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1.发明授权Novel 6-position cyclosporin analogs as non-immunosuppressive antagonists of cyclosporin binding to cyclophilin 失效新型6位环孢菌素类似物作为环己酮与亲环蛋白结合的非免疫抑制拮抗剂
公开(公告)号：US4914188A
公开(公告)日：1990-04-03
申请号：US121827
申请日：1987-11-16
申请人： Francis J. Dumont , Philippe L. Durette , Arsenio A. Pessolano , Joshua S. Boger , Nolan H. Sigal
发明人： Francis J. Dumont , Philippe L. Durette , Arsenio A. Pessolano , Joshua S. Boger , Nolan H. Sigal
摘要： Novel cyclosporin analogs containing a MeAla or MeAbu residue at the 6-position of the cyclic undecapeptide have been synthesized and found unexpectedly to exhibit antagonistic activity toward cyclosporin A binding to its cytosolic protein receptor, cyclophilin, without being immunosuppressive.
摘要翻译： 已经合成了在环状十一肽的6位含有MeAla或MeAbu残基的新型环孢菌素类似物，意外地出现，表现出对环胞菌素A与其胞质蛋白受体亲环蛋白结合的拮抗作用，没有免疫抑制。
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公开(公告)号：US5342935A
公开(公告)日：1994-08-30
申请号：US985088
申请日：1992-12-02
IPC分类号： C07H19/01 , C07D267/00
CPC分类号： C07H19/01
摘要： Hydroxymacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation at C-20. These macrolides are useful as antagonists of FK-506-type immunosuppressants. The compounds of the present invention are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, the compounds of the present invention have utility as antidotes for overdoses of FK-506-type immunosuppressants.
摘要翻译： 羟基甲基丙烯酰胺和一般结构式I的衍生物：我已经通过在C-20氧化由合适的前体制备。 这些大环内酯可用作FK-506型免疫抑制剂的拮抗剂。 本发明的化合物可用于修饰FK-506型免疫抑制剂在治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应中的剂量。 此外，本发明的化合物可用作FK-506型免疫抑制剂过量的解毒剂。
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公开(公告)号：US5190950A
公开(公告)日：1993-03-02
申请号：US766908
申请日：1991-09-26
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： A method for the modification of treatment of an immuno regulatory disorder or disease with an FK-506-type immunosuppressive macrolide comprising the administration to a mammalian species in need of such modification of an effective amount of a compound of the formula I. ##STR1##
摘要翻译： 一种用FK-506型免疫抑制性大环内酯治疗免疫调节性疾病或疾病的方法，包括向需要这种修饰的哺乳动物物种施用有效量的式I化合物。
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