Substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs as activators of caspases and inducers of apoptosis and the use thereof
AssigneeCytovia, Inc.
InventorsSui Xiong Cai, John A. Drewe, Han-Zhong Zhang
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Abstract
The present invention is directed to substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs thereof, represented by the general Formula I: wherein X, Ar1, R2-R6 and R12 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Claims13
A method of treating a disorder selected from the group consisting of Hashimoto's thyroiditis, autoimmune lymphoproliferative syndrome, rheumatoid arthritis, inflammation, inflammatory bowel disease, Crohn's disease, ulcerative colitis, and a skin disease in an animal suffering therefrom, comprising administering to an animal in need of such treatment an effective amount of a compound of Formula I:
- or a pharmaceutically acceptable salt or prodrug thereof, wherein:
- X is N—R1;
- R1 is hydrogen or optionally substituted alkyl;
- R2-R6 are independently hydrogen, halo, nitro or cyano;
- or haloalkyl, aryl, fused aryl, carbocylic, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, carbocycloalkyl, hydroxyalkyl, amino, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, aryloxy, arylalkoxy, haloalkoxy, carboxy, carbonylamido or alkylthiol, each of which is optionally substituted;
- R12 is hydrogen or optionally substituted alkyl;
- and
- Ar1 is optionally substituted and is aryl.
Dependencies are inferred from the claim text.