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2. 发明申请

WO1997015574A1 POLYMORPHIC FORMS OF A GROWTH HORMONE SECRETAGOGUE 审中-公开
标题翻译：生长激素密码子的多形态
公开(公告)号：WO1997015574A1
公开(公告)日：1997-05-01
申请号：PCT/US1996016955
申请日：1996-10-23
申请人： MERCK & CO., INC. , DRAPER, Jerome, P. , DUBOST, David, C. , KAUFMAN, Michael, J. , MCCAULEY, James, A. , VANDRILLA, Jennifer, L. , VARSOLONA, Richard, J.
发明人： MERCK & CO., INC.
IPC分类号： C07D471/10
CPC分类号： C07D471/10 , A61K38/00 , C07K5/06034
摘要： This invention is concerned with polymorphic forms of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering 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, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)-ethyl]-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.
摘要翻译：本发明涉及化合物N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基] - 2-（苯基甲氧基）乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐，其是生物激素促分泌素，其可用于食用动物以促进其生长，从而使食用肉制品的生产更有效，并且在人类中，或以生长激素分泌不足为特征的医疗状况，以及治疗由生长激素的合成代谢作用改善的医疗状况。本发明的多晶型物质具有优于其他已知形式的N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基 ] -2-（苯基甲氧基） - 乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐的热力学稳定性和药物制剂中的适用性。本发明还涉及制备这些多晶型物的方法，包含这些多晶型形式作为活性成分的药物制剂以及化合物的多晶形式及其制剂在治疗某些疾病中的用途。

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