Multifluoro-substituted chalcones and analogs as activators of caspases and inducers of apoptosis and the use thereof
AssigneeCytovia, Inc.
InventorsSui Xiong Cai, P. Sanjeeva Reddy, John A. Drewe, Bao Ngoc Nguyen, Shailaja Kasibhatla
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Abstract
The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis 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.
Claims8
A compound of Formula I:
- or pharmaceutically acceptable salts or prodrugs thereof, wherein:
- Ar is optionally substituted aryl or optionally substituted heteroaryl;
- R6-R8 are independently hydrogen, halo, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, nitro, amino, cyano, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, aryloxy, arylalkoxy, haloalkoxy, carboxy, carbonylamido or alkylthiol;
- and
- R9 and R10 are independently hydrogen, alkyl or cycloalkyl;
- with the proviso that when Ar is 4-trifluoromethylphenyl, then
- (a) at least one of R6-R8 are other than hydrogen;
- or
- (b) Ar is further substituted with at least one group other than hydrogen;
- or
- (c) at least one of R9 and R10 is other than hydrogen.
A compound of Formula II:
- or pharmaceutically acceptable salts or prodrugs thereof, wherein:
- R1-R8 are independently hydrogen, halo, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, nitro, amino, cyano, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, aryloxy, arylalkoxy, haloalkoxy, carboxy, carbonylamido or alkyithiol, each of which is optionally substituted;
- provided that when R3 is CF3, then at least one of R1-R2 and R4-R8 is other than hydrogen.
Dependencies are inferred from the claim text.