发明公开
EP0462664A2 Specific 17beta-thiobenzoyl-4-aza-5alpha-androst-1-en-3-ones as antiandrogenic agents
失效
17-β-硫代苯甲酰基-4-氮杂-5-α-雄甾-1-烯-3-酮als抗雄激素药物Medikamente。
- 专利标题： Specific 17beta-thiobenzoyl-4-aza-5alpha-androst-1-en-3-ones as antiandrogenic agents
- 专利标题（中）： 17-β-硫代苯甲酰基-4-氮杂-5-α-雄甾-1-烯-3-酮als抗雄激素药物Medikamente。
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申请号： EP91201491.7申请日： 1991-06-14
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公开(公告)号： EP0462664A2公开(公告)日： 1991-12-27
- 发明人: Steinberg, Nathan G. , Rasmusson, Gary H. , Salzmann, Thomas N.
- 申请人： MERCK & CO. INC.
- 申请人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人： MERCK & CO. INC.
- 当前专利权人： MERCK & CO. INC.
- 当前专利权人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构： Thompson, John Dr.
- 优先权： US540965 19900620
- 主分类号： C07J73/00
- IPC分类号： C07J73/00 ; A61K31/56
摘要：
Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogenic agents of the formula:
wherein
R is selected from hydrogen, methyl and ethyl and
R ² is phenyl substituted with one or more of:
-SH, -SC₁-C₄ alkyl, -SO-C₁-C₄alkyl, -SO₂-C₁-C₄ alkyl, -SO₂N-(C₁-C₄ alkyl)₂, C₁-C₄ alkyl, -(CH₂) m SH, -S(CH₂) n OCOCH₃, where m is 1-4, n is 1-3, and providing C₁-C₄ alkyl is only present when one of the above sulfur-
containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
wherein
R is selected from hydrogen, methyl and ethyl and
R ² is phenyl substituted with one or more of:
-SH, -SC₁-C₄ alkyl, -SO-C₁-C₄alkyl, -SO₂-C₁-C₄ alkyl, -SO₂N-(C₁-C₄ alkyl)₂, C₁-C₄ alkyl, -(CH₂) m SH, -S(CH₂) n OCOCH₃, where m is 1-4, n is 1-3, and providing C₁-C₄ alkyl is only present when one of the above sulfur-
containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
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