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Last Updated: December 13, 2025

Claims for Patent: 7,151,102


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Summary for Patent: 7,151,102
Title:Phthalazinone derivatives
Abstract: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 and B together represent an optionally substituted, fused aromatic ring; RC is represented by —L—RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.
Inventor(s):Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Charles Richard White, Roger Frank Newton, Diane Gillian Douglas, Penny Jane Eversley, Julia Vile
Assignee:Kudos Pharmaceuticals Ltd
Application Number:US10/021,506
Patent Claims: 1. A compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent optionally monosubstituted, fused benzene; RC is —CH2—RL; RL is substituted phenyl, wherein the substituents are selected from the group consisting of: C3-20 heterocyclyl; ester; amido; acyloxy; sulfonamido; ureido; and optionally further substituted; and RN is hydrogen.

2. A compound according to claim 1, wherein the fused benzene is unsubstituted.

3. A compound according to claim 1, wherein RL is substituted by a ureido group, or a sulfonamido group.

4. A pharmaceutical composition comprising a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused benzene; RC is —CH2—RL; RL is optionally substituted phenyl; and RN is hydrogen; and a pharmaceutically acceptable carrier or diluent.

5. The pharmaceutical composition of claim 4, wherein the fused benzene is unsubstituted.

6. The pharmaceutical composition of claim 4, wherein RL is substituted by one or more substituents selected from the group consisting of: C1-7 alkyl; C5-20 aryl; C3-20 heterocyclyl; halo; hydroxy; ether; nitro; cyano; carbonyl groups; amino; sulfonamido; ureido; acyloxy; thiol; thioether; sulfoxide; and sulfone.

7. The pharmaceutical composition of claim 6, wherein RL is substituted by a ureido group, or a sulfonamido group.

8. A compound of the formula: or an isomer, salt, solvate, chemically protected form and prodrug thereof.

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