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    Process for the preparation of a growth hormone secretagogue
    33.
    发明授权
    Process for the preparation of a growth hormone secretagogue 失效
    制备生长激素促分泌素的方法

    公开(公告)号：US5723616A

    公开(公告)日：1998-03-03

    申请号：US736173

    申请日：1996-10-23

    申请人： Peter G. Houghton ,  Audrey Molina ,  Joannis Houpis ,  Joseph E. Lynch ,  Ralph P. Volante

    发明人： Peter G. Houghton ,  Audrey Molina ,  Joannis Houpis ,  Joseph E. Lynch ,  Ralph P. Volante

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07D451/00

    CPC分类号： C07K5/06034 ,  A61K38/00

    摘要： The present invention is directed to a novel process for the preparation of the compound N-�1(R)-�(1,2-dihydro-1-methanesulfonyl-spiro�3H-indole-3,4'-piperdin!-1'-yl)carbonyl!-2-(phenylmethyl-oxy)ethyl!-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.

    摘要翻译： 本发明涉及一种制备化合物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-（苯基甲基 - 氧基）乙基] -2-氨基-2-甲基 - 丙酰胺及其盐，其结构如下：＆lt; IMAGE＆gt;并且具有刺激天然释放的能力 或内源性生长激素。 该化合物可用于治疗需要刺激生长激素生成或分泌的条件，例如在天然生长激素缺乏的人或用于食物或羊毛生产的动物中刺激生长激素将导致较大的， 更有生产力的动物。

    Process for the preparation of N-formimidoyl thienamycin and reagents therefor
    38.
    发明授权
    Process for the preparation of N-formimidoyl thienamycin and reagents therefor 失效
    制备N-甲脒基噻吩霉素及其试剂的方法

    公开(公告)号：US4374772A

    公开(公告)日：1983-02-22

    申请号：US244934

    申请日：1981-03-19

    申请人： George G. Hazen ,  Ralph P. Volante ,  Kenneth E. Wilson

    发明人： George G. Hazen ,  Ralph P. Volante ,  Kenneth E. Wilson

    IPC分类号： C07D477/02 ,  C07D487/04

    CPC分类号： C07D477/02

    摘要： Disclosed is a novel class of substituted and unsubstituted benzyl formimidates, represented in a convenient acid addition salt form (I); and the use of these reagents in the preparation of the antibiotic N-formimidoyl thienamycin (II): ##STR1## wherein A is a non-critical anion such as chloro, bromo, hydrogen sulfate or an alkyl aralkyl or aryl sulfonate, wherein the alkyl moiety has 1-6 carbon atoms and the aryl moiety is phenyl, for example; n is 0, 1 or 2; and X is independently selected from nitro, halo (chloro, bromo, fluoro, and iodo), loweralkyl having from one to six carbon atoms, phenyl, and phenylalkyl having from 7-12 carbon atoms, and --COOR, wherein R is hydrogen or loweralkyl having from one to six carbon atoms.

    摘要翻译： 公开了一类新颖的取代和未取代的苄基甲酰亚胺酯，以方便的酸加成盐形式（I）表示; 以及这些试剂在制备抗生素N-甲亚氨基硫霉素（II）中的用途：其中A是非关键阴离子如氯，溴，硫酸氢或烷基芳烷基或芳基 磺酸盐，其中烷基部分具有1-6个碳原子，并且芳基部分是苯基; n为0,1或2; 和X独立地选自硝基，卤代（氯，溴，氟和碘），具有1至6个碳原子的低级烷基，苯基和具有7-12个碳原子的苯基烷基和-COOR，其中R是氢或 具有1至6个碳原子的低级烷基。