7-substituted 4-aza cholanic acid derivatives and their use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546 77, 546159, 546285, 562499, 549 69, 549480, 548557, A61K 3144, C07D22118, C07D22104

Patent

active

055959962

ABSTRACT:
Compounds of the Formula I ##STR1## wherein: the dotted line indicates that a double bond may be present or absent; R.sup.1 is H, methyl or ethyl; R.sup.2 is .alpha.- or .beta.-C.sub.1-10 straight or branched alkyl; R.sup.3 is CO.sub.2 H, CN, CO.sub.2 R.sup.4, COHNR.sup.4, or CON(R.sup.4).sub.2 ; R.sup.4 is H, C.sub.1-10 straight or branched alkyl, aryl, heteroaryl, or aralkyl; Aryl is phenyl, substituted phenyl, naphthyl, or biphenyl; Heteroaryl is pyridyl, pyrrolyl, thienyl, furanyl or quinolinyl; and Aralkyl is C.sub.1-10 alkyl substituted with one to three phenyl or substituted phenyl moieties; and their pharmaceutically acceptable salts are described. These compounds are 5.alpha.-reductase type 1 inhibitors. They may be used for treating conditions associated with an excess of DHT, either alone or in combination with other 5.alpha.-reductase inhibitors.

REFERENCES:
patent: 5215894 (1993-06-01), Arison et al.
patent: 5304562 (1994-04-01), Biollaz
patent: 5359071 (1994-10-01), Durette et al.
patent: 5378710 (1995-01-01), Biollaz
patent: 5418238 (1995-05-01), Panzeri et al.

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