Pyrroloimidazolyl and imidazopyridinyl substituted

专利名称：Pyrroloimidazolyl and imidazopyridinyl

substituted 1H- benzimidazole derivatives

发明人：Marcel A. C. Janssen,Alfons H. M.

Raeymaekers,Eddy J. E. Freyne,Michael N.Greco

申请号：US08/2565申请日：19940707公开号：US057102A公开日：19951010

摘要：Pyrroloimidazolyl and imidazopyridinyl substituted 1H- benzimidazolederivatives having the formula ##STR1## wherein n is 0 or 1;

< P>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;< P>

R. sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7cycloalkyl; phenyl; substituted phenyl; C. sub.1-4 alkyl substituted with phenyl,substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7cycloalkyl; and< P>< P>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 alkylsubstituted with phenyl, piperazinyl, 4-(C.sub.1- 4 alkyl) piperazinyl or morpholinyl;

each substituted phenyl independently is phenyl substituted with a substituentindependently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6alkyl, 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, havingsex hormone synthesis inhibiting properties. Compositions containing said compounds offormula (I). Preparations of said compounds and compositions, and use thereof fortreating mammals suffering from sex hormone disorders.

申请人：JANSSEN PHARMACEUTICA, N.V.

代理人：Charles J. Metz

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