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175 条记录 (耗时 0.114 秒)

    Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof
    25.
    发明授权
    Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof 有权
    作为芳香族蛋白酶抑制剂的双环胍衍生物，组合物及其用途

    公开(公告)号：US07759354B2

    公开(公告)日：2010-07-20

    申请号：US11451074

    申请日：2006-06-12

    申请人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Ying Huang ,  Elizabeth M. Smith

    发明人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Ying Huang ,  Elizabeth M. Smith

    IPC分类号： C07D273/06 ,  A61K31/551 ,  A61P31/18 ,  A61K31/553 ,  A61K31/519 ,  C07D243/04 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.

    摘要翻译： 本申请提供了式及其立体异构体，互变异构体或其药学上可接受的盐和溶剂合物的化合物，其中每个式（当存在时）中的U，W，R，R 1，R 2，R 3和R 4如说明书中所定义， 和包含这些化合物的药物组合物。 还公开了使用这些化合物和组合物来抑制天冬氨酰蛋白酶的方法，并且治疗多种疾病和适应症，包括（但不限于）心血管疾病和认知和神经变性疾病。 公开本发明的化合物单独使用或与一种或多种另外的活性成分如胆碱酯酶抑制剂和毒蕈碱m1激动剂和/或m2拮抗剂组合使用。

    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
    27.
    发明申请
    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
    碳链取代的哌啶及其衍生物可用作组胺H3拮抗剂

    公开(公告)号：US20070010513A1

    公开(公告)日：2007-01-11

    申请号：US11455873

    申请日：2006-06-19

    申请人： Robert Aslanian ,  Michael Berlin ,  Ying Huang ,  Kevin McCormick ,  Mwangi Mutahi ,  Neng-Yang Shih ,  Pauline Ting ,  Wing Tom ,  Junying Zheng

    发明人： Robert Aslanian ,  Michael Berlin ,  Ying Huang ,  Kevin McCormick ,  Mwangi Mutahi ,  Neng-Yang Shih ,  Pauline Ting ,  Wing Tom ,  Junying Zheng

    IPC分类号： A61K31/538 ,  A61K31/4709 ,  A61K31/4704 ,  C07D265/12

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

    摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R1 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐，其中：M 1和M 3是CH或N; M 2是CH，CF或N; Y是-C（-O） - ， - C（-S） - ， - （CH 2 CH 2）q - ， - C（-NOR 7） / SO 2 - ） - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H，烷基，烯基或任选取代的环烷基，芳基，杂芳基，杂环烷基或下式的基团：其中环A是单杂芳基环; R 1是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征非酒精性脂肪性肝病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌或认知缺陷障碍的组合物和方法。

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    28.
    发明授权
    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
    用作PDE4抑制剂的取代的2-喹啉基 - 恶唑

    公开(公告)号：US07511062B2

    公开(公告)日：2009-03-31

    申请号：US11130359

    申请日：2005-05-16

    申请人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John H. Schwerdt ,  Pauline C. Ting ,  Shing-Chun Wong ,  Li Xiao

    发明人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John H. Schwerdt ,  Pauline C. Ting ,  Shing-Chun Wong ,  Li Xiao

    IPC分类号： C07D215/38 ,  A61K31/44

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4 H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

    摘要翻译： 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ， - CH 2 F，-CHF 2，-CF 3，-C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟基烷基或-C（O）O烷基; R5和R6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH2F，-CHF2，-CF3，-C（O）OH或-C（O） R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 -C（O）-O-烷基; 和R8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部任意取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8，并且与它们相连的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    29.
    发明申请
    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
    用作PDE4抑制剂的取代的2-喹啉基 - 恶唑

    公开(公告)号：US20060106062A1

    公开(公告)日：2006-05-18

    申请号：US11130359

    申请日：2005-05-16

    申请人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    发明人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    IPC分类号： A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

    摘要翻译： 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

    METHODS, CELLS AND SYSTEMS FOR INCORPORATING NON-CANONICAL AMINO ACIDS INTO PROTEINS
    30.
    发明申请
    METHODS, CELLS AND SYSTEMS FOR INCORPORATING NON-CANONICAL AMINO ACIDS INTO PROTEINS 有权
    将非经典氨基酸掺入蛋白质的方法，细胞和系统

    公开(公告)号：US20120237971A1

    公开(公告)日：2012-09-20

    申请号：US13353106

    申请日：2012-01-18

    申请人： Ying Huang ,  Wenshe Liu ,  Ying Huang

    发明人： Ying Huang ,  Wenshe Liu ,  Ying Huang

    IPC分类号： C12P21/00 ,  C12N1/21 ,  C12N15/63 ,  C12N1/00

    CPC分类号： C12N15/67

    摘要： The present disclosure pertains to methods of incorporating one or more non-canonical amino acids into a protein during a translation of the protein in bacterial cells. The present disclosure also pertains to methods of incorporating one or more non-canonical amino acids into a protein during an in vitro translation of the protein. In additional embodiments, the present disclosure pertains to isolated bacterial cells and in vitro translation systems (e.g., cell-free extract systems) for incorporating one or more non-canonical amino acids into a protein during a translation of the protein.

    摘要翻译： 本公开涉及在蛋白质在细菌细胞中翻译期间将一种或多种非标准氨基酸掺入蛋白质的方法。 本公开还涉及在体外翻译蛋白质期间将一种或多种非标准氨基酸掺入蛋白质的方法。 在另外的实施方案中，本公开涉及在翻译蛋白质期间将一种或多种非标准氨基酸掺入到蛋白质中的分离的细菌细胞和体外翻译系统（例如，无细胞提取系统）。