| 摘要 |
Piperazinyl cyclohexanecarboxamide derivatives (I) are new. Compounds of formula (I) and their salts, hydrates and solvates are new: R1 = COR4, (CH2)aR4, SO2R4, CONR5R6 or COOR7; a = 0-3; R4 = A; 3-8C cycloalkyl optionally substituted with A or OH; 6-10C aryl or Het(5-10,1-3) optionally substituted with 1-3 of halo, CF3, OCF3, CN, COOH, NO2, OH, SO2NH2, OA, COOA, NH2, NHA, NAA, 2-5C alkanoylamino, 3-8C cycloalkyl, 6-10C aryl, Het(5-6,1-3) and Het'(5-7,1-3) where N is substituted with H, 1-4C alkyl or 3-7C cycloalkyl; or 1-6C alkyl optionally interrupted by O, S or NH and optionally substituted with OH, NHA, NAA, Ph or Het'(5-7,1-2) where N is substituted with H, 1-4C alkyl or 3-7C cycloalkyl; A = 1-6C alkyl; Het(x,y) = heteroaryl with x ring members and y heteroatoms selected from N, O and S; Het'(x,y) = heterocyclyl with x ring members and y heteroatoms selected from N, O and S; R5, R6 = H; 6-10C aryl or Het(5-10,1-3) optionally substituted with halo, CF3, OCF3, CN, NO2, OH, NH2, A or OA; adamantyl; 1-8C alkyl optionally interrupted by 1-3 O atoms and optionally substituted with 1-3 of OH, Ph, CF3, 3-8C cycloalkyl, OA, NHA, NAA, Het'(5-6,1-3) or Het(5-10,1-3); 3-8C cycloalkyl optionally substituted with 1-3 of 1-4C alkyl, OH or oxo; or Het'(5-6,1-3) where N is substituted with H or 1-4C alkyl; or NR5R6 = saturated Het'(4-7,2-3) optionally substituted with OH, oxo, A or 1-6C hydroxyalkyl; R7 = 6-10C aryl or Het(5-10,1-3) optionally substituted with halo, CF3, OCF3, CN, NO2, OH, NH2, A or OA; adamantyl; 1-8C alkyl optionally interrupted by 1-3 O atoms and optionally substituted with 1-3 of OH, Ph, CF3, 3-8C cycloalkyl, OA, NHA, NAA, Het'(5-6,1-3) or Het(5-10,1-3); 3-8C cycloalkyl optionally substituted with 1-3 of 1-4C alkyl, OH or oxo; or Het'(5-6,1-3) where N is substituted with H or 1-4C alkyl; R2 = 1-8C alkyl optionally interrupted by S, O, SO or SO2; or phenyl, benzyl or Het(5-6,1-2) optionally substituted with 1-3 of halo, CF3, OCF3, CN, NO2, OH, NH2, A or OA; R3 = CH2OH or CONR8R9; R8, R9 = H or A; alternatively, CHR2R3 is 2-hydroxy-1-indanyl. Independent claims are also included for: (1) a process for preparing compounds (I); and (2) a medicament comprising at least one compound (I) and at least one excipient or other active ingredient.
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