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Generated: January 19, 2018

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Claims for Patent: 7,981,889

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Summary for Patent: 7,981,889
Title:Phthalazinone derivatives
Abstract: Compounds of the formula (I): ##STR00001## wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NR.sup.X or CR.sup.XR.sup.Y; if X.dbd.NR.sup.X then n is 1 or 2 and if X.dbd.CR.sup.XR.sup.Y then n is 1; R.sup.X is selected from the group consisting of H, optionally substituted C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; R.sup.Y is selected from H, hydroxy, amino; or R.sup.X and R.sup.Y may together form a spiro-C.sub.3-7 cycloalkyl or heterocyclyl group; R.sup.C1 and R.sup.C2 are both hydrogen, or when X is CR.sup.XR.sup.Y, R.sup.C1, R.sup.C2, R.sup.X and R.sup.Y, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R.sup.1 is selected from H and halo.
Inventor(s): Barr Martin; Niall Morrison (Cambridge, GB), Smith; Graeme Cameron (Cambridge, GB), Jackson; Stephen Philip (Cambridge, GB), Loh; Vincent Junior M (Horsham, GB), Cockcroft; Xiao-Ling Fan (Horsham, GB), Williams Matthews; Ian Timothy (Horsham, GB), Menear; Keith Allan (Horsham, GB), Kerrigan; Frank (Cornwall, GB), Ashworth; Alan (London, GB)
Assignee: Kudos Pharmaceuticals Limited (Cambridge, GB) Maybridge Limited (Cornwall, GB)
Application Number:12/109,260
Patent Claims: 1. A compound of the formula (Ib): ##STR00440## or an isomer or salt thereof, or a mixture of any thereof, wherein: A and B together represent a fused aromatic ring, optionally substituted with one or more substituent groups selected from halo, nitro, hydroxyl, ether, thiol, thioether, amino, C.sub.1-7 alkyl, C.sub.3-20 heterocyclyl and C.sub.5-20 aryl; R.sup.x is selected from H, C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups, wherein the acyl, C.sub.1-20 alkyl, C.sub.5-20 aryl or C.sub.3-20 heterocyclyl group is optionally substituted with one or more substituent groups selected from C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, halo, hydroxyl, ether, nitro, cyano, acyl, carboxy, ester, amido, amino, acylamido, ureido, acyloxy, thiol, thioether, sulfoxide, sulfonyl, thioamido and sulfonamido; R.sup.C1 and R.sup.C2 are both hydrogen; and R.sup.1 is selected from H and halo.

2. The compound, or isomer or salt, or mixture thereof according to claim 1, wherein the fused aromatic ring represented by A and B together is benzene.

3. The compound, or isomer or salt, or mixture thereof according to claim 1, wherein R.sup.1 is selected from H, Cl, and F.

4. The compound, or isomer or salt, or mixture thereof according to claim 1, wherein R.sup.x is selected from H, C.sub.1-20 alkyl, C.sub.5-20 aryl, acyl, sulfonyl, amido, and thioamido groups, wherein the acyl, C.sub.1-20 alkyl or C.sub.5-20 aryl group is optionally substituted with one or more substituent groups selected from C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, halo, hydroxyl, ether, nitro, cyano, acyl, carboxy, ester, amido, amino, acylamido, ureido, acyloxy, thiol, thioether, sulfoxide, sulfonyl, thioamido and sulfonamido.

5. The compound, or isomer or salt, or mixture thereof according to claim 1, which is of formula (II): ##STR00441## wherein: R.sup.C3 is selected from C.sub.1-7 alkyl, C.sub.5-20 aryl, and C.sub.3-20 heterocyclyl, wherein the C.sub.1-7 alkyl, C.sub.5-20 aryl or C.sub.3-20 heterocyclyl group is optionally substituted with one or more substituent groups selected from C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, halo, hydroxyl, ether, nitro, cyano, acyl, carboxy, ester, amido, amino, acylamido, ureido, acyloxy, thiol, thioether, sulfoxide, sulfonyl, thioamido and sulfonamido.

6. The compound, or isomer or salt, or mixture thereof according to claim 1, which is of formula (III): ##STR00442## wherein R is selected from: ##STR00443##

7. A composition comprising two or more entities chosen from a compound of formula (IV), ##STR00444## and salts of a compound of formula (IV).

8. A pharmaceutical composition comprising a compound of formula (Ib): ##STR00445## or an isomer or salt thereof, or a mixture thereof, wherein: A and B together represent a fused aromatic ring, optionally substituted with one or more substituent groups selected from halo, nitro, hydroxyl, ether, thiol, thioether, amino, C.sub.1-7 alkyl, C.sub.3-20 heterocyclyl and C.sub.5-20 aryl; R.sup.x is selected from H, C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups, wherein the acyl, C.sub.1-20 alkyl, C.sub.5-20 aryl or C.sub.3-20 heterocyclyl group is optionally substituted with one or more substituent groups selected from C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, halo, hydroxyl, ether, nitro, cyano, acyl, carboxy, ester, amido, amino, acylamido, ureido, acyloxy, thiol, thioether, sulfoxide, sulfonyl, thioamido and sulfonamido; R.sup.C1 and R.sup.C2 are both hydrogen; and R.sup.1 is selected from H and halo; and one or more pharmaceutically acceptable entities chosen from carriers, excipients, buffers, adjuvants, and stabilizers.

9. The pharmaceutical composition of claim 8, wherein the compound is of formula (II): ##STR00446## or an isomer or salt, or mixture thereof, wherein: R.sup.C3 is selected from C.sub.1-7 alkyl, C.sub.5-20 aryl, and C.sub.3-20 heterocyclyl, wherein the C.sub.1-7 alkyl, C.sub.5-20 aryl or C.sub.3-20 heterocyclyl group is optionally substituted with one or more substituent groups selected from C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, halo, hydroxyl, ether, nitro, cyano, acyl, carboxy, ester, amido, amino, acylamido, ureido, acyloxy, thiol, thioether, sulfoxide, sulfonyl, thioamido and sulfonamido.

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