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US 2012/0258993 A1Published application
Non-natural macrocyclic amide hdac6 inhibitor compounds and their uses as therapeutic agents
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsGiuseppe Giannini, Walter Cabri, Stephan Hanessian, Luciana Auzzas, Andreas Larsson
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Abstract
The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.
Claims14
A compound having the general formula I
- wherein,
- X is CONH or NHCO;
- Y is O, NH, NHCO or CONH;
- Z is CONHOH, SH, SAc, COCH3 or CO2H;
- Ar is C6-aryl or C5-C10-heteroaryl, wherein said aryl or heteroaryl can be optionally substituted with 1 to 4 groups chosen from the group consisting of C1-C3-alkyl, hydroxyl, alkoxy, amino or alkylamino;
- R1 is H, CONHR2, NHR2, amino-(C1-C2)-alkyl or (C1-C2)-alkyl-amino-(C1-C2)-alkyl;
- R2 is H or C1-C3-alkyl;
- m is an integer comprised between 4 and 6;
- n is an integer comprised between 0 and 1;
- their tautomers, their geometrical isomers, their optically active forms such as enantiomers, diastereomers and their racemate forms, as well as their pharmaceutically acceptable salts thereof.
7 more elements
(canceled)
Dependencies are inferred from the claim text.