公开(公告)号：US20110245159A1

公开(公告)日：2011-10-06

申请号：US12937040

申请日：2010-09-29

申请人： Hamid R. Hoveyda ,  Martin Vézina ,  Eric Fournier ,  René Gagnon ,  Patrick Bhérer

发明人： Hamid R. Hoveyda ,  Martin Vézina ,  Eric Fournier ,  René Gagnon ,  Patrick Bhérer

IPC分类号： A61K38/12 ,  C07K5/08 ,  C07K1/14 ,  C07K1/107 ,  C07K1/34 ,  A61P1/00 ,  A61P1/14 ,  A61P1/04 ,  A61P1/08 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61P25/00 ,  A61P19/08 ,  A61P35/00

CPC分类号： C07D273/00 ,  A61K9/0019

摘要： The present invention provides novel salts and solvates of macrocyclic compounds that bind to and/or are functional agonists of the ghrelin (growth hormone secretagogue) receptor. The invention also relates to polymorphs of these salts and solvates, pharmaceutical compositions containing these salts or solvates, and methods of using the pharmaceutical compositions. These pharmaceutical compositions are useful as therapeutics for a range of disease indications, in particular, for treatment and prevention of gastrointestinal disorders including, but not limited to, postoperative ileus, gastroparesis, including diabetic and postsurgical gastroparesis, opioid bowel dysfunction, chronic intestinal pseudo-obstruction, short bowel syndrome, functional gastrointestinal disorders and gastrointestinal dysmotility, such as that occurring in conjunction with other disease states, in critical care situations or as a result of treatment with pharmaceutical agents. Additionally, the pharmaceutical compositions have application to the treatment and prevention of metabolic and/or endocrine disorders, cardiovascular disorders, central nervous system disorders, bone disorders, inflammatory disorders, hyperproliferative disorders, disorders characterized by apoptosis and genetic disorders.

摘要翻译： 本发明提供与生长素释放肽（生长激素促分泌素）受体结合和/或是功能性激动剂的大环化合物的新型盐和溶剂化物。 本发明还涉及这些盐和溶剂合物的多晶型物，含有这些盐或溶剂化物的药物组合物，以及使用该药物组合物的方法。 这些药物组合物可用作一系列疾病适应症，特别是用于治疗和预防胃肠道疾病的治疗剂，包括但不限于术后肠梗阻，胃轻瘫，包括糖尿病和手术后胃轻瘫，阿片样物质肠功能障碍， 梗阻，短肠综合征，功能性胃肠道疾病和胃肠动力障碍，例如与其他疾病状态一起发生，在重症监护情况下或作为药物治疗的结果。 此外，药物组合物可用于治疗和预防代谢和/或内分泌疾病，心血管疾病，中枢神经系统疾病，骨骼疾病，炎症性疾病，过度增殖性疾病，以凋亡和遗传疾病为特征的疾病。