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1. 发明授权

KR100320167B1 성장호르몬분비촉진제 失效
公开(公告)号：KR100320167B1
公开(公告)日：2003-11-14
申请号：KR1019980704973
申请日：1996-12-04
申请人： 화이자 인코포레이티드
发明人： 카르피노필립에이 , 자르딘다실바폴에이 , 레프커브루스에이 , 라간존에이
IPC分类号： C07K5/06
CPC分类号： C07K5/06034 , A61K38/00 , C07D471/04 , C07K5/0202
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating would healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2, or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula I.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中取代基如说明书中所定义，它们是生长激素分泌素并增加内源性生长激素的水平。本发明化合物可用于治疗和预防骨质疏松症，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻重要手术后的蛋白质分解代谢反应，减少因慢性疾病导致的恶病质和蛋白质损失，加速治愈或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，活动性，皮肤厚度的维持，代谢稳态或肾脏动态平衡。本发明化合物还可用于治疗与以下药物联合使用时的骨质疏松症：双膦酸盐化合物如阿仑膦酸盐; 雌激素，孕二烯酮和任选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及用于其的药物组合物。此外，本发明涉及用于增加人类或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素，（Hexarelin），GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及用于制备式I化合物的中间体。

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