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281 条记录 (耗时 0.059 秒)

    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
    52.
    发明申请
    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 审中-公开

    公开(公告)号：US20060142324A1

    公开(公告)日：2006-06-29

    申请号：US11355439

    申请日：2006-02-15

    申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

    System and method for multiple pass cooperative processing
    53.
    发明授权
    System and method for multiple pass cooperative processing 有权
    多通道协同处理系统和方法

    公开(公告)号：US07003512B1

    公开(公告)日：2006-02-21

    申请号：US10912174

    申请日：2004-08-06

    申请人： Jeffrey A. Bedell ,  William Hurwood ,  Benjamin Z. Li ,  Sadanand Sahasrabudhe ,  Xinyi Wang ,  Jun Yuan

    发明人： Jeffrey A. Bedell ,  William Hurwood ,  Benjamin Z. Li ,  Sadanand Sahasrabudhe ,  Xinyi Wang ,  Jun Yuan

    IPC分类号： G06F17/30

    CPC分类号： G06F17/30595 ,  G06F17/30592 ,  G06Q10/10 ,  Y10S707/99932 ,  Y10S707/99933 ,  Y10S707/99934 ,  Y10S707/99935

    摘要： A system for collaborative processing, comprising a controlling module with access to at least one relational database capable of performing a first set of functions on the data in the database and at least one external analytical engine, the external analytical engine being external to the relational database and being capable of a second set of functions on the data in the database. The controlling module is capable of iteratively processing a multi-step calculation including generating SQL statements to the relational database, passing preliminary results to an external analytical engine and saving data back into the relational database for further processing until the multi-step calculation is performed.

    摘要翻译： 一种用于协同处理的系统，包括控制模块，该控制模块可访问至少一个能够对数据库中的数据执行第一组功能的关系数据库和至少一个外部分析引擎，所述外部分析引擎在关系数据库外部 并且能够对数据库中的数据进行第二组功能。 控制模块能够迭代处理多步计算，包括生成SQL语句到关系数据库，将初步结果传递给外部分析引擎，并将数据保存回关系数据库进行进一步处理，直到执行多步计算。

    Antimicrobial theta defensins and methods of using same
    54.
    发明申请
    Antimicrobial theta defensins and methods of using same 审中-公开
    抗微生物θ防御素及其使用方法

    公开(公告)号：US20050261193A1

    公开(公告)日：2005-11-24

    申请号：US11126468

    申请日：2005-05-10

    申请人： Michael Selsted ,  Yi-Quan Tang ,  Jun Yuan ,  Andre Ouellette

    发明人： Michael Selsted ,  Yi-Quan Tang ,  Jun Yuan ,  Andre Ouellette

    IPC分类号： A61K38/00 ,  A61K38/10 ,  A61K38/12 ,  C07K7/08 ,  C07K14/47 ,  C12N15/12 ,  C12P21/00

    CPC分类号： C07K7/08 ,  A61K38/12 ,  C07K14/4723 ,  C12P21/00 ,  Y02A50/473 ,  Y02A50/481

    摘要： The present invention relates to an isolated cyclic peptide, theta defensin, having antimicrobial activity, and to theta defensin analogs. A theta defensin can have the amino acid sequence Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5, wherein Xaa1 to Xaa8 are defined; wherein Xaa1 can be linked through a peptide bond to Xaa8; and wherein crosslinks can be formed between Xaa3 and Xaa3, between Xaa5 and Xaa5, and between Xaa7 and Xaa7. For example, the invention provides a theta defensin having the amino acid sequence Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg (SEQ ID NO:1), wherein the Gly at position 1 (Gly-1) is linked through a peptide bond to Arg-18, and wherein disulfide bonds are present between Cys-3 and Cys-16, between Cys-5 and Cys-14, and between Cys-7 and Cys-12. The invention also relates to antibodies that specifically bind a theta defensin and to isolated nucleic acid molecules encoding a theta defensin. In addition, the invention relates to methods of using theta defensin or a theta defensin analog to reduce or inhibit microbial growth or survival in an environment capable of sustaining microbial growth or survival by contacting the environment with the theta defensin.

