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    PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS
    82.
    发明公开
    PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS 失效
    VERFAHREN ZUR HERSTELLUNG药物增容剂盐酸N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰氨基嘌呤

    公开(公告)号：EP0967221A4

    公开(公告)日：2002-05-02

    申请号：EP98932585

    申请日：1998-07-21

    申请人： KANEKA CORP

    发明人： UEDA YASUYOSHI ,  KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  YANAGIDA YOSHIFUMI ,  FUSE YOSHIHIDE

    IPC分类号： A61P9/12 ,  C07K1/02 ,  C07K1/08 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062

    CPC分类号： C07K5/0222 ,  C07K5/06026

    摘要： A process for preparing pharmacologically acceptable salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids, comprising the steps of: condensing an amino acid with N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxyanhydride under basic conditions; decarboxylating the condensate under neutral to acidic conditions to prepare an N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acid; and converting the product to a pharmacologically acceptable salt thereof, characterized in that a series of procedures up to the formation of a pharmacologically acceptable salt or up to the withdrawal of the pharmaceutically acceptable salt thereof are carried out in an aqueous liquid to inhibit the production of a by-product (3). According to this process, high-quality pharmacologically acceptable salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids can be prepared in high yields in a cost-effective manner on a commercial scale.

    摘要翻译： 制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸的药理学上可接受的盐的方法，包括以下步骤：使氨基酸与N-（1（S） - 乙氧羰基-3 - 苯基丙基）-L-丙氨酸N-羧酸酐在碱性条件下; 在中性至酸性条件下将缩合物脱羧基以制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸; 并将该产物转化成其药理学上可接受的盐，其特征在于在含水液体中进行一系列形成药理学上可接受的盐或直至其药学上可接受的盐的程序，以抑制 一个副产品（3）。 根据该方法，可以以商业规模以高成本效益的方式高产率地制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸的高质量药理学上可接受的盐。

    Dipeptide derivatives as growth hormone secretagogues
    89.
    发明公开
    Dipeptide derivatives as growth hormone secretagogues 有权
    Dipeptide zurFörderungder Sekretion des Wachstumshormons

    公开(公告)号：EP1002802A1

    公开(公告)日：2000-05-24

    申请号：EP99309036.4

    申请日：1999-11-12

    申请人： Pfizer Products Inc.

    发明人： Griffith, David Andrew ,  Bronk, Brian Scott

    IPC分类号： C07K5/03 ,  C07K5/062 ,  A01K67/00 ,  A61K38/05 ,  A61K38/06 ,  A61P5/06

    CPC分类号： C07K5/06034 ,  A61K38/05 ,  C07K5/0207 ,  C07K5/06191 ,  A61K2300/00

    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 therapeutically effective in treating osteoporosis and/or frailty, 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 wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty 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 therapeutically effective 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： 本发明涉及式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其为生长激素分泌因子并且增加内源性生长激素的水平。 本发明的化合物在治疗骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症方面具有治疗上的有效性; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少由于慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，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，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。 当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物，例如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。 此外，本发明涉及治疗有效增加人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。 本发明还涉及可用于制备式I化合物的中间体。