| 摘要 |
N, 3-Disubstituted azepane or azepan-2-one derivatives (I) are new. Azepane derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. W = CO or CH2; X = alkylene, CO, S(O)n, S(O)n-A1, CO-A1, A1-S(O)n-A1 or A1-CO-A1 (bonded to the ring at the left-hand terminal); or X may also be a direct bond if W = CH2; A1 = alkylene; n = 0-2; Y = aryl, heteroaryl, cycloalkyl or heterocycloalkyl (all optionally substituted (os) by R8); R1 - R4 = H or as for Y; or pairs of adjacent groups R1 - R4 may together form bonds; T = CHR5, NR5 or NR5CO (bonded to the ring at the left-hand terminal); R5 = H; or alkyl, aryl, heteroaryl, aralkyl or heteroaralkyl (all os by one or more R7); V = H; or aryl or heteroaryl (both os by one or more R7); A2 = -(CR6R'6)p; p = 0-4 (but not 0 if T = NR5); R6, R'6 = H, alkyl (os by R9), alkenyl, alkynyl or R9; R9 = OR5, NR5R'5, S(O)nR5, CONR5R'5, NR5COR'5, NR5SO2R'5, SO2NR5R'5 or NR5COOR'5; R'5 = as R5; R7 = halo, alkyl, alkoxy, OH, SH, alkylthio, CN, NH2 (os by 1 or 2 alkyl), NO2, COOH, alkoxycarbonyl, CONH2 (os by 1 or 2 alkyl), carbamoyl, os aryl, os aralkyl, os heteroaryl, os heteroaralkyl, os cycloalkyl, os cycloalkylalkyl, os heterocycloalkyl or os heterocycloalkylalkyl; R8 = halo, =O, OH, CN, NO2, COOH, alkoxycarbonyl, U-R80 or A80-U-R80; A80 = alkylene;and U = direct bond, O, NH, S(O)n, NHCO, CONH, SO2NH or NHSO2; R80 = alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl; alkyl or alkylene moieties have 1-6C; cycloalkyl moieties have 3-8C; heterocycloalkyl moieties are 5-7 membered and contain 1-3 of N, O and S as heteroatom(s); aryl moieties are phenyl or naphthyl; heteroaryl moieties are mono- or bicyclic 5-11 membered systems containing at least one aromatic ring and 1-5 of N, O and S as heteroatom(s); the substituents in os aryl, heteroaryl, aralkyl or heteroaralkyl are one or more of CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part); and the substituents in os cycloalkyl, heterocycloalkyl, cycloalkylalkyl or heterocycloalkylalkyl are one or more of =O, CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part). An Independent claim is included for the preparation of (I).
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