Kudos Pharmaceuticals Limited

Maybridge Limited

The Institute of Cancer Research: Royal Cancer Hospital

The Institute of Cancer Research

Kudo Pharmaceuticals Limited

Graeme Cameron Smith

Stephen Philip Jackson

Alan Ashworth

Keith Allan Menear

Niall Morrison Barr Martin

Xiao-Ling Fan Cockcroft

Frank Kerrigan

Ian Timothy Williams Matthews

Vincent Junior M Loh

Niall Martin

Niall Morrison Martin

Julia Vile

Penny Jane Eversley

Ian Timothy Matthews

Mark O'Connor

Charles Richard White

Roger Frank Newton

Diane Gillian Douglas

Vincent M Loh

Compounds of the formula (I): 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 both hydrogen, or when X is CRR, R, R, Rand R, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and Ris selected from H and halo.

Phthalazinone derivatives

Compounds of the formula (I): 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 both hydrogen, or when X is CRR, R, R, Rand R, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; andRis selected from H and halo.

Compounds of the formula (I): 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 both hydrogen, or when X is CRR, R, R, Rand R, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and

The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.

DNA damage repair inhibitors for treatment of cancer

DNA damage repair inhibitors for the treatment of cancer

Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRor CRR; if X=NRthen n is 1 or 2 and if X=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 both hydrogen, or when X is CRR, R, R, Rand R, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and Ris selected from H and halo.

Growing community of inventors

Cambridge, United Kingdom

Graeme Cameron Smith