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    Process for Preparing 4-Acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the Intermediates Thereof
    22.
    发明申请
    Process for Preparing 4-Acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the Intermediates Thereof 失效
    制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂的方法及其中间体

    公开(公告)号：US20100256358A1

    公开(公告)日：2010-10-07

    申请号：US12601962

    申请日：2008-05-22

    申请人： Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

    发明人： Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

    IPC分类号： C07D243/14 ,  C07C233/13 ,  C07C251/24 ,  C07C211/29 ,  C07C209/28

    CPC分类号： C07C211/29 ,  C07C209/52 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

    摘要： The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

    摘要翻译： 本发明涉及一种制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂的方法及其中间体。 本发明提供由式I表示的化合物和由式II表示的化合物，以及通过使用式（I）表示的化合物制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂 I，式II表示的化合物和邻硝基苯甲醛。 本发明具有合成步骤较短，原料易得，操作简单等优点。 此外，通过避免使用昂贵且危险的氢化铝锂，该方法是经济和安全的。

    BICYCLIC HETEROCYCLIC COMPOUND
    23.
    发明申请
    BICYCLIC HETEROCYCLIC COMPOUND 审中-公开
    双相杂环化合物

    公开(公告)号：US20100113391A1

    公开(公告)日：2010-05-06

    申请号：US12596643

    申请日：2008-04-17

    申请人： Yuji Koga ,  Takao Okuda ,  Takashi Kamikubo ,  Michihito Kageyama ,  Hiroyuki Moritomo

    发明人： Yuji Koga ,  Takao Okuda ,  Takashi Kamikubo ,  Michihito Kageyama ,  Hiroyuki Moritomo

    IPC分类号： A61K31/695 ,  C07D215/22 ,  C07D239/80 ,  C07F7/02 ,  C07D243/14 ,  A61K31/47 ,  A61K31/517 ,  A61K31/5513 ,  A61P7/02

    CPC分类号： C07D217/24 ,  C07D239/96 ,  C07D243/14 ,  C07D401/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06

    摘要： [Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.

    摘要翻译： [问题]提供了表现出P2Y12抑制作用的化合物，可用作医药，特别是作为血小板聚集抑制剂。 解决方法本发明人急切地研究P2Y12抑制剂。 结果发现，在具体位置具有被低级烷基，环烷基或低级亚烷基 - 环烷基取代的氨基的喹唑啉二酮，异喹诺酮等双环杂环化合物显示优异的血小板聚集抑制作用， 从而完成了本发明。 由于本发明化合物表现出优异的P2Y12抑制作用和血小板聚集抑制作用，因此作为血小板聚集抑制剂是有用的。

    Methods and Tools for The Therapy of Neurodegenerative Pathologies
    24.
    发明申请
    Methods and Tools for The Therapy of Neurodegenerative Pathologies 审中-公开
    神经退行性病变治疗方法与工具

    公开(公告)号：US20090317842A1

    公开(公告)日：2009-12-24

    申请号：US12309492

    申请日：2007-07-20

    申请人： Fabien Schweighoffer ,  Laurent Desire ,  Jérôme Bourdin

    发明人： Fabien Schweighoffer ,  Laurent Desire ,  Jérôme Bourdin

    IPC分类号： G01N33/53 ,  C07D471/04 ,  C07D243/14

    CPC分类号： G01N33/6896 ,  G01N33/5306 ,  G01N33/9426 ,  G01N2800/2821 ,  G01N2800/52

    摘要： The present invention concerns compositions and methods for the treatment of neurodegenerative diseases in which the cognitive functions are altered, such as observed in Alzheimer's disease. More particularly, the invention presents a strategy for human clinical monitoring of the activity and/or effectiveness of neuroprotective treatments, based on biochemical assay of certain platelet parameters, and thus can be done by blood sampling. The invention also concerns methods, tools, constructions and compositions suitable for implementing these strategies.

    摘要翻译： 本发明涉及用于治疗其中认知功能改变的神经变性疾病的组合物和方法，例如在阿尔茨海默病中观察到的。 更具体地说，本发明基于某些血小板参数的生物化学测定，提出了人类临床监测神经保护治疗的活性和/或有效性的策略，因此可以通过血液取样进行。 本发明还涉及适于实施这些策略的方法，工具，构造和组合。

    Registry Method and Control System for Dea Schedule II-V Medicines
    26.
    发明申请
    Registry Method and Control System for Dea Schedule II-V Medicines 有权
    注册表方法和控制系统Dea Schedule II-V药物

    公开(公告)号：US20090208413A1

    公开(公告)日：2009-08-20

    申请号：US11922794

    申请日：2006-02-23

    申请人： Alan J Reis ,  Christian Schafmeister

    发明人： Alan J Reis ,  Christian Schafmeister

    IPC分类号： A61K51/00 ,  C07D243/14 ,  C07C211/01 ,  C07C209/44 ,  C07D211/32 ,  C07D489/00 ,  C07D211/58 ,  C07C215/42 ,  C07D471/04 ,  C12Q1/02

    CPC分类号： C07D487/04 ,  C07B2200/05 ,  C07D243/24 ,  G06F19/00 ,  G06F19/326 ,  G06F19/3456

    摘要： The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.

