| 摘要 |
1-Carboxyalkyl-4-(hetero)aryl-piperazine derivatives (I) are new. 1-Carboxyalkyl-4-(hetero)aryl-piperazine derivatives of formula (I) and their isomers and salts are new. n = 3-5; RA = (i) phenyl substituted by R1 and R2; (ii) heteroaryl or monocyclic heteroaryl or phenyl, both substituted by phenyl or monocyclic heteroaryl, where phenyl moieties are optionally substituted (os) by F, Cl or Br and phenyl or heteroaryl moieties are os by T', OH, OT, COOH, COOT, CONH2, CONHT or CONT2; R1 = H, F, Cl, Br, T', OH, 1-4C alkoxy, phenyl-(1-3C) alkoxy, COOH, COOT, CONH2, CONHT, CONT2, NO2, NH2, NHT, NT2, phenyl-(1-3C) alkylamino, N-(T)-phenyl-(1-3C) alkylamino, NHCOT, NTCOT, NHSO2T or NTSO2T; R2 = H, F, Cl, Br or T; or R1 + R2 = OCH2O; T = 1-3C alkyl; T' = T (os by one or more F); RB = H or T; RC = (i) H; (ii) 1-10C alkyl, 3-7C cycloalkyl or (3-7C) cycloalkyl-(1-3C) alkyl (all os by one or more F); or (iii) phenyl, naphthyl or heteroaryl (all os by F, Cl, Br, T', OH, OT, COOH, COOT, CONH2, CONHT, CONT2, Q, NO2, NH2, NHT, NT2, NHCOT, NTCOT, NHSO2T or NTSO2T); RD = as for RC (iii); Q = 3-7 membered cycloalkyleneimino; or 6- or 7-membered cycloalkyleneimino in which the CH2 in the 4-position is replaced by O, S, SO, SO2, NH or NT; RE = COOH; (1-6C) alkoxycarbonyl or (3-7C) cycloalkoxycarbonyl, where the C-atom linked to O in the alkoxy moiety is primary or secondary and the alkyl or cycloalkyl moiety is os (but not in the 1-position relative to O) by OT, NH2, NHT or NT2; or phenyl-(1-3C) alkoxycarbonyl or heteroaryl-(1-3C) alkoxycarbonyl; heteroaryl moieties = 6-membered heteroaryl containing 1-3 N; or 5-membered heteroaryl containing (a) one NH, NT, O or S, (b) one NH or NT plus one O or S or (c) 1 or 2 N. An Independent claim is included for the preparation of (I).
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