno(3,2-d)pyrimidines and furano(3,2-d)pyrimidines and their use as purinergic receptor antagonists

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Wokingham, United Kingdom

Roger John Gillespie