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1. 发明授权

US07888020B2 Association of EDG5 polymorphism V286A with type II diabetes mellitus and venous thrombosis/pulmonary embolism and the use thereof 失效
标题翻译： EDG5多态性V286A与II型糖尿病和静脉血栓形成/肺栓塞的关系及其用途
公开(公告)号：US07888020B2
公开(公告)日：2011-02-15
申请号：US11834998
申请日：2007-08-07
申请人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Sylvain Ricard , Sandrine Mace , Jean-Francois Deleuze
发明人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Sylvain Ricard , Sandrine Mace , Jean-Francois Deleuze
IPC分类号： C12Q1/68 , C12P19/34 , C07H21/04
CPC分类号： C12Q1/6883 , C12Q2600/156
摘要： The present invention relates to a method of identifying an increase in risk for type II Diabetes mellitus, venous thrombosis, or pulmonary embolism in a subject, wherein the presence of an amino acid exchange at position 286 from valine (Val) to alanine (Ala) in the EDG5 protein in a biological sample taken from the subject.
摘要翻译：本发明涉及鉴定受试者中II型糖尿病，静脉血栓形成或肺栓塞风险增加的方法，其中286位从缬氨酸（Val）到丙氨酸（Ala）的氨基酸交换的存在在取自受试者的生物样品中的EDG5蛋白中。

2. 发明授权

US08198022B2 Association of EDG5 polymorphism V286A with type II diabetes mellitus and venous thrombosis/pulmonary embolism and the use thereof 失效
标题翻译： EDG5多态性V286A与II型糖尿病和静脉血栓形成/肺栓塞的关系及其用途
公开(公告)号：US08198022B2
公开(公告)日：2012-06-12
申请号：US13006619
申请日：2011-01-14
申请人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Sylvain Ricard , Sandrine Mace , Jean-Francois Deleuze
发明人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Sylvain Ricard , Sandrine Mace , Jean-Francois Deleuze
IPC分类号： C12Q1/68 , C12Q1/70 , C07H21/04
CPC分类号： C12Q1/6883 , C12Q2600/156
摘要： The present invention relates to a method of identifying an increase in risk for type II Diabetes mellitus, venous thrombosis, or pulmonary embolism in a subject, wherein the presence of an amino acid exchange at position 286 from valine (Val) to alanine (Ala) in the EDG5 protein in a biological sample taken from the subject.
摘要翻译：本发明涉及鉴定受试者中II型糖尿病，静脉血栓形成或肺栓塞风险增加的方法，其中286位从缬氨酸（Val）到丙氨酸（Ala）的氨基酸交换的存在在取自受试者的生物样品中的EDG5蛋白中。

3. 发明申请

US20110104704A1 ASSOCIATION OF EDG5 POLYMORPHISM V286A WITH TYPE II DIABETES MELLITUS AND VENOUS THROMBOSIS/PULMONARY EMBOLISM AND THE USE THEREOF 失效
标题翻译： EDG5多态性V286A与II型糖尿病和静脉血栓形成/肺动脉栓塞的联合及其使用
公开(公告)号：US20110104704A1
公开(公告)日：2011-05-05
申请号：US13006619
申请日：2011-01-14
申请人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
发明人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/156
摘要： The present invention relates to a method of identifying an increase in risk for type II Diabetes mellitus, venous thrombosis, or pulmonary embolism in a subject, wherein the presence of an amino acid exchange at position 286 from valine (Val) to alanine (Ala) in the EDG5 protein in a biological sample taken from the subject.
摘要翻译：本发明涉及鉴定受试者中II型糖尿病，静脉血栓形成或肺栓塞风险增加的方法，其中286位从缬氨酸（Val）到丙氨酸（Ala）的氨基酸交换的存在在取自受试者的生物样品中的EDG5蛋白中。

