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US 2006/0235012 A1Published application
Carboline and betacarboline derivatives for use as hdac enzyme inhibitors
AssigneeChroma Therapeutics Ltd.
InventorsAlan Davidson, Christopher Yarnold, Charlton Hugh
Life of this patent
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Abstract
Compounds of formula (IA) and (IB) are inhibitors of histone deacetylase activity and useful for the treatment of, inter alia, cancers: wherein fused rings A1 and A2 are optionally substituted; linker radical R1 represents a radical of formula
Claims28
A compound of formula (IA) or (1B), or a salt, hydrate or solvate thereof
- wherein fused rings A1 and A2 are optionally substituted;
- R1 represents a radical of formula -(Alk1)n-(X)m-(Alk2)p-Z wherein
- Z represents a radical of formula —C(═O)NH(OH), or —N(OH)C(═O)Y wherein Y represents hydrogen, C1-C6 alkyl, a phenyl or cycloalkyl ring, or a monocyclic heterocyclic radical having 5 or 6 ring atoms;
- Alk1 represents an optionally substituted, straight or branched, C1-C6 alkylene radical,
- Alk2 represents an optionally substituted, straight or branched, C1-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene radical which may optionally contain an ether (—O—), thioether (—S—) or amino (—NRA—) link wherein RA is hydrogen or C1-C3 alkyl;
- X represents an optionally substituted phenyl or 5- or 6-membered heteroaryl ring;
- and
- n, m and p are independently 0 or 1, provided that at least one of n, m and p is 1 and the length of radical -(Alk1)n-(X)m-(Alk2)p- is equivalent to that of a hydrocarbon chain of from 2-10 carbon atoms;
- R12 is hydrogen and R2 is (a) an optional substituent or (b) a radical of formula -(Alk3)r-Q wherein r is 0 or 1, Alk3 represents an optionally substituted, straight or branched, C1-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene radical and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic group;
- or R12 and R2 taken together with the carbon atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring;
- R13 is hydrogen and R3 is (i) an optional substituent or (ii) a radical of formula -(Alk3)r-Q wherein r is 0 or 1, Alk3 represents an optionally substituted, straight or branched, C1-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene radical and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic group;
- or R13 and R3 taken together with the carbon atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring;
- and
- R4 is hydrogen or C1-C6 alkyl.
11 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.