Kudos Pharmaceuticals Limited

Maybridge Limited

Kudo Pharmaceuticals Limited

Frank Kerrigan

Keith Allan Menear

Niall Morrison Barr Martin

Xiao-Ling Fan Cockcroft

Stephen Philip Jackson

Alan Ashworth

Graeme Cameron Smith

Ian Timothy Williams Matthews

Vincent Junior M Loh

Graeme Cameron Murray Smith

Sylvie Gomez

Muhammad Hashim Javaid

Marc Geoffrey Hummersone

Xiao-ling Fan Cockcroft

Stefano Forte

Ian Timothy William Matthews

Penny Jane Eversley

Vincent Junior Ming-lai Loh

Vincent Junior Ming-Iai Loh

Naill Morrison Barr Martin

Janet Hoare

Lesley Dixon

Niall Morrison Martin

Vincent M Loh

Ian Timothy Matthews

Niall Morrison Barr Kudos Pharmac Ltd Martin

Graeme Cameron Murray Kudos Pharmac Ltd Smith

Xiao-Ling Fan Chemovation Ltd Cockcroft

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

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

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.

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.

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=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 independently selected from the group consisting of hydrogen and Calkyl, 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; 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: or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.

Growing community of inventors

Cornwall, United Kingdom

Frank Kerrigan