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    • 9. 发明授权
    • Halomacrolides and derivatives having immunosuppressive activity
    • 具有免疫抑制活性的灭麦芽糖和衍生物
    • US5143918A
    • 1992-09-01
    • US759747
    • 1991-09-12
    • Richard J. BochisMatthew J. Wyvratt, Jr.
    • Richard J. BochisMatthew J. Wyvratt, Jr.
    • C07H19/01
    • C07H19/01
    • Novel C-3" and C-4" halogen-substituted macrolides of FK-506 type structural Formula I: ##STR1## are described. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart 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 such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasulitides erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.
    • 描述了FK-506型结构式I的新型C-3“和C-4”卤素取代的大环内酯类。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主中用于治疗自身免疫性疾病(如幼年型糖尿病,多发性硬化和类风湿性关节炎),感染性疾病和/或预防外来器官移植排斥反应。 骨髓和心脏移植。 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,如牛皮癣,特应性皮肤病,接触性皮炎和进一步湿疹性皮肤病,脂溢性皮炎,扁平苔藓,天疱疮,大疱 类天疱疮,大疱性表皮松解症,荨麻疹,血管紧张素,血管舒张红斑,皮肤嗜酸粒细胞,红斑狼疮或斑秃。