NOVEL 4-PIPERIDINYLCARBONYL DERIVATIVES

摘要

4-piperidinylcarbonyl derivatives having formula (I), wherein -A?1=A2-A3=A4¿- is a bivalent radical having the formula -CH=CH-CH=CH- (a-1), -N=CH-CH=CH- (a-2), -CH=N-CH=CH- (a-3), -CH=CH-N=CH- (a-4), -CH=CH-CH=N- (a-5), -N=CH-N=CH- (a-6) or -CH=N-CH=N- (a-7); R1 is aryl1 or a radical of formula -D-R2 wherein D is O or S; R2 is C¿1-6?alkyl optionally substituted with hydroxy, C1-6alkyloxy, carboxyl or C1-6alkyloxy-carbonyl; m is 1, 2, 3 or 4; n is 0, 1 or 2; L is hydrogen; C1-12alkyl; C3-6cycloalkyl; C3-6alkenyl optionally substituted with aryl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; arylcarbonyl; arylC1-6alkyloxycarbonyl; -Alk-R?3¿ (b-1); -Alk-Y-R4 (b-2); -Alk-Z1-C(=X)-Z2-R5 (b-3); -CH¿2?-CHOH-CH2-O-R?6¿ (b-4) or -Alk-CHOH-R14 (b-5); wherein Alk is C¿1-6?alkanediyl; R?3¿ is cyano, aryl or Het; R?4 and R5¿ are hydrogen, aryl, Het or C¿1-6?alkyl optionally substituted with aryl or Het; R?6¿ is aryl or naphthalenyl; R14 is aryl; Y is O, S, NR7; said R7 being hydrogen, C¿1-6?alkyl or C1-6alkylcarbonyl; Z?1 and Z2¿ independently are O, S, NR8 or a direct bond; R8 being hydrogen or C¿1-6?alkyl; X is O, S or NR?9¿; said R9 being hydrogen, C¿1-6?alkyl or cyano; provided that when -A?1=A2-A3=A4¿- is a radical of formula (a-1) and R1 is phenyl optionally substituted with C¿1-6?alkyl, C1-6alkyloxy, halo or hydroxy; then L is other than hydrogen, C1-6alkyloxycarbonyl or other than a radical of formula -Alk-R?3¿ (b-1), -Alk-O-R4 (b-2-a), -Alk-C(=O)-R5 (b-3-a) or -Alk-CHOH-R14 (b-5) wherein R?3, R4, R5 and R14¿ are phenyl optionally substituted with halo, hydroxy, C¿1-6?alkyl, C1-6alkyloxy, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof having antihistaminic properties, compositions containing the same and methods of treating warm-blooded animals suffering from allergic diseases.