Quinoxaline derivatives and their use to treat benign and malignant tumor disorders.

摘要

Quinoxaline compounds (I) and their salts, hydrates, solvates, racemates, enantiomers and/or diastereomers, or in the form of mixtures of the enantiomers and/or diastereomers, in the form of the tautomers and their polymorphic forms are new. Quinoxaline compounds of formula (I) and their salts, hydrates, solvates, racemates, enantiomers and/or diastereomers, or in the form of mixtures of the enantiomers and/or diastereomers, in the form of the tautomers and their polymorphic forms are new. X : O or S; R 1 : H, 1-12C alkyl (optionally substituted), CN or halo; R 2, R 3 : H or 1-12C alkyl (optionally substituted); R 4 : 1-12C alkyl, cycloalkyl, heterocyclyl, (hetero)aryl, alkylaryl or alkylheteroaryl (all optionally substituted) or H; and R 5-R 8 : 1-12C alkyl or (hetero)aryl (all optionally substituted), H, halo, CN, OH, 1-12C alkoxy, amino, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonylamino or alkoxycarbonylaminoalkyl, where the substituents are F, Cl, Br, I, CN, CF 3, NH 2, NH-alkyl, NH-aryl, N(alkyl) 2, NH-CO-alkyl, NH-CO-aryl, NH-CO-heteroaryl, NH-SO 2-alkyl, NH-SO 2-aryl, NH-SO 2-heteroaryl, NH-CO-NH-alkyl, NH-CO-NH-aryl, NH-CO-NH-heteroaryl, NH-C(O)O-alkyl, NH-C(O)O-aryl, NH-C(O)O-heteroaryl, NO 2, SH, S-alkyl, OH, OCF 3, O-alkyl, O-aryl, O-CO-alkyl, O-CO-aryl, O-CO-heteroaryl, OC(O)O-alkyl, O-C(O)O-aryl, O-C(O)O-heteroaryl, O-CO-NH-alkyl, O-CO-N(alkyl) 2, OCO-NH-aryl, O-CO-NH-heteroaryl, OSO 3H, OSO 2-alkyl, OSO 2-aryl, OSO 2-heteroaryl, OP(O)(OH) 2, alkyl-P(O)(OH) 2CHO, CO 2H, C(O)O-alkyl, C(O)O-aryl, C(O)O-heteroaryl, CO-alkyl, CO-aryl, CO-heteroaryl, SO 3H, SO 2-NH 2, SO 2-NH-alkyl, SO 2-NH-aryl, SO 2-NH-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, where the radicals alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl (all optionally substituted). With the proviso that at least one of the substituents R 5-R 8is optionally substituted (hetero)aryl radical. An independent claim is included for a composition comprising (I). [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.