公开(公告)号：US5726319A

公开(公告)日：1998-03-10

申请号：US510026

申请日：1995-08-01

申请人： Peter Lin ,  William R. Schoen ,  Judith M. Pisano ,  Matthew J. Wyvratt

发明人： Peter Lin ,  William R. Schoen ,  Judith M. Pisano ,  Matthew J. Wyvratt

IPC分类号： A61K38/00 ,  C07C275/24 ,  C07D257/04 ,  C07K5/06 ,  C07D257/00

CPC分类号： C07D257/04 ,  C07C275/24 ,  C07K5/06026 ,  C07K5/06191 ,  A61K38/00

摘要： There are disclosed certain compounds identified as substituted dipeptide analogs which 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 increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such substituted dipeptide analogs as the active ingredient thereof are also disclosed.

摘要翻译： 公开了鉴定为取代的二肽类似物的某些化合物，其促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。 还公开了含有这种取代的二肽类似物作为其活性成分的生长促进组合物。

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。