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55 条记录 (耗时 0.031 秒)

    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
    11.
    发明授权
    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity 失效
    具有免疫抑制活性的O-芳基，O-烷基，O-烯基和O-炔基大环内酯

    公开(公告)号：US5250678A

    公开(公告)日：1993-10-05

    申请号：US875036

    申请日：1992-05-01

    申请人： Mark Goulet ,  Frederick Wong ,  Peter J. Sinclair ,  Matthew J. Wyvratt

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

    IPC分类号： A61K31/41 ,  A61K31/40 ,  A61K31/445 ,  A61P17/00 ,  A61P29/00 ,  A61P31/12 ,  A61P37/06 ,  C07D498/18 ,  C07D491/16 ,  A61K31/435

    CPC分类号： C07D498/18

    摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## 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 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, 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.

    Imidazolidyl rapamycin derivatives
    15.
    发明授权
    Imidazolidyl rapamycin derivatives 失效
    咪唑烷雷怕霉素衍生物

    公开(公告)号：US5310903A

    公开(公告)日：1994-05-10

    申请号：US26925

    申请日：1993-03-05

    申请人： Mark Goulet ,  William H. Parsons ,  Matthew J. Wyvratt

    发明人： Mark Goulet ,  William H. Parsons ,  Matthew J. Wyvratt

    IPC分类号： C07D498/18 ,  A61K31/395

    CPC分类号： C07D498/18

    摘要： Imidazolidyl rapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.

    摘要翻译： 一般结构式I的咪唑烷基雷帕霉素衍生物：通过C-42和/或C-31的烷基化和/或芳基化从合适的前体制备。 这些化合物可用于哺乳动物宿主用于治疗自身免疫性疾病和炎症疾病，感染性疾病，预防外来器官移植排斥和治疗实体瘤。

    Naphtho-fused lactams promote release of growth hormone
    20.
    发明授权
    Naphtho-fused lactams promote release of growth hormone 失效
    萘普生内含物促进生长激素的释放

    公开(公告)号：US06211174B1

    公开(公告)日：2001-04-03

    申请号：US09159451

    申请日：1998-09-24

    申请人： Robert J. Devita ,  Matthew J. Wyvratt

    发明人： Robert J. Devita ,  Matthew J. Wyvratt

    IPC分类号： C07D22314

    CPC分类号： C07D281/08 ,  A61K31/66 ,  C07D223/14 ,  C07D267/10 ,  A61K31/55 ,  A61K2300/00

    摘要： The present invention is directed to certain naphtho-fused lactams of the general structural formula: wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone.

    摘要翻译： 本发明涉及以下通式的某些萘并稠合内酰胺：其中R1，R1a，R1b，R2a，R2b，R3a，R4，R5，R6，A，L，X，n，p和w分别为 本文定义。 这些化合物促进人和动物中生长激素的释放。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。