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US 2010/0063144 A1Published application
Compounds and uses thereof
AssigneeImperial Innovations Limited
InventorsEric Ofori Aboagye, David Michael Vigushin, Wendy Vigushin
Life of this patent
Estimating the term…
Abstract
There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.
Claims37
A compound of formula I,
- wherein
- R1a represents C1-4 alkyl (which latter group is optionally substituted by one or more substituents selected from halogeno and aryl), aryl, (CH2)2-L1 or the structural fragment
- wherein Rx represents H or N(R1b)R2b;
- R1b and R2b independently represent C1-4 alkyl (which latter group is optionally substituted by one or more substituents selected from halogeno and aryl), aryl or (CH2)2-L2;
- Ry represents halogeno or C1-4 alkyl;
- R2a represents H, C1-4 alkyl (which latter group is optionally substituted by one or more substituents selected from halogeno and aryl), aryl or (CH2)2-L3;
- L1, L2 and L3 each represents, independently at each occurrence, a leaving group;
- R3 represents halogeno or C1-4 alkyl;
- a represents, independently at each occurrence, an integer from 0 to 4;
- X1—X2 represents C(O)—CH(Y1), C(H)═C(Y1), CH2—CH(Y1), NH—CH(Y1), CH2—C(O), NH—C(O) or CH(Y1);
- b represents 0 or 1;
- X3—X4 represents CH═C(Y2), O—CH(Y2), NH—CH(Y2), O—C(O) or NH—C(O);
- c represents an integer from 0 to 10;
- X5—X6 represents CH2—CH2, CH═CH or O—CH2;
- and
- Y1 and Y2 independently represent, at each occurrence, H or C1-4 alkyl;
- or a pharmaceutically acceptable derivative thereof,
- provided that at least one of the following is the case:
- (a) R1a represents (CH2)2-L1;
- (b) R1b and/or R2b represents (CH2)2-L2;
- (c) R2 represents (CH2)2-L3.
18 more elements
A compound of formula I,
- wherein
- R1a represents C1-4 alkyl (which latter group is optionally substituted by one or more substituents selected from halogeno and aryl), aryl or (CH2)2-L1;
- R2a represents H, C1-4 alkyl (which latter group is optionally substituted by one or more substituents selected from halogeno and aryl), aryl or (CH2)2-L3;
- L1, L2 and L3 each represents, independently at each occurrence, a leaving group;
- R3 represents halogeno or C1-4 alkyl;
- a represents, independently at each occurrence, an integer from 0 to 4;
- X1—X2 represents C(O)—CH(Y1), C(H)═C(Y1), CH2—CH(Y1), NH—CH(Y1), CH2—C(O), NH—C(O) or CH(Y1);
- b represents 0 or 1;
- X3—X4 represents CH═C(Y2), O—CH(Y2), NH—CH(Y2), O—C(O) or NH—C(O);
- c represents an integer from 0 to 10;
- Z represents —SO2.NH— or —NH.SO2—;
- d represents 0 or 1;
- X5—X6 represents CH2—CH2, CH═CH or O—CH2;
- and
- Y1 and Y2 independently represent, at each occurrence, H or C1-4 alkyl;
- or a pharmaceutically acceptable derivative thereof,
- provided that at least one of the following is the case:
- (a) R1a represents (CH2)2-L1;
- (c) R2a represents (CH2)2-L3.
16 more elements
(canceled)
A compound of formula:
Dependencies are inferred from the claim text.