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2. 发明公开

EP2632448A4 CIS 3,4-DIHYDROXY-2-(3-METHYLBUTANOYL)-5-(-3-METHYLBUTYL)-4-(4-METHYLPENTANOYL)CYCLOPENT-2-EN-1-ONE DERIVATIVES, SUBSTANTIALLY ENANTIOMERICALLY PURE COMPOSITIONS AND METHODS 审中-公开
标题翻译：顺式-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基 - ） - 4-（4- METHYLPENTANOYL-）环戊-2-烯-1-酮衍生物，基本上对映体纯的组合物和方法 ENSURE
公开(公告)号：EP2632448A4
公开(公告)日：2014-03-19
申请号：EP11837235
申请日：2011-10-28
申请人： KINDEX THERAPEUTICS LLC , CARROLL BRIAN , DARLAND GARY , DESAI ANURADHA , KONDA VEERA , DAHLBERG CLINTON J , URBAN JAN
发明人： CARROLL BRIAN , DARLAND GARY , DESAI ANURADHA , KONDA VEERA , DAHLBERG CLINTON J , URBAN JAN
IPC分类号： A61K31/122
CPC分类号： A61K31/122 , C07B2200/13 , C07C49/707
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.

3. 发明公开

EP2632448A1 CIS 3,4-DIHYDROXY-2-(3-METHYLBUTANOYL)-5-(-3-METHYLBUTYL)-4-(4-METHYLPENTANOYL)CYCLOPENT-2-EN-1-ONE DERIVATIVES, SUBSTANTIALLY ENANTIOMERICALLY PURE COMPOSITIONS AND METHODS 审中-公开
标题翻译：顺式-3,4-二羟基-2-（3-甲基丁酰基）-5-（3-甲基丁基 - ） - 4-（4- METHYLPENTANOYL-）环戊-2-烯-1-酮衍生物，基本上对映体纯的组合物和方法 ENSURE
公开(公告)号：EP2632448A1
公开(公告)日：2013-09-04
申请号：EP11837235.8
申请日：2011-10-28
申请人： KinDex Therapeutics, LLC , Carroll, Brian , Darland, Gary , Desai, Anuradha , Konda, Veera , Dahlberg, Clinton J. , Urban, Jan
发明人： CARROLL, Brian , DARLAND, Gary , DESAI, Anuradha , KONDA, Veera , DAHLBERG, Clinton, J. , URBAN, Jan
IPC分类号： A61K31/122
摘要： The present application provides cis 3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one derivatives and substantially enantiomerically pure compositions thereof. These derivatives include (+)-(4S,5R)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, (−)-(4R,5S)-3,4-dihydroxy-2-(3-methylbutanoyl)-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopent-2-en-1-one, and salts and crystals thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, activate GPR120, inhibit inflammation, and treat conditions responsive to PPARγ modulation, conditions responsive to GPR120 modulation, and metabolic disturbances such as diabetes.

4. 发明申请

WO2011072775A1 STECKVERBINDUNG ZWISCHEN EINEM WISCHBLATT UND EINEM WISCHARM 审中-公开
标题翻译：一个WISCHBLATT和刮水臂杆连接器
公开(公告)号：WO2011072775A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/006754
申请日：2010-11-05
申请人： DAIMLER AG , ERNEY, Thomas , FITTERER, Holger , MITTLER, Alexander , SCHLAGETER, Rainer , SCHULZE, Michael , URBAN, Jan
发明人： ERNEY, Thomas , FITTERER, Holger , MITTLER, Alexander , SCHLAGETER, Rainer , SCHULZE, Michael , URBAN, Jan
IPC分类号： B60S1/04 , B60S1/38
CPC分类号： B60S1/0425 , B60S1/3849
摘要： Die Erfindung betrifft eine Steckverbindung (24) zwischen einem Wischblatt (26) und einem Wischarm (10) einer Wischvorrichtung für eine Scheibe eines Fahrzeugs. Ein von dem Wischarm (10) seitlich abstehender Bolzen (12) ist in eine Buchse (28) einführbar, wobei der Bolzen (12) eine sich in Richtung seiner Mittelachse (M) erstreckende Ausnehmung (16) aufweist. Entlang der Ausnehmung (16) ist beim Aufstecken der Buchse (28) auf den Bolzen (12) eine sich in radialer Richtung erstreckende, an einer Innenwandung der Buchse (28) angeordnete Erhebung (30) führbar. Die Ausnehmung (16) weist einen Erweiterungsbereich (20) auf, in welchen die Erhebung (30) durch ein Verdrehen des Bolzens (12) und der Buchse (28) gegenüber einander verbringbar ist. In dem Erweiterungsbereich (20) ist zwischen dem Bolzen (12) und der Buchse (28) ein das Verdrehen begrenzender Anschlag (22) ausgebildet. Dadurch ist eine Verriegelungsposition der Buchse (28) genau definiert.
摘要翻译：本发明涉及一种刮水片（26）和一刮水器装置的用于车辆的风挡玻璃刮水臂（10）之间的插塞连接（24）。一刮水器臂（10）横向突出的螺栓（12）插入到衬套（28），其特征在于，所述螺栓（12）具有一个在其中心轴线（M）延伸的凹部（16）的方向的。沿着凹部（16）嵌合在螺栓上的套筒（28）（12）当布置在所述插座（28）投影（30）出来的内壁在径向方向上延伸。所述凹部（16）具有延伸区（20），其中，所述高度（30）通过转动螺栓（12）和所述衬套（28）彼此相对，可以提出。在膨胀区（20）包括在所述螺栓（12）和所述套筒（28）之间形成的止挡限制的旋转（22）。其特征在于所述套筒（28）的一锁定位置被精确限定。

