Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives
AssigneeJanssen Pharmaceutica NV
InventorsMarcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
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AssigneeJanssen Pharmaceutica NV
InventorsMarcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
Estimating the term…
Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1; R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy; R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; and R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl; each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, formyl, (hydroxyimino)methyl, cyano, amino, mono- and di(C.sub.1-6 alkyl)amino and nitro, having sex hormone synthesis inhibiting properties. Compositions containing said compounds of formula (I). Preparations of said compounds and compositions, and use thereof for treating mammals suffering from sex hormone disorders.
A method of inhibiting the action of the enzymes 17-hydroxyl-/17,20-lyase and aromatase in mammals, which method comprises administering to said mammals a therapeutically effective amount of a compound of the formula:
Dependencies are inferred from the claim text.