EP0426225A2 — (6,7-dihydro-5H-pyrrolo[1,2-c]-imidazol-5-yl)- and (5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) substituted 1H-benzotriazole derivatives

USPTO Abstract

(6,7-dihydro-5 H -pyrrolo[1,2-c]imidazolyl-5-yl)- and (5,6,7,8-tetrahydroimidazo­[1,5-a]pyridinyl-5-yl) substituted 1 H -benzotriazole derivatives of formula wherein n is 0 or 1; R¹ is H, NO₂, NH₁, C₁₋₆-alkylamino, halo, C₁₋₆alkyl, OH or C₁₋₆alkyloxy; R² is hydrogen; C₁₋₁₀alkyl; substituted C₁₋₁₀alkyl; C₃₋₆alkenyl; C₃₋₆alkynyl; C₃₋₇cycloalkyl; bicyclo[2.2.1]heptan-2-yl; 2,3-dihydro-1 H -indenyl; 1,2,3,4-­tetrahydronaphthalenyl; phenyl; substituted phenyl; or a radical of formula -OR³; R³ is hydrogen, C₁₋₁₀alkyl; substituted C₁₋₁₀alkyl; C₃₋₆alkenyl; phenyl-­C₃₋₆alkenyl; C₃₋₆alkynyl; pyrimidinyl; diphenylmethyl; 1-C₁₋₄alkylpiperidin-4-yl; the acid addition salts and stereochemically isomeric forms thereof, said compounds being inhibitors of the enzyme aromatase. Pharmaceutical compositions comprising said compounds as active ingredient; method of preparing said compounds and pharmaceutical compositions.