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164 条记录 (耗时 0.034 秒)

    IMIDAZOLE-2-THIONES
    41.
    发明申请
    IMIDAZOLE-2-THIONES 有权
    咪唑-2 -THIONES

    公开(公告)号：US20080091028A1

    公开(公告)日：2008-04-17

    申请号：US11873537

    申请日：2007-10-17

    申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

    发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

    IPC分类号： C07D215/12 ,  C07D215/02 ,  C07D215/22 ,  C07D233/06 ,  C07D233/30

    CPC分类号： C07D233/84 ,  C07D233/70 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

    摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

    摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

    Process for Preparing Rebamipide
    43.
    发明申请
    Process for Preparing Rebamipide 有权
    制备瑞巴派特的方法

    公开(公告)号：US20070249835A1

    公开(公告)日：2007-10-25

    申请号：US10587509

    申请日：2005-11-30

    申请人： Shinji Nishitani ,  Norio Fukuda

    发明人： Shinji Nishitani ,  Norio Fukuda

    IPC分类号： C07D215/02

    CPC分类号： C07D215/227

    摘要： The invention provides an improved process for preparing rebamipide that is useful as a medicament, which makes it possible to prepare rebamipide with high purity and high yield. The invention is an improved process for preparing rebamipide of the formula (1), comprising subjecting a carbostyril amino acid compound of the formula (5) or a salt thereof containing a compound of the formula (11) as an impurity to a reduction treatment in the presence of hydrogen and a catalyst in a basic aqueous solution, thereby selectively reducing the impurity compound (11) to transform into the carbostyril amino acid compound (5); and then acylating the compound (5) in a basic aqueous solution to give rebamipide (1).

    摘要翻译： 本发明提供了一种用于制备可用作药物的瑞巴派特的改进方法，其使得可以以高纯度和高产率制备瑞巴派特。 本发明是制备式（1）的瑞巴派特的改进方法，其包括使式（5）的喹诺酮类氨基酸化合物或其含有式（11）化合物的盐作为杂质进行还原处理 在碱性水溶液中存在氢和催化剂，从而选择性地还原杂质化合物（11）以转化成喹诺酮类氨基酸化合物（5）; 然后在碱性水溶液中酰化化合物（5），得到瑞巴派特（1）。

    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
    44.
    发明申请
    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 有权
    对映体纯氨基取代稠合双环的合成

    公开(公告)号：US20070060757A1

    公开(公告)日：2007-03-15

    申请号：US11598955

    申请日：2006-11-14

    申请人： Ernest McEachern ,  Gary Bridger ,  Krystyna Skupinska ,  Renato Skerlj ,  Wen Yang

    发明人： Ernest McEachern ,  Gary Bridger ,  Krystyna Skupinska ,  Renato Skerlj ,  Wen Yang

    IPC分类号： C07D217/02 ,  C07D215/02

    CPC分类号： C07D217/22 ,  C07D215/06 ,  C07D215/20 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D215/48 ,  C07D221/04 ,  C07D241/42 ,  C07D307/79 ,  C07D491/04

    摘要： This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

    摘要翻译： 本发明描述了合成和拆分外消旋氨基取代的稠合双环体系的各种方法。 一个方法利用氨基取代的稠合双环芳族环系统的选择性氢化。 另一种方法是通过亚硝化制备外消旋氨基取代的稠合双环体系。 此外，本发明描述了外消旋混合物的酶拆分以产生氨基取代的稠合双环的（R） - 和（S）形式，以及外消旋化方法以回收未预期的对映异构体。 本发明进一步提供的是主要氨基取代的稠合双环体系的（R） - 或（S） - 对映异构体的不对称合成。

    Antitumor agents
    45.
    发明申请
    Antitumor agents 有权

    公开(公告)号：US20070060612A1

    公开(公告)日：2007-03-15

    申请号：US11223806

    申请日：2005-09-09

    申请人： Jerome Horwitz ,  Lisa Polin

    发明人： Jerome Horwitz ,  Lisa Polin

    IPC分类号： A61K31/4704 ,  C07D215/02

    CPC分类号： C07D215/22

    摘要： The invention provides compounds of formula I: wherein Y is F, Cl or Br; or a pharmaceutically acceptable salt thereof. The compounds are effective antitumor agents. The invention also provides pharmaceutical compositions comprising a compound of formula I or a salt thereof, intermediates useful for preparing a compound of formula I, and therapeutic methods comprising administering a compound of formula I or a salt thereof to a mammal in need thereof.

    Process for the preparation of aripiprazole
    46.
    发明申请
    Process for the preparation of aripiprazole 失效
    制备阿立哌唑的方法

    公开(公告)号：US20060258869A1

    公开(公告)日：2006-11-16

    申请号：US11448504

    申请日：2006-06-07

    申请人： Pandurang Deshpande ,  Parven Luthra ,  Ashok Shanishchara ,  Ramesh Manepalli ,  Dharmesh Mistry

    发明人： Pandurang Deshpande ,  Parven Luthra ,  Ashok Shanishchara ,  Ramesh Manepalli ,  Dharmesh Mistry

    IPC分类号： C07D215/02 ,  C07D215/00

    CPC分类号： C07D215/227

    摘要： The present invention relates to an improved process for the preparation of 7-[4[-(2,3-dichlorophenyl) -1-piperazinyl]butoxy]3,4-dihydro-2-(1H) quinolinone (Aripiprazole) having dimer impurity less than 0.15%, particularly, the present invention relates to an improved process for the preparation of 7-(4-chlorobutoxy)-3,4-dihydrocarbostyril of formula (I) having dimer impurity less than 0.5% comprising a step of, reacting 7-hydroxy-tetrahydroquinolinone of formula (III) with 1-bromo-4-chlorobutane in the presence of a base in a solvent.

    摘要翻译： 本发明涉及制备具有二聚体杂质的7- [4 - [（2,3-二氯苯基）-1-哌嗪基]丁氧基] 3,4-二氢-2-（1H）喹啉酮（阿立哌唑）的改进方法 小于0.15％，特别是本发明涉及制备具有二聚体杂质小于0.5％的式（I）的7-（4-氯丁氧基）-3,4-二氢喹诺酮的改进方法，包括以下步骤：使 （III）的7-羟基 - 四氢喹啉酮与1-溴-4-氯丁烷在碱存在下在溶剂中反应。