Vernalis Research Limited

Joanne Lerpiniere

Roger John Gillespie

Suneel Gaur

Gemma Caroline Stratton

Scott Murray Weiss

Claire Elizabeth Dawson

Samantha Jayne Bamford

Stefania Leonardi

Robert Mark Pratt

Lars Jacob Stray Knutsen

Paul Richard Giles

David Reginald Adams

Ian Anthony Cliffe

Simon Edward Ward

David Bebbington

David Reginald Adoms

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

The use of a compound of formula (I): wherein Ris selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NRR, NRCONR, NRCONRR,NRCORand NRSOR; Ris selected from aryl attached via an unsaturated carbon; Ris selected from H, alkyl, COR, COR, CONRR, CONRNRRand 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 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, 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 

Triazolo[4,5-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 subject; 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

Use of a compound of formula (I): wherein Ris selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NRR, NRCOR, NRCONRR, NRCORand NRSOR; Ris selected from heteroaryl attached via an unsaturated carbon; Ris selected from H, alkyl, halogen, OR, SRand NRR; Ris selected from H, acyclic alkyl, CONRR, CONRNRR, COR, 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 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, 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. 

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

Thieno-and furopyrimidine derivatives as A2A-receptor antagonists

Use of a compound of formula (I) as defined herein, or a pharmaceutically acceptable salt 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 A receptors, may be beneficial, such as a movement disorder, for example, Parkinson's Disease or progressive supemuclear palsy, Huntingtons disease, multiple system atrophy, corticobasal degeneration, Wilsons disease, Hallerrorder-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.

Growing community of inventors

Wokingham, United Kingdom

Joanne Lerpiniere