PROCESS FOR PRODUCING (1H-AZOL-1-YL-METHYL)-SUBSTITUTED BENZOTRIAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

摘要

Novel (1H-azol-1-ylmethyl)substituted benzotriazole derivatives of formula CHEM wherein A1=A2-A3=A4 is -CH=N-CH=CH-, -CH=N-CH=N- or -CH=N-N=CH-; R is hydrogen or C1-6alkyl; R1 is hydrogen, C1-10 alkyl, C3-7cycloalkyl, Ar1, Ar2-C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R2 is hydrogen; optionally substituted C1-10alkyl; Ar1; C2-6alkenyl; C2-6alkynyl; C3-7cycloalkyl; bicyclo[2.2.1]heptan-2-yl; 2,3-dihydro-1H-indenyl; 1,2,3,4-tetrahydronaphthalenyl; hydroxy; optionally substituted C2-6alkenyloxy; C2-6alkynyloxy; pyrimidinyloxy; di(Ar2)methoxy; (1-C1-4alkyl-4-piperidinyl)oxy; or optionally substituted C1-10alkyloxy; R3 is hydrogen, nitro, amino, mono- and di(C1-6alkyl)amino, halo, C1-6alkyl, hydroxy or C1-6alkyloxy; wherein Ar1 is phenyl, substituted phenyl, naphthalenyl, pyridinyl, aminopyridinyl, imidazolyl, triazolyl, thienyl, halothienyl, furanyl, C1-6alkylfuranyl, halofuranyl or thiazolyl; and Ar2 is phenyl, substituted phenyl or pyridinyl; the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof, which compounds are estrogene hormone biosynthesis inhibitory agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.