| 摘要 |
Dihydroindolone derivatives (I) and their optical and geometric isomers, or addition salts with an acid or base are new. Dihydroindolone derivatives of formula (I) and their optical and geometric isomers, or addition salts with an acid or base are new. m : 1 or 2; n : 1 or 2; A : a pyrrolyl group optionally substituted by 1-3 groups of 1-6C alkyl; X : C(O), S(O) or SO 2; either R 1>, R 2> : 1-6C alkyl; or NR 1>R 2> : a heterocyclic group; R 3>R 4> : a heterocyclic group; R 5> : H or 1-6C alkyl; and R 6> : H or halo, where the heterocyclic group is a mono or bicyclic 5-8 membered group (optionally containing one to three heteroatoms of N, O or S, and one or more unsaturations, and optionally substituted by one or more 1-6C alkyl, 1-6C alkenyl, oxo, hydroxy, 1-6C alkoxy, aryl, arylalkyl or arylalkenyl), the aryl is phenyl group optionally substituted by one or more halo or 1-6C alkyl, and X represents the double bond, which is in configuration is Z or E. Independent claims are included for: (1) the preparations of (I); and (2) combination comprising (I) with an anticancer agent comprising genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors or kinase inhibitors. [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : None given.. |
