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21 条记录 (耗时 0.034 秒)

    BIRCH REDUCTION OF STEROID SUBSTRATES VIA ALKALI METAL - SILICA GEL MATERIALS
    12.
    发明申请
    BIRCH REDUCTION OF STEROID SUBSTRATES VIA ALKALI METAL - SILICA GEL MATERIALS 审中-公开
    通过阿尔卡利金属 - 二氧化硅凝胶材料减少固体底物

    公开(公告)号：US20110082306A1

    公开(公告)日：2011-04-07

    申请号：US12933971

    申请日：2009-03-24

    申请人： Michael J. Costanzo ,  Mitul N. Patel ,  Paul F. Vogt

    发明人： Michael J. Costanzo ,  Mitul N. Patel ,  Paul F. Vogt

    IPC分类号： C07J51/00

    CPC分类号： C07J1/0077 ,  C07J51/00

    摘要： Steroids are well known, medicinal relevant, chemical entities. There are numerous steroids which have fully or partially reduced ‘A’ rings. These fully or partially reduced ‘A’ rings have been reduced in the past through Birch and other dissolving metal reductions. Novel reducing conditions for steroid substrates are described which utilizes stabilized alkali metal-silica gel materials. The invention relates to a method for reducing a double bond within a steroid by contacting an unsaturated steroid having a phenyl ring with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a proton source under reaction conditions sufficient to form a reduced steroid having a diene structure.

    摘要翻译： 类固醇是众所周知的，药物相关的化学实体。 有许多类固醇有完全或部分减少的“A”戒指。 这些完全或部分减少的“A”环已经通过桦木和其他溶解金属减少而减少。 描述了使用稳定的碱金属 - 硅胶材料的类固醇底物的新型还原条件。 本发明涉及通过在质子源存在下使反应条件下使具有苯环的不饱和类固醇与阶段0或阶段I碱金属 - 硅胶材料接触的方法，该方法足以形成 具有二烯结构的还原类固醇。

    Peptidyl heterocyclic ketones useful as tryptase inhibitors
    13.
    发明授权
    Peptidyl heterocyclic ketones useful as tryptase inhibitors 有权
    肽基杂环酮可用作类胰蛋白酶抑制剂

    公开(公告)号：US06469036B1

    公开(公告)日：2002-10-22

    申请号：US09482802

    申请日：2000-01-13

    申请人： Michael J. Costanzo ,  Bruce E. Maryanoff ,  Stephen C. Yabut

    发明人： Michael J. Costanzo ,  Bruce E. Maryanoff ,  Stephen C. Yabut

    IPC分类号： A61K3140

    CPC分类号： C07K5/06139 ,  C07D277/64 ,  C07D417/12 ,  C07K5/06026

    摘要： The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

    摘要翻译： 本发明涉及一系列作为炎性细胞丝氨酸蛋白酶抑制剂的肽基杂环酮及其组合物和预防和治疗各种免疫缺陷性炎症性疾病的方法。 更具体地，这些化合物是类胰蛋白酶的有效和选择性抑制剂，因此对于预防和治疗与呼吸道相关的炎性疾病如哮喘和过敏性鼻炎是有效的。

    Substituted spiroheterocycles
    15.
    发明授权
    Substituted spiroheterocycles 有权
    取代螺旋环

    公开(公告)号：US07825110B2

    公开(公告)日：2010-11-02

    申请号：US11857891

    申请日：2007-09-19

    申请人： Min A. Xiang ,  Mona Patel ,  Philip Rybczynski ,  Joseph Gunnet ,  Keith T. Demarest ,  Richard Look ,  Bruce Maryanoff ,  Michael J. Costanzo ,  Stephen C. Yabut

    发明人： Min A. Xiang ,  Mona Patel ,  Philip Rybczynski ,  Joseph Gunnet ,  Keith T. Demarest ,  Richard Look ,  Bruce Maryanoff ,  Michael J. Costanzo ,  Stephen C. Yabut

    IPC分类号： A61P9/00 ,  A61K31/55 ,  C07D223/14

    CPC分类号： C07D487/10

    摘要： The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal insufficiency, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

    摘要翻译： 本发明涉及式I的非肽取代的螺杂肼苯并氮平，其可用作加压素受体拮抗剂，用于治疗与加压素受体活性相关的病症，例如涉及增加的血管阻力和心脏功能不全（包括充血性心力衰竭，低钠血症和高血压）的那些。 包含式I化合物的药物组合物和治疗诸如高血压，充血性心力衰竭，心脏功能不全，冠状动脉血管痉挛，心脏缺血，肝硬化，低钠血症，肾血管痉挛，肾功能不全，肾衰竭，糖尿病性肾病，脑水肿， 还公开了脑缺血，中风，血栓形成或保水。