发明公开
EP1002792A1 2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME
失效
2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN,IHRE MEDISINISCHE ANWENDUNG UND ZWISCHENPRODUKTE ZU IHRER SYNTHESE
- 专利标题: 2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME
- 专利标题(中): 2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN,IHRE MEDISINISCHE ANWENDUNG UND ZWISCHENPRODUKTE ZU IHRER SYNTHESE
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申请号: EP98911211.5申请日: 1998-04-03
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公开(公告)号: EP1002792A1公开(公告)日: 2000-05-24
- 发明人: ADACHI, Kunitomo Yoshitomi Pharm. Industries, , AOKI, Yoshiyuki Yoshitomi Pharm. Industries, Ltd. , HANANO, Tokushi Yoshitomi Pharm. Industries, Ltd. , TESHIMA, Koji Yoshitomi Pharm. Industries, Ltd., , HOSHINO, Yukio Yoshitomi Pharm. Industries, Ltd. , FUJITA, Tetsuro
- 申请人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 申请人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541-0046 JP
- 专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541-0046 JP
- 代理机构: von Kreisler, Alek, Dipl.-Chem.
- 优先权: JP8625597 19970404
- 国际公布: WO9845249 19981015
- 主分类号: C07C225/16
- IPC分类号: C07C225/16 ; C07C215/34 ; C07C223/02 ; A61K31/135
摘要:
The present invention relates to a compound of the general formula
wherein R 1 , R 2 , R 3 and R 4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.
wherein R 1 , R 2 , R 3 and R 4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.
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