    摘要翻译： 本发明提供用于合成标记药物的组合物和方法。 本发明进一步提供了通过药物执行时间表V注册为药物执法机构（DEA）时间表II的所有药剂的预防或停止处方药物滥用的方法。 根据本发明，提供了用于监测患者对规定药物治疗的依从性的方法。 本发明还提供了当患者不能使用其处方药物时便于替换处方的方法。 此外，本发明还提供了一种通过自愿或强制性体系增强药物测试来提高员工遵守雇主药物政策的方法。

    BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS
    27.
    发明申请
    BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS 有权
    苯唑酮类化合物可用于治疗皮肤病症

    公开(公告)号：US20090118244A1

    公开(公告)日：2009-05-07

    申请号：US12266239

    申请日：2008-11-06

    申请人： Gary D. Glick

    发明人： Gary D. Glick

    IPC分类号： A61K31/5513 ,  C07D243/14 ,  A61K31/56 ,  A61K31/59 ,  C12N5/08 ,  A61P17/06 ,  A61P17/00

    CPC分类号： C07D243/24 ,  A61K31/5513 ,  A61K45/06

    摘要： The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.

    摘要翻译： 本发明提供一种苯并二氮杂酮化合物及其药物组合物。 本发明还提供了通过施用苯并二氮杂酮来治疗某些皮肤病症例如特应性皮炎，红斑痤疮或银屑病的方法以及通过将这些细胞暴露于苯并二氮杂酮来降低角化细胞细胞的增殖的方法。

    Aminodiazepines as Toll-Like Receptor Modulators
    28.
    发明申请
    Aminodiazepines as Toll-Like Receptor Modulators 有权
    氨基二氮卓作为Toll样受体调节剂

    公开(公告)号：US20080306050A1

    公开(公告)日：2008-12-11

    申请号：US12064196

    申请日：2006-08-17

    申请人： George A. Doherty ,  Zachary Jones

    发明人： George A. Doherty ,  Zachary Jones

    IPC分类号： A61K31/5513 ,  C07D243/14 ,  A61P37/02

    CPC分类号： C07D243/20

    摘要： Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

    摘要翻译： 提供了可用于通过Toll样受体TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

    Urea derivative, medicinal composition containing the same, and medicinal use of these
    29.
    发明申请
    Urea derivative, medicinal composition containing the same, and medicinal use of these 审中-公开
    尿素衍生物，含有其的药物组合物及其药用

    公开(公告)号：US20080161294A1

    公开(公告)日：2008-07-03

    申请号：US11903904

    申请日：2007-09-25

    申请人： Ritsu Suzuki ,  Kenji Yokoyama ,  Tatsuhiro Kondo ,  Hideaki Hirasawa ,  Mikie Kambara ,  Hiroaki Kobayashi

    发明人： Ritsu Suzuki ,  Kenji Yokoyama ,  Tatsuhiro Kondo ,  Hideaki Hirasawa ,  Mikie Kambara ,  Hiroaki Kobayashi

    IPC分类号： A61K31/5513 ,  A61P3/10 ,  C07D243/14

    CPC分类号： A61K45/06 ,  A61K31/5513 ,  C07D243/14 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D413/12

    摘要： Urea derivatives represented by the following general formula (I): which have an agonism of V2 receptor, are useful as agents for the treatment or prevention of diabetes insipidus, nocturia, nocturnal enuresis, overactive bladder or the like.In the formula, R1 represents a hydrogen atom or a C1-6 alkyl group which may have a substituent, R2 is a hydrogen atom or a C1-6 alkyl group, R3 is a hydrogen atom, a C1-6 alkyl group or the like, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, R7 is a hydrogen atom, a heteroaryl group which may have a substituent, a C3-8 cycloalkyl group, an amino group which may have a substituent or a C1-6 alkoxy group which may have a substituted group, M1 is a single bond, a C1-4 alkylene group or the like, Y is N or CRF (in the formula, and RF represents a hydrogen atom, a C1-6 alkyl group or the like, or pharmaceutically acceptable salts thereof, or prodrugs thereof, or pharmaceutical compositions comprising the same and pharmaceutical uses thereof.

    摘要翻译： 由以下通式（I）表示的具有V2受体激动作用的尿素衍生物可用作治疗或预防尿崩症，夜尿症，夜间遗尿症，膀胱过度活动症等的药剂。 在该式中，R 1表示可以具有取代基的氢原子或C 1-6烷基，R 2是氢 原子或C 1-6烷基，R 3是氢原子，C 1-6烷基等，R R 5，R 5和R 6独立地是氢原子，卤素原子等，R 7， 可以具有取代基的杂芳基，C 3-8环烷基，可以具有取代基的氨基或C 1-6烷基， 可以具有取代基的烷氧基，M 1是单键，C 1-4亚烷基等，Y是N或CRF （在该式中，R“F”表示氢原子，C 1-6烷基等，或其药学上可接受的盐或前体药物 或其药物组合物及其药物用途。