发明公开
EP0445975A1 New hydroxymacrolide derivatives having immunosuppressive activity
失效
羟基马来酰胺 - 诱导mit免疫抑制剂Wirkung。
- 专利标题： New hydroxymacrolide derivatives having immunosuppressive activity
- 专利标题（中）： 羟基马来酰胺 - 诱导mit免疫抑制剂Wirkung。
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申请号： EP91301686.1申请日： 1991-02-28
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公开(公告)号： EP0445975A1公开(公告)日： 1991-09-11
- 发明人: Bochis, Richard J. , Ok, Hyun O. , Wyvratt, Matthew J.
- 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： US486700 19900301
- 主分类号： C07H19/01
- IPC分类号： C07H19/01 ; C07D498/18 ; A61K31/70
摘要：
Novel hydroxymacrolide derivatives of the general structual Formula I:
have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectous diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.
have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectous diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.
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