4-H-SUBSTITUTED CHROME AND ANALAGOS AS CASPASE ACTIVATORS AND INDUCTORS OF APOPTOSIS AND USE AS ANTICANCERIGEN AGENTS.

摘要

Use of a compound selected from the group consisting of: 2-Amino-3-cyano-7-ethylamino-4- (3-bromophenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3-chlorophenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3-nitrophenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3,4,5-trimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3,5-dimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3-methoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7-ethylamino-4- (3-cyanophenyl) -4H-chromene; 2-Amino-3-cyano-7-methoxy-4- (3-pyridyl) -4H-chromene; 2-Amino-3-cyano-4- (3-pyridyl) -4H-indole [4,5-b] pyran; 2,7-Diamino-3-cyano-4- (3-bromophenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3-cyanophenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3-methoxyphenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3-chlorophenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3-methylphenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3-pyridyl) -4H-chromene; 2-Amino-3-cyano-7-methoxy-4- (2,4-dimethoxypyrimidinyl) -4H-chromene; 2-Amino-3-cyano-7-methoxy-4- (1,2,3,6-tetrahydrophenyl) -4H-chromene; 2-Amino-3-cyano-4- (5-bromo-3-pyridyl) -7-ethylamino-4H-chromene; 2,7-Diamino-3-cyano-4- (5-methyl-3-pyridyl) -4H-chromene; 2-Amino-3-cyano-4- (5-methyl-3-pyridyl) -4H-indole [4,5-b] pyran; 2-Amino-3-cyano-4- (5-bromo-3-pyridyl) -4H-indole [4,5-b] pyran; 2,7-Diamino-3-cyano-4- (5-bromo-3-pyridyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (5-methoxy-3-pyridyl) -4H-chromene; 2-Amino-3-cyano-4- (5-methoxy-3-pyridyl) -4H-indole [4,5-b] pyran; 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4H-indole [7,6-b] pyran; 2-Amino-3-cyano-4- (3-methoxyphenyl) -4H-indole [7,6-b] pyran; 3-Cyano-2,7,8-triamino-4- (3-methoxyphenyl) -4H-chromene; 3-Cyano-2,7,8-triamino-4- (3-bromo-4,5-dimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-4- (3-methoxyphenyl) -4H-indole [4,5-b] pyran; 2-Amino-3-cyano-4- (3,5-dimethoxyphenyl) -4H-indole [7,6-b] pyran; 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4H-imidazo [4,5-h] chromene; 2-Amino-3-cyano-4- (3,4,5-trimethoxyphenyl) -4H-indole [7,6-b] pyran; 2-Amino-3-cyano-7,8-methylenedioxy-4- (3-bromo-4,5-dimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7,8-methylenedioxy-4- (3-methoxyphenyl) -4H-chromene; 2-Amino-3-cyano-4- (3-methoxyphenyl) -4H-imidazo [4,5-h] chromene; 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4H-furo [2,3-h] chromene; 2-Amino-3-cyano-4- (3-methoxyphenyl) -4H-furo [2,3-h] chromene; 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4H-thieno [2,3-h] chromene; 2-Amino-3-cyano-4- (3-methoxyphenyl) -4H-pyrazo [2,3-h] chromene; 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4 H -pyrazo [2,3-h] chromene; 2,7-Diamino-3-cyano-4- (3-iodophenyl) -4H-chromene; 2,7-Diamino-3-cyano-4- (3,4,5-trimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7-hydroxy-4- (3,4,5-trimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7- (2-methylbutanoylamino) -4- (3-bromo-4,5-dimethoxyphenyl) -4H-chromene; 2-Amino-3-cyano-7-dimethylamino-4- (3- (2-phenylbutanoyloxy) phenyl) -4H-chromene; 2-Amino-3-cyano-7-dimethylamino-4- (3- (2-methylbutanoyloxy) phenyl) -4H-chromene; and 2-Amino-3-cyano-4- (3-bromo-4,5-dimethoxyphenyl) -4H-chromene; or one of its pharmaceutically acceptable salts or prodrugs, to prepare a medicament for the treatment of a disorder sensitive to the induction of apoptosis in an animal suffering from it; wherein said prodrug is: a) an ester of a hydroxy-containing compound obtained by condensation with a C1-4 carboxylic acid, C3-6 dioic acid or anhydride thereof; b) an imine of an amino-containing compound, obtained by condensation of an aldehyde or C1-4 ketone; c) a carbamate of an amino-containing compound; d) an acetal or ketal of an alcohol-containing compound, obtained by condensation with a chloromethyl and methyl ether or chloromethyl and ethyl ether; or e) a phosphonate or phosphono compound obtained by condensation with a phosphate ester, phosphoryl chloride or phosphoric acid.