Cancer Research Technology Limited

Cyclacel Limited

Vernalis (Cambridge) Limited

Institute of Cancer Research of Royal Cancer Hospital

Paul Workman

Florence Irene Raynaud

Bernard Paul Nutley

Edward McDonald

Peter Martin Fischer

Stuart Wilson

Niall Morrison Barr Martin

Bernard Thomas Golding

Graeme Cameron Murray Smith

Roger John Griffin

David Richard Newell

Ian Robert Hardcastle

Michael Jarman

Laurent Jean Martin Rigoreau

Nicola Curtin

Hilary Alan Calvert

Xiao-ling Fan Cockcroft

Vincent Junior Ming-lai Loh

Brian William Dymock

Martin James Drysdale

Xavier Barril-Alonso

Laurence Pearl

Chrisostomos Prodromou

Mike Jarman

Ted McDonald

Edward Mcdonald

The present invention relates to compounds of formula 1  A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.

Purine derivatives

The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein Rand Rare independently hydrogen, an optionally substituted Calkyl group, Cheterocyclyl group, or Caryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CRand O, O and CR'and NR&#x2033;and N, where the unsaturation is in the appropriate place in the ring, and where one of Rand Ror R&#x2032;is an optionally substituted Cheteroaryl or Caryl group, and the other of Rand Ror R&#x2032;is H, or Rand Ror R&#x2033;together are &#x2014;A&#x2014;B&#x2014;, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.

DNA-PK inhibitors

The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.

2,6,9-substituted purine derivatives and their use in the treatment of proliferative disorders

The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.

The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, wherein A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.

The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Aris independently: a Caryl group, and is optionally substituted; Aris independently: a Caryl group, and is optionally substituted; Ris independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; Calkyl; Cheterocycyl; or Caryl; R&#x3c;SP&#x3e;N&#x3c;/SP&#x3e; is independently: &#x2014;H; Calkyl; Cheterocycyl; or, Caryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, such compounds for medical use, such compounds use in the treatment of conditions mediated by HSP90, including, for example, cancer, and use of such compounds in the preparation of medicaments for such treatments.

3,4-diarylpyrazoles and their use in the therapy of cancer

The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein Rand Rare independently hydrogen, an optionally substituted Calkyl group, Cheterocyclyl group, or Caryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CRand O, O and CR'and NR&#x2033;and N, where the unsaturation is in the appropriate place in the ring, and where one of Rand Ror R&#x2032;is an optionally substituted Cheteroaryl or Caryl group, and the other of Rand Ror R&#x2032;is H, or Rand Ror R&#x2033;together are -A-B&#x2014;, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.

The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein Rand Rare independently hydrogen, an option ally substituted Calkyl group, Cheterocyclyl group, or Caryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and Ris an optionally substituted Cheterocyclyl or Caryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK, 

Thiopyrane-4-ones as DNA protein kinase inhibitors

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Paul Workman