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: ##STR00001## or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; R.sub.C is represented by --L--R.sub.L, where L is of formula: --(CH.sub.2).sub.n1-Q.sub.n2-(CH.sub.2).sub.n3-- wherein n.sub.1, n.sub.2 and n.sub.3 are each selected from 0, 1, 2 and 3, the sum of n.sub.1, n.sub.2 and n.sub.3 is 1, 2 or 3 and Q is selected from O, S, NH, C(.dbd.O) or --CR.sub.1R.sub.2--, where R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen or optionally substituted C.sub.1-7 alkyl, or may together with the carbon atom to which they are attached form a C.sub.3-7 cyclic alkyl group, which may be saturated (a C.sub.3-7 cycloalkyl group) or unsaturated (a C.sub.3-7 cycloalkenyl group), or one of R.sub.1 and R.sub.2 may be attached to an atom in R.sub.L to form an unsaturated C.sub.3-7 cycloalkenyl group which comprises the carbon atoms to which R.sub.1 and R.sub.2 are attached in Q, --(CH.sub.2).sub.n3-- (if present) and part of R.sub.L; and R.sub.L is optionally substituted C.sub.5-20 aryl; and R.sub.N is selected from hydrogen, optionally substituted C.sub.1-7 alkyl, C.sub.3-20 heterocyclyl, and C.sub.5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone. |
| Inventor(s): | Martin; Niall Morrison Barr (Cambridge, GB), Smith; Graeme Cameron Murray (Cambridge, GB), White; Charles Richard (Carlisle, GB), Newton; Roger Frank (Cornwall, GB), Douglas; Diane Gillian (Cornwall, GB), Eversley; Penny Jane (Cornwall, GB), Vile; Julia (Cornwall, GB) |
| Assignee: | Kudos Pharmaceuticals Limited (Cambridge, GB) Maybridge PLC (Cornwall, GB) |
| Application Number: | 10/021,506 |
| Patent Claims: |
1. A compound of formula: ##STR00029## or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent optionally
monosubstituted, fused benzene; R.sub.C is --CH.sub.2--R.sub.L; R.sub.L is substituted phenyl, wherein the substituents are selected from the group consisting of: C.sub.3-20 heterocyclyl; ester; amido; acyloxy; sulfonamido; ureido; and optionally
further substituted; and R.sub.N is hydrogen.
2. A compound according to claim 1, wherein the fused benzene is unsubstituted. 3. A compound according to claim 1, wherein R.sub.L is substituted by a ureido group, or a sulfonamido group. 4. A pharmaceutical composition comprising a compound of formula: ##STR00030## or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused benzene; R.sub.C is --CH.sub.2--R.sub.L; R.sub.L is optionally substituted phenyl; and R.sub.N 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 R.sub.L is substituted by one or more substituents selected from the group consisting of: C.sub.1-7 alkyl; C.sub.5-20 aryl; C.sub.3-20 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 R.sub.L is substituted by a ureido group, or a sulfonamido group. 8. A compound of the formula: ##STR00031## or an isomer, salt, solvate, chemically protected form and prodrug thereof. |
