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    Imidazolidyl macrolides having immunosuppressive activity
    1.
    发明公开
    Imidazolidyl macrolides having immunosuppressive activity 失效
    咪唑烷 - Makrolide mit免疫抑制剂Wirkung。

    公开(公告)号：EP0536896A1

    公开(公告)日：1993-04-14

    申请号：EP92308132.7

    申请日：1992-09-08

    申请人： MERCK & CO. INC.

    发明人： Goulet, Mark ,  Wyvratt, Matthew J. ,  Sinclair, Peter J. ,  Wong, Frederick

    IPC分类号： C07H19/01 ,  A61K31/70

    CPC分类号： C07H19/01

    摘要： Imidazolidyl macrolides of the general structural Formula I:

    have been prepared from suitable precursors by alkylation and/or arylation at C-3˝ and/or C-4˝ of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

    摘要翻译： 通过在环己基环的C-3 =和/或C-4 =烷基化和/或芳基化，由合适的前体制备通式结构式I的咪唑烷基大环内酯：。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

    Aminomacrolides and derivatives having immunosuppressive activity
    2.
    发明公开
    Aminomacrolides and derivatives having immunosuppressive activity 失效
    氨基马可洛尔和Deriv mit mit免疫抑制剂Wirkung。

    公开(公告)号：EP0428365A1

    公开(公告)日：1991-05-22

    申请号：EP90312340.4

    申请日：1990-11-13

    申请人： MERCK & CO. INC.

    发明人： Beattie, Thomas R. ,  Fischer, Michael H. ,  Ok, Hyun O. ,  Wyvratt, Matthew J.

    IPC分类号： C07H19/01 ,  A61K31/70

    CPC分类号： C07H19/01

    摘要： Aminomacrolides of the general structural Formula I:
    have been prepared from suitable precursors by incorporation of a nitrogen substituent at C-3˝ and/or C-4˝ of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ 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.

    摘要翻译： 通过在环己基环的C-3秒和/或C-4秒处引入氮取代基，由合适的前体制备通式结构式I的氨基马来酰氯：。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫疾病，感染性疾病和/或预防外来器官移植排斥反应。 此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。

    O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl macrolides
    10.
    发明公开
    O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl macrolides 失效
    O-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基 - 马来酰胺。

    公开(公告)号：EP0532088A1

    公开(公告)日：1993-03-17

    申请号：EP92202658.8

    申请日：1992-09-02

    申请人： MERCK & CO. INC.

    发明人： Sinclair, Peter J. ,  Goulet, Mark ,  Wong, Frederick ,  Parsons, William H. ,  Goulet, Joung ,  Wyvratt, Matthew J.

    IPC分类号： C07H19/01 ,  A61K31/70

    CPC分类号： C07H19/01

    摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of the general structural Formula I:

    have been prepared from suitable precursors by alkylation and/or arylation at C-3'' and/or C-4'' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

    摘要翻译： 通过在C-3“和/或C-4'上烷基化和/或芳基化，从合适的前体制备通式为结构式I的O-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基大环内酯： 的环己基环。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。