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    • 6. 发明授权
    • Alkylidene macrolides having immunosuppressive activity
    • 具有免疫抑制活性的亚烷基大环内酯类
    • US5284840A
    • 1994-02-08
    • US897738
    • 1992-06-12
    • Kathleen RupprechtRobert Baker
    • Kathleen RupprechtRobert Baker
    • C07D498/18A61K31/395C07D267/00
    • C07D498/18
    • Alkylidene macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by derivitization at C-9 or C-22. 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.
    • 通过在C-9或C-22衍生化,从合适的前体制备通式结构式I的亚烷基大环内酯: 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。