4. 发明授权

US07262273B2 Association of EDG5 polymorphism V286A with type II diabetes mellitus and venous thrombosis/pulmonary embolism and the use thereof 失效
标题翻译： EDG5多态性V286A与II型糖尿病和静脉血栓形成/肺栓塞的关系及其用途
公开(公告)号：US07262273B2
公开(公告)日：2007-08-28
申请号：US10393870
申请日：2003-03-21
申请人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
发明人： Detlef Kozian , Evi Kostenis , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
IPC分类号： C07K1/00 , G01N33/53
CPC分类号： C12Q1/6883 , C12Q2600/156
摘要： The present invention relates to a method of identifying an increase in risk for type II Diabetes mellitus, venous thrombosis, or pulmonary embolism in a subject, wherein the presence of an amino acid exchange at position 286 from valine (Val) to alanine (Ala) in the EDG5 protein in a biological sample taken from the subject.
摘要翻译：本发明涉及鉴定受试者中II型糖尿病，静脉血栓形成或肺栓塞风险增加的方法，其中286位从缬氨酸（Val）到丙氨酸（Ala）的氨基酸交换的存在在取自受试者的生物样品中的EDG5蛋白中。

5. 发明申请

US20070259378A1 METHOD FOR IDENTIFYING AGONISTS OR ANTAGONISTS OF THE G-PROTEIN COUPLED RECEPTOR MAS-LIKE 1 失效
标题翻译：鉴定G蛋白偶联受体MAS-1的激动剂或拮抗剂的方法1
公开(公告)号：US20070259378A1
公开(公告)日：2007-11-08
申请号：US11556216
申请日：2006-11-03
申请人： Evi Kostenis , Johann Gassenhuber
发明人： Evi Kostenis , Johann Gassenhuber
IPC分类号： G01N33/53
CPC分类号： G01N33/5041 , A61K38/046 , A61K38/08 , G01N33/5008 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2500/10
摘要： The invention relates to a method for identifying a compound which stimulates or attenuates the activity of the G protein-coupled receptor mas-like 1.
摘要翻译：本发明涉及鉴定刺激或减弱G蛋白偶联受体mas样1的活性的化合物的方法。

6. 发明申请

US20090105218A1 CRTH2 Receptor Ligands For Therapeutic Use 审中-公开
标题翻译： 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。

7. 发明申请

US20080119456A1 Substituted Thiazoleacetic Acid as Crth2 Ligands 审中-公开
标题翻译：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。

8. 发明授权

US08404436B1 Methods of identifying modulators of GPR17 有权
标题翻译：识别GPR17调节剂的方法
公开(公告)号：US08404436B1
公开(公告)日：2013-03-26
申请号：US13407512
申请日：2012-02-28
申请人： Evi Kostenis , Andreas Spinrath , Stephanie Hennen , Lucas Peters , Christa E. Muller , Rhalid Akkari , Younis Baqi , Kirsten Ritter
发明人： Evi Kostenis , Andreas Spinrath , Stephanie Hennen , Lucas Peters , Christa E. Muller , Rhalid Akkari , Younis Baqi , Kirsten Ritter
IPC分类号： C12Q1/00 , G01N33/53 , C07D209/04
CPC分类号： C07D209/42 , A61K31/405 , C07D405/04 , C07D409/04 , C07K14/723 , C12Q1/025 , G01N33/5041 , G01N33/566 , G01N33/6896 , G01N33/74 , G01N2333/4719 , G01N2500/00 , G01N2800/285 , G01N2800/2871
摘要： The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.
摘要翻译：本发明涉及测定化合物改变GPR17的生物学活性的能力的方法。所述方法尤其包括在合适量的式I的GPR17激动剂存在下使测试化合物与GPR17或功能性GPR17片段接触的步骤。

9. 发明授权

US07794927B2 Method for identifying agonists or antagonists of the G-protein coupled receptor mas-like 1 失效
标题翻译：用于鉴定G蛋白偶联受体mas样的激动剂或拮抗剂的方法1
公开(公告)号：US07794927B2
公开(公告)日：2010-09-14
申请号：US11556216
申请日：2006-11-03
申请人： Evi Kostenis , Johann Gassenhuber
发明人： Evi Kostenis , Johann Gassenhuber
IPC分类号： C12Q1/00 , C07K14/435
CPC分类号： G01N33/5041 , A61K38/046 , A61K38/08 , G01N33/5008 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2500/10
摘要： The invention relates to a method for identifying a compound which stimulates or attenuates the activity of the G protein-coupled receptor mas-like 1.
摘要翻译：本发明涉及鉴定刺激或减弱G蛋白偶联受体mas样1的活性的化合物的方法。

10. 发明申请

US20050042720A1 Novel promiscuous G alpha protein mutants and their use 审中-公开
标题翻译：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。

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