| 摘要 |
Substituted cyclohexylmethyl-amine derivatives (I), optionally as racemates, pure or mixed stereoisomers (especially enantiomers and diastereomers), salts with acids or bases and/or solvates, especially hydrates. - Substituted cyclohexylmethyl-amine derivatives of formula (I), optionally as racemates, pure or mixed stereoisomers (especially enantiomers and diastereomers), salts with acids or bases and/or solvates, especially hydrates are new - A = hydrogen or (hetero)aryl, optionally substituted one or more times; - R1 = 1-10C alkyl or 3-10C cycloalkyl, optionally unsaturated, linear or branched and substituted one or more times; (hetero)aryl, or (hetero)aryl or 3-10C cycloalkyl connected through 1-3C alkyl (optionally unsaturated), 1-3C alkylene or ethynyl, all optionally substituted one or more times by fluoro, chloro, bromo, iodo, OR18, SR18, SO2R18, SO2OR18, cyano, COOR18, NR19R20, 1-10C alkyl, 3-10C cycloalkyl or silyl (optionally substituted one or more times), (hetero)aryl (optionally substituted one or more times), or (hetero)aryl or 3-10C cycloalkyl, connected through 1-3C alkyl (optionally unsaturated) or 1-3C alkylene; - R18, R19 and R20 = hydrogen, 1-10C alkyl or 3-10C cycloalkyl, optionally unsaturated, linear or branched and substituted one or more times; (hetero)aryl, or (hetero)aryl or 3-10C cycloalkyl connected through 1-3C alkyl (optionally unsaturated) or 1-3C alkylene, or R19 and R20 are together CH2CH2(O or R21)CH2CH2, or (CH2)z; - z = 3-6; - R21 = hydrogen, optionally substituted phenyl or 1-10C alkyl, saturated or unsaturated, linear or branched, optionally substituted one or more times; - R2 and R3 = as defined for R18, or together form a ring as for R19 and R20; - X completes one of the partial structures B = hydroxy, OR7, hydrogen, fluoro, chloro or NR8R9; R7 = R18 but not hydrogen; R8 and R9 are as R18 or together form a ring as R19 and R20; Z-Y = any of five specified groups; some compounds are excluded by provisos - . The full definitions are given in the DEFINITIONS (Full Definitions) Field. - ACTIVITY - Analgesic. No details of tests for analgesic activity are given. - MECHANISM OF ACTION - None given in the source material. |