5. 发明申请

WO2008021388A1 HETEROARYL DERIVATIVES AS CYTOKINE INHIBITORS 审中-公开
标题翻译：异氟烷衍生物作为细胞因子抑制剂
公开(公告)号：WO2008021388A1
公开(公告)日：2008-02-21
申请号：PCT/US2007/018049
申请日：2007-08-16
申请人： KEMIA, INC. , BOMAN, Erik , ERNST, Justin , MONTALBAN, Antonio, Garrido , LARSON, Christopher , LUM, Christopher , PEI, Yazhong , SEBO, Lubomir , URBAN, Jan , WANG, Zhijun , ZHU, Jay
发明人： BOMAN, Erik , ERNST, Justin , MONTALBAN, Antonio, Garrido , LARSON, Christopher , LUM, Christopher , PEI, Yazhong , SEBO, Lubomir , URBAN, Jan , WANG, Zhijun , ZHU, Jay
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/89 , C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/08 , C07D491/08 , C07D491/18
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines. In particular, compounds of the invention are useful as anti-inflammatory, anti-pain or anti-cancer agents.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。进一步提供了制备这些试剂及其在预防或治疗由细胞因子介导的病症中的用途的方法。特别地，本发明的化合物可用作抗炎，抗疼痛或抗癌剂。

6. 发明申请

WO2014011680A3 TETRAHYDRO-ISOHUMULONE DERIVATIVES, METHODS OF MAKING AND USING 审中-公开
标题翻译：四氢异冰片衍生物，制备和使用方法
公开(公告)号：WO2014011680A3
公开(公告)日：2014-03-20
申请号：PCT/US2013049788
申请日：2013-07-09
申请人： KONDA VEERA , URBAN JAN , DESAI ANURADHA , DAHLBERG CLINTON J
发明人： KONDA VEERA , URBAN JAN , DESAI ANURADHA , DAHLBERG CLINTON J
IPC分类号： C07C49/743
CPC分类号： C07C225/14 , A61K31/122 , A61K31/135 , C07C49/707 , C07C49/743 , C07C59/90 , C07C69/02 , C07C69/22 , C07C69/28 , C07C69/612 , C07C69/614 , C07C69/78 , C07C69/96 , C07C251/42 , C07C2601/08 , C07C2601/10
摘要： The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARy, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARy modulation such as diabetes.
摘要翻译：本申请提供新的四氢异葎草酮（THIAA）衍生物和基本上对映体纯的组合物及其药物制剂。本申请还提供了使用所公开的化合物和组合物活化PPARγ，抑制炎症和治疗与炎症反应的病症和对PPARγ调节如糖尿病有反应的病症的方法。

