| 摘要 |
(1) N-Aryl-pyrrolidine, -piperidine and -homopiperidine derivs. of formula (I) and their acid-addn. and quat. salts and their hydrates and alcoholates are new. p = 0, 1 or 2; A = H, OR1, CN, CONR1R2, COR1, COOR1, OCOR1, CH2OR1 or CH2NR1R2; m = 0-6; Q = CH, CH2 or CH(OH); d, n = 0 or 1 and the dotted lines are opt. double bonds; Ar = X,Y,ZC6H2, pyridyl, thienyl, furyl or naphthyl; R = Ar gp., X,Y,ZC6H2CH2, cycloalkyl or 1-8C alkyl; D = Ar gp., quinolyl, Ar(CH2)5 or a gp. of formulae (II)-(IV). In (III) when X = H, bond a may be a single bond; s = 1-4; t = 0, 1 or 2; X,Y,Z = H, 1-8C alkyl, halogen, NO2, OR1, COR1, CF3, CN, CONR1R1, NR1R1, COOR1, SO2R2, SR2, SOR2, NR1-COR2, CH2COOM, SO2NR1R2, NR1-SO2Me, NR1-CONR1R2 or NR1-COOR2; B = O, S, SO, SO2, NR1 or N-COOR1; z = 0 or 1, but it is not 0 when n = 0 and D = opt. substd. Ph, or (A)d = H or CN or aminocarbonyl, or a there is a double bond between the alpha C atom and a C atom of the pyrrolidino etc. ring; R1 = H, 1-8C alkyl, Ph or Ph-(1-8C)alkyl; R2 = 1-8C alkyl, Ph or Ph-(1-8C) alkyl; M = metal ion. (2) Pharm. compsn. for use as a Ca antagonist in the treatment of hypertension comprises a cpd. (I) but without the proviso about (B)z. (3) Pharm. compsn. for use as an antihistamine or for the redn. of gastric secretion comprises a cpd. (I) but without the proviso about (B)z. |
