Phthalazinone derivatives
AssigneesKudos Pharmaceuticals Limited, Maybridge Limited
InventorsNiall Morrison Barr Martin, Graeme Cameron Murray Smith, Penny Jane Eversley, Xiao-Ling Cockcroft, Frank Kerrigan, Janet Hoare, Lesley Dixon
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Abstract
A compound of formula: 1 or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from: 2 and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.
Claims28
A compound of formula:
- 91
- or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein:
- A and B together represent an optionally substituted, fused aromatic ring;
- RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted;
- wherein R2 is selected from:
- 92
- wherein:
- n is 0 or 1;
- Y is selected from NRN1 and CRC1RC2;
- RN1 is selected from H, optionally substituted C1-10 alkyl, optionally substituted C5-6 aryl and optionally substituted C1-10 alkylacyl;
- RC1, RC2, RC3, RC4, RC5, RC6, RC7 and RC8 are independently selected from H, R, SR and NHC(═O)OR, where R is optionally substituted C1-10 alkyl or optionally substituted C5-6 aryl;
- RC4 and RC6, RC6 and RC8 or RC8 and RC2 may optionally together form a double bond;
- RC1 and RC2, RC5 and RC6 or RC7 and RC8 together with the carbon atom to which they are attached may optionally form a spiro-fused C5-7 carbocylic or heterocyclic ring;
- and
- RC5 and RC7 or RC7 and RC1 together with the carbon atoms to which they are attached form an optionally substituted ring system;
- b)
- 93
- wherein
- m is 0 or 1;
- X is selected from NRN2 and CRC9RC10;
- RN2 is selected from H, optionally substituted C1-10 alkyl, optionally substituted C5-6 aryl and optionally substituted C1-10 alkylacyl;
- RC9, RC10, RC11, RC12, RC13 and RC14 are independently selected from H, R, SR and NHC(═O)OR, where R is as defined above;
- RC12 and RC10 or RC10 and RC14 may optionally together form a double bond;
- RC11 and RC12, RC9 and RC10 or RC13 and RC14 together with the carbon atom to which they are attached may optionally form a spiro-fused C5-7 carbocylic or heterocyclic ring;
- and
- RC11 and RC9 or RC9 and RC13 together with the carbon atoms to which they are attached may form an optionally substituted ring system.
Dependencies are inferred from the claim text.