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    Amino O-aryl macrolides having immunosuppressive activity
    4.
    发明授权
    Amino O-aryl macrolides having immunosuppressive activity 失效
    具有免疫抑制活性的氨基O-芳基大环内酯类

    公开(公告)号：US5262533A

    公开(公告)日：1993-11-16

    申请号：US876634

    申请日：1992-05-06

    申请人： Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

    发明人： Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

    IPC分类号： C07D498/18 ,  C07D491/16 ,  A61K31/395

    CPC分类号： C07D498/18

    摘要： Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/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. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

    摘要翻译： 一般结构式I的氨基O-芳基大环内酯是通过在环己基环的C-3“/ C-4”处的芳基化和胺化由合适的前体制备的。 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。 此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发或脱发性秃发症中， 在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管的炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性小肠结肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。

    Alkyl and alkenyl macrolides having immunosuppressive activity
    5.
    发明授权
    Alkyl and alkenyl macrolides having immunosuppressive activity 失效
    具有免疫抑制活性的烷基和链烯基大环内酯类

    公开(公告)号：US5284877A

    公开(公告)日：1994-02-08

    申请号：US897711

    申请日：1992-06-12

    申请人： Helen M. Organ ,  Mark A. Holmes ,  Judith M. Pisano ,  Matthew J. Wyvratt

    发明人： Helen M. Organ ,  Mark A. Holmes ,  Judith M. Pisano ,  Matthew J. Wyvratt

    IPC分类号： C07D498/18 ,  C07H19/01 ,  A61K31/395 ,  C07D267/00

    CPC分类号： C07D498/18 ,  C07H19/01

    摘要： Alkyl and alkenyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and derivitization at C-17. 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. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia oralopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing entercolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

    摘要翻译： 一般结构式I的烷基和链烯基大环内酯：通过在C-17处的氧化和衍生，由合适的前体制备。 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。 此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发性秃发症的过程中， 在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。