New 1-(4-amino-benzyl)-pyrrolidine propionic acid derivatives

摘要

Pyrrolidine derivatives of formula (I), and their salts are new: R1 = OH, 1-10C alkoxy, 3-10C alkenyloxy, 1-3C alkyl-(6-10C)aryloxy or NR6R7; R2 = 1-10C alkyl, 2-10C alkenyl, 3-10C alkynyl or (CH2)m-B-(CH2)nR5 (all optionally substituted by a COR1 group, or optionally substituted by one or more halo); (6-10C)aryl-(1-3C)alkyl or (6-10C)-aryl (both optionally ring substituted by 1-2 halo, 1-4C alkoxy, NO2 or CN); or 3-8C cycloalkyl, (4-10C)cycloalkyl-(1-4C)alkyl, (5-10C)cycloalkyl-(2-4C)alkenyl or (5-10C)cycloalkyl-(2-4C)alkynyl; R3 = H, 1-8C alkyl, 3-8C cycloalkyl, (6-10C)aryl-(1-3C)alkyl, 2-6C alkenyl or 3-6C alkynyl; or R2 + R3 = 2-4C alkylene, optionally substituted by halo; R4 = H, 1-6C alkyl, (6-10C)aryl-(1-3C)alkyl, 3-10C alkenyl, COO-(1-6C)alkyl, COO-(1-6C)alkyl-(6-10C)aryl or C(=NH)NH2; R5 = H, or a group of formula (i): R6, R7 = H, 1-10C alkyl, (6-10C)aryl-(1-3C)alkyl, 1-10C alkylamino or 1-10C alkylguanidino; R8 = 6-10C aryl or (6-10C)aryl-(1-3C)alkyl (both optionally substituted by one or more COR1, halo, NO2, CN, 1-4C alkoxy or amino); or 1-6C alkyl, 3-8C cycloalkyl or (2-6C)alkenyl; R9 = NH(CH2)oNHR4, O(CH2)oNH2 or O(CH2)oNH-C(=NH)NH2; A = a single or double bond; B = O, NR3 or S; Y = a direct bond, or an amino acid; m = 1-5; n = 1-5; o = 1-10.