Kudos Pharmaceuticals Limited

Maybridge Limited

Cancer Research Technology Limited

Other

Astrazeneca Ab

Graeme Cameron Murray Smith

Niall Morrison Barr Martin

Keith Allan Menear

Roger John Griffin

Laurent Jean Martin Rigoreau

Marc Geoffrey Hummersone

Bernard Thomas Golding

David Richard Newell

Ian Robert Hardcastle

Nicola Curtin

Xiao-ling Fan Cockcroft

Heather Mary Ellen Duggan

Frederic Georges Marie Leroux

Xiao-Ling Fan Cockcroft

Frank Kerrigan

Charles Richard White

Roger Frank Newton

Stephen Philip Jackson

Alan Ashworth

Hilary Alan Calvert

Sylvie Gomez

Karine Fabienne Malagu

Muhammad Hashim Javaid

Penny Jane Eversley

Paul Workman

Bernard Paul Nutley

Florence Irene Raynaud

Kappusamy Saravanan

Vincent Junior Ming-lai Loh

Ian Timothy Williams Matthews

Julia Vile

Vincent Junior M Loh

Stefano Forte

Ian Timothy William Matthews

Diane Gillian Douglas

Mark O'Connor

Mark Frigerio

Marine Desage-El Murr

Vincent Junior Ming-Iai Loh

Naill Morrison Barr Martin

Janet Hoare

Lesley Dixon

Nicholas David Lakin

Alan Yin Kai Lau

Alan John Whittle

Karine Malagu

Diana Gillian Douglas

Marc Geoffery Hummersone

Niall Morrisson Barr Martin

Gesine Johanna Hermann

There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors

Compounds

A compound of the formula (I): wherein: where Yis selected from CH and N, Yis selected from CH and N, Yis selected from CH, CF and N; and where Q is O or S; wherein

Phthalazinone derivatives

A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein:

A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: Rand Rare independently selected from 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; Q is &#x2014;NH&#x2014;C(&#x2550;O)&#x2014; or &#x2014;O&#x2014;; Y is an optionally substituted Calkylene group; X is selected from SRor NRR, wherein, R, or Rand Rare independently selected from hydrogen, optionally substituted Calkyl, Caryl, or Cheterocyclyl groups, or Rand Rmay together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is &#x2014;O&#x2014;, X is additionally selected from &#x2014;C(&#x2550;O)&#x2014;NRR, wherein Rand Rare independently selected from hydrogen, optionally substituted Calkyl, Caryl, or Cheterocyclyl groups, or Rand Rmay 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 if Q is &#x2014;NH&#x2014;C(&#x2550;O)&#x2014;, &#x2014;Y&#x2014;X may additionally be selected from Calkyl.

DNA-PK inhibitors

Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of:

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.

A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRor CRR; if X&#x2550;NRthen n is 1 or 2 and if X&#x2550;CRRthen n is 1; Ris selected from the group consisting of H, optionally substituted Calkyl, Caryl, Cheterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; Ris selected from H, hydroxy, amino; or Rand Rmay together form a spiro-Ccycloalkyl or heterocyclyl group; Rand Rare independently selected from the group consisting of hydrogen and Calkyl, or when X is CRR, R, R, R, Rand R, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; Ris selected from H and halo; and Het is selected from: where Yis selected from CH and N, Yis selected from CH and N, Yis selected from CH, CF and N, where only one or two of Y, Yand Ycan be N; and where Q is O or S.

A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein:

ATM inhibitors

Compounds of formula I:A-B-C&#x2003;&#x2003;(I)and isomers, salts, solvates, chemically protected forms, and prodrugs thereof are provided, wherein variables A, B and C are defined herein and wherein such compounds act as mTor inhibitors.

mTOR inhibitor compounds

Growing community of inventors

Cambridge, United Kingdom

Graeme Cameron Murray Smith