    摘要翻译： 本发明涉及具有抗微生物活性的分离的环肽，θ防御素，以及θ防御素类似物。 θ防御素可以具有氨基酸序列Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa1-Xaa6-Xaa4-Xaa4-Xaa1-Xaa1-Xaa6-Xaa4-Xaa5-Xaa1-Xaa3-Xaa7-Xaa5，其中Xaa1至Xaa8是 定义 其中Xaa1可通过肽键与Xaa8连接; 并且其中可以在Xaa3和Xaa3之间，Xaa5和Xaa5之间以及Xaa7和Xaa7之间形成交联。 例如，本发明提供具有氨基酸序列Gly-Phe-Cy-Arg-Cys-Leu-Cys-Arg-Arg-Gly-Val-Cys-Arg-Cys-Ile-Cys-Thr-Arg的θ防御素 SEQ ID NO：1），其中位置1处的Gly（Gly-1）通过肽键与Arg-18连接，并且其中二硫键存在于Cys-3和Cys-16之间，Cys-5和Cys之间 -14，以及Cys-7和Cys-12之间。 本发明还涉及特异性结合θ防御素和编码θ防御素的分离的核酸分子的抗体。 此外，本发明涉及使用θ防御素或θ防御素类似物以通过使环境与θ防御素接触来在能够维持微生物生长或存活的环境中减少或抑制微生物生长或存活的方法。

    Aryl fused substituted 4-oxy-pyridines
    56.
    发明授权
    Aryl fused substituted 4-oxy-pyridines 失效
    芳基稠合取代的4-氧 - 吡啶

    公开(公告)号：US06828329B2

    公开(公告)日：2004-12-07

    申请号：US09892024

    申请日：2001-06-26

    申请人： Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    发明人： Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    IPC分类号： A61K3144

    CPC分类号： C07D215/233 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了下式的化合物：其中X，Q，W和如本文所定义。 这些化合物是GABAA脑受体的激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作，过量与 苯二氮卓类药物和增强记忆力。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

    2,4-substituted quinoline derivatives
    58.
    发明授权
    2,4-substituted quinoline derivatives 失效
    2,4-取代喹啉衍生物

    公开(公告)号：US06559163B2

    公开(公告)日：2003-05-06

    申请号：US09931549

    申请日：2001-08-16

    申请人： Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    发明人： Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    IPC分类号： A61K314709

    CPC分类号： C07D231/12 ,  C07D215/52 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04

    摘要： Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了式或其药学上可接受的盐的化合物，其中：表示：并且A，B，G，D，E，Ra，Rb，W和Z在本文中定义。 这些化合物是GABAA脑受体的激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作，过量与 苯二氮卓类药物和增强记忆力。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

    Bicyclic and tricyclic heteroaromatic compounds
    59.
    发明授权
    Bicyclic and tricyclic heteroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US06511987B1

    公开(公告)日：2003-01-28

    申请号：US09709887

    申请日：2000-11-10

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchinson

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchinson

    IPC分类号： C07D47104

    CPC分类号： C07D217/26 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。 这些化合物以高选择性和/或高亲和力结合GABA A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。 还公开了可用于制备这些化合物的中间体。

    Certain isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands
    60.
    发明授权
    Certain isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands 失效
    某些异喹啉胺和酞嗪胺衍生物：促肾上腺皮质激素释放因子受体CRF1特异性配体

    公开(公告)号：US06440969B2

    公开(公告)日：2002-08-27

    申请号：US09852991

    申请日：2001-05-10

    申请人： Jun Yuan ,  Taeyoung Yoon

    发明人： Jun Yuan ,  Taeyoung Yoon

    IPC分类号： C07D23730

    CPC分类号： C07D401/12 ,  C07D217/22 ,  C07D237/34

    摘要： Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula or the pharmaceutically acceptable salts thereof wherein Ar, R1, R2, R3, R4 and W are various organic and inorganic substituents.

    摘要翻译： 公开了在人CRF1受体上是高选择性部分激动剂或拮抗剂的化合物，其可用于治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁症，头痛和焦虑症的诊断和治疗。 所述化合物具有其药学上可接受的盐，其中Ar，R 1，R 2，R 3，R 4和W是各种有机和无机取代基。