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21 条记录 (耗时 0.027 秒)

    Substituted Thiazoleacetic Acid as Crth2 Ligands
    1.
    发明申请
    Substituted Thiazoleacetic Acid as Crth2 Ligands 审中-公开
    取代噻唑乙酸作为Crth2配体

    公开(公告)号：US20080119456A1

    公开(公告)日：2008-05-22

    申请号：US11597839

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/55 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D277/30 ,  C07D417/04 ,  C07D417/06

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N═N—. —NR7—, —CR7═CR8—, —CR7═N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎; 其中X 1是-S - ， - O - ， - N-N-。 -NR 7 - ，-CR 7 -CR 8 - ，-CR 7-N-，其中R R 7和R 8独立地是氢或C 1 -C 3烷基; A是羧基-COOH或羧基生物电子等排体; 环Ar 2和Ar 3各自独立地表示苯基或5或6元单环杂芳基环，或由5-或6-元环组成的双环系统 苯并稠合或稠合到5-或6-元单环杂芳基环的碳环或杂环，所述环或环系统任选被取代; 环B如Ar 2和Ar 3所定义，或任选取代的N-吡咯烷基，N-哌啶基或N-氮杂环丁基环; s为0或1; L1，L2和L4是描述中定义的连接基团; Q 1和Q 2表示如说明书中定义的取代基。

    CRTH2 Receptor Ligands For Medicinal Uses
    2.
    发明申请
    CRTH2 Receptor Ligands For Medicinal Uses 失效
    CRTH2受体配体用于药用

    公开(公告)号：US20090099189A1

    公开(公告)日：2009-04-16

    申请号：US11597873

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A61K31/53 ,  C07D263/32 ,  A61K31/421 ,  C07D403/02 ,  C07D231/12 ,  A61K31/415

    CPC分类号： A61K31/415 ,  A61K31/454 ,  C07D231/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/34

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，Ar 3各自独立地表示苯基或5-或6-元单环杂芳基环，或由5-或6-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。

    CRTH2 receptor ligands for medicinal uses
    4.
    发明授权
    CRTH2 receptor ligands for medicinal uses 失效
    用于药用的CRTH2受体配体

    公开(公告)号：US08022063B2

    公开(公告)日：2011-09-20

    申请号：US11597873

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Øystein Rist ,  Evi Kostenis ,  Thomas Högberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Øystein Rist ,  Evi Kostenis ,  Thomas Högberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A01N43/00 ,  C07D231/00

    CPC分类号： A61K31/415 ,  A61K31/454 ,  C07D231/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/34

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，Ar 3各自独立地表示苯基或5-或6-元单环杂芳基环，或由5-或6-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。

    CRTH2 Receptor Ligands For Therapeutic Use
    5.
    发明申请
    CRTH2 Receptor Ligands For Therapeutic Use 审中-公开
    CRTH2受体配体用于治疗用途

    公开(公告)号：US20090105218A1

    公开(公告)日：2009-04-23

    申请号：US11597938

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    IPC分类号： A61K31/196 ,  A61K31/44 ,  A61K31/381 ,  A61K31/341 ,  A61K31/5375 ,  A61K31/445 ,  A61K31/55 ,  A61P17/00 ,  A61P25/00 ,  A61P1/00 ,  A61P11/00

    CPC分类号： A61K31/245 ,  A61K31/196 ,  A61K31/341 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/63 ,  A61K31/635

    摘要： Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH═CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are not in ortho relationship; ring B is as defined for Ar2, or an optionally substituted cycloalkyl, N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; and s is 0 or 1.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，其中：A表示羧基-COOH或羧基生物电子等排体; L 1是键，-CH 2 - ， - OCH 2 - ， - CH 2 CH 2 - 或-CH-CH-; L2是CONH，-NHCO-，SO2NR1，-NR1SO2，其中R1是氢或C1-C3烷基，或式（X）或（Y）的二价基团，其中环Q是非芳族杂环， 7个环原子，包括所示的氮; L3是描述中定义的式 - （Alk1）m-（Z）n-（Alk2）p的二价连接基团; 环Ar1是任选取代的二价苯基或二价5-或6-元单环杂芳基，其中L1和H [B] sL3L2Ar2CONH-基团与相邻的环碳原子连接; 环Ar2是任选取代的1,3-亚苯基或任选取代的二价5-或6-元单环杂芳基，其中AL1Ar1NHCO-基和H [B] sL3L2-自由基与环碳原子连接， 不在邻近关系; 环B如Ar 2所定义，或任选取代的环烷基，N-吡咯烷基，N-哌啶基或N-氮杂环基; s为0或1。

    Novel promiscuous G alpha protein mutants and their use
    9.
    发明申请
    Novel promiscuous G alpha protein mutants and their use 审中-公开
    新型混杂的Gα蛋白突变体及其用途

    公开(公告)号：US20050042720A1

    公开(公告)日：2005-02-24

    申请号：US10830716

    申请日：2004-04-24

    申请人： Evi Kostenis

    发明人： Evi Kostenis

    IPC分类号： C07H21/04 ,  C07K14/47 ,  G01N33/566 ,  C07K14/705 ,  C12N9/48

    CPC分类号： C07H21/04 ,  C07K14/4722 ,  G01N33/566 ,  G01N2333/726 ,  G01N2500/00

    摘要： The present invention provides q-type G proteins, and nucleic acids encoding q-type G proteins, with one or more mutations in the linker I and/or linker II region, which render the proteins responsive to one or more non-q type G protein coupled receptors. The invention further relates to methods of identifying modulators of a G-protein coupled receptor.

    摘要翻译： 本发明提供了q型G蛋白和编码q型G蛋白的核酸，其在接头I和/或接头II区中具有一个或多个突变，其使蛋白质响应于一种或多种非q型G 蛋白偶联受体。 本发明还涉及鉴定G蛋白偶联受体的调节剂的方法。