7. 发明申请

WO2006091737A1 MODULATORS OF GSK-3 ACTIVITY 审中-公开
标题翻译： GSK-3活性调节剂
公开(公告)号：WO2006091737A1
公开(公告)日：2006-08-31
申请号：PCT/US2006/006447
申请日：2006-02-23
申请人： KEMIA, INC. , SEBO, Lubomir , KAHL, Jeffrey , LUM, Christopher , PEI, Yazhong , PRYOR, Kent, E. , URBAN, Jan , JONES, Bryan , SULLIVAN, Robert
发明人： SEBO, Lubomir , KAHL, Jeffrey , LUM, Christopher , PEI, Yazhong , PRYOR, Kent, E. , URBAN, Jan , JONES, Bryan , SULLIVAN, Robert
IPC分类号： C07D239/48 , A61K31/505 , C07D487/04
CPC分类号： C07D239/48 , C07D487/04
摘要： In various aspects, the present invention relates to novel compounds, which modulate GSK-3 activity; to processes for the preparation of such compounds; and to compositions including such compounds. Compounds of the invention are useful as GSK-3 modulators and in the treatment of CNS diseases, such as Alzheimer's disease and mood disorders, and metabolic diseases, such as insulin requiring states.
摘要翻译：在各个方面，本发明涉及调节GSK-3活性的新化合物; 制备这些化合物的方法; 和包括这些化合物的组合物。本发明的化合物可用作GSK-3调节剂并用于治疗诸如阿尔茨海默氏病和情绪障碍的CNS疾病，以及诸如需要胰岛素的代谢疾病。

8. 发明申请

WO2002092010A2 REVERSE-TURN MIMETICS AND METHODS RELATING THERETO 审中-公开
标题翻译：反向转换MIME和与之相关的方法
公开(公告)号：WO2002092010A2
公开(公告)日：2002-11-21
申请号：PCT/US2002/015679
申请日：2002-05-16
申请人： MOLECUMETICS, LTD. , URBAN, Jan , NAKANISHI, Hiroshi , LEE, Min, S.,
发明人： URBAN, Jan , NAKANISHI, Hiroshi , LEE, Min, S.,
IPC分类号： A61K
CPC分类号： C07D487/04 , C07D487/14
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

9. 发明申请

WO2014011680A2 TETRAHYDRO-ISOHUMULONE DERIVATIVES, METHODS OF MAKING AND USING 审中-公开
标题翻译：四氢 - 异构体衍生物，制备和使用方法
公开(公告)号：WO2014011680A2
公开(公告)日：2014-01-16
申请号：PCT/US2013/049788
申请日：2013-07-09
申请人： KONDA, Veera , URBAN, Jan , DESAI, Anuradha , DAHLBERG, Clinton J.
发明人： KONDA, Veera , URBAN, Jan , DESAI, Anuradha , DAHLBERG, Clinton J.
IPC分类号： A61K31/122
CPC分类号： C07C225/14 , A61K31/122 , A61K31/135 , C07C49/707 , C07C49/743 , C07C59/90 , C07C69/02 , C07C69/22 , C07C69/28 , C07C69/612 , C07C69/614 , C07C69/78 , C07C69/96 , C07C251/42 , C07C2601/08 , C07C2601/10
摘要： The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARy, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARy modulation such as diabetes.
摘要翻译：本申请提供了新颖的四氢 - 异h草酮（THIAA）衍生物和基本上对映体纯的组合物及其药物制剂。本申请还提供了使用所公开的化合物和组合物来活化PPARγ，抑制炎症和治疗与炎症相关的病症和响应于PPARγ调节（例如糖尿病）的病症的方法。

10. 发明申请

WO2008089034A2 CYTOKINE INHIBITORS 审中-公开
标题翻译：细胞因子抑制剂
公开(公告)号：WO2008089034A2
公开(公告)日：2008-07-24
申请号：PCT/US2008/050723
申请日：2008-01-10
申请人： KEMIA, INC. , GARRIDO MONTALBAN, Antonio , DAHL, Russell , BOMAN, Erik , ERNST, Justin , LUM, Christopher , WANG, Zhijun , URBAN, Jan , PEI, Yazhong
发明人： GARRIDO MONTALBAN, Antonio , DAHL, Russell , BOMAN, Erik , ERNST, Justin , LUM, Christopher , WANG, Zhijun , URBAN, Jan , PEI, Yazhong
IPC分类号： A61K31/551
CPC分类号： C07D295/088 , C07C1/26 , C07C17/10 , C07C255/60 , C07C2529/40 , C07D207/09 , C07D207/14 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/56 , C07D213/64 , C07D213/74 , C07D233/61 , C07D239/48 , C07D243/08 , C07D249/06 , C07D257/04 , C07D263/32 , C07D265/30 , C07D295/13 , C07D295/192 , C07D295/24 , C07D295/26 , C07D307/52 , C07D401/04 , C07D401/12 , C07D403/04 , C07D413/12 , C07D487/08 , C07D491/08 , C07D498/08 , C07C9/00 , C07C19/075
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines, such as for example arthritis, pain, cardiovascular disease and cancer.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。特别地，本发明的化合物可用作抗炎剂。还提供了用于制备这些试剂的方法及其在预防或治疗由细胞因子（例如关节炎，疼痛，心血管疾病和癌症）介导的病症中的用途。

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