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11. 发明授权

EP2480077B1 PYRROLIDINES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权转让
标题翻译：吡咯烷ALS胰高血糖素受体拮抗剂，其组合物及使用方法
公开(公告)号：EP2480077B1
公开(公告)日：2015-02-18
申请号：EP10819272.5
申请日：2010-09-16
申请人： Merck Sharp & Dohme Corp.
发明人： GILBERT, Eric, J. , MILLER, Michael, W. , DEMONG, Duane Eugene , STAMFORD, Andrew, W. , GREENLEE, William, J.
IPC分类号： A01N43/36 , A61K31/40 , C07D207/09 , C07D207/50
CPC分类号： A61K31/40 , C07D207/08 , C07D207/09 , C07D207/48 , C07D207/50

12. 发明公开

EP2825522A1 RUTHENIUM-BASED METATHESIS CATALYSTS AND PRECURSORS FOR THEIR PREPARATION 审中-公开
标题翻译：钌基METHYESIS催化剂及其制备前体
公开(公告)号：EP2825522A1
公开(公告)日：2015-01-21
申请号：EP13716968.6
申请日：2013-03-13
申请人： Umicore AG & Co. KG
发明人： PLENIO, Herbert , PEECK, Lars
IPC分类号： C07C211/55 , C07F15/00 , C08G61/08 , C07C211/57
CPC分类号： C07F15/0046 , B01J31/181 , B01J31/2265 , B01J31/2295 , B01J2231/543 , B01J2531/821 , C07C67/30 , C07C67/333 , C07C211/54 , C07C211/55 , C07C2601/10 , C07D207/20 , C07D207/48 , C08G61/08 , C08G2261/418 , C08G2261/419 , C07C69/74
摘要： The invention is directed to ruthenium-based metathesis catalysts of the Hoveyda-Grubbs type. The new N -chelating diarylamino-based ruthenium catalysts described herein are stable in solid state and in solution and reveal rapid initiation behavior. Further, the corresponding N -substituted styrene precursor compounds are disclosed. The catalysts are prepared in a cross-metathesis reaction starting from N -substituted styrene precursors. The new Hoveyda-Grubbs type catalysts are suitable to catalyze ring-closing metathesis (RCM), cross metathesis (CM) and ring-opening metathesis polymerization (ROMP). Low catalyst loadings are sufficient to convert a wide range of substrates via metathesis reactions.
摘要翻译：本发明涉及Hoveyda-Grubbs型钌基复分解催化剂。本文所述的新型N-螯合二芳基氨基钌催化剂在固态和溶液中稳定并且显示快速起始行为。此外，公开了相应的N-取代的苯乙烯前体化合物。催化剂以N-取代的苯乙烯前体开始的交叉复分解反应制备。新型Hoveyda-Grubbs型催化剂适用于催化闭环复分解（RCM），交叉复分解（CM）和开环复分解聚合（ROMP）。低催化剂负载量足以通过复分解反应转化宽范围的底物。

13. 发明授权

EP2356092B1 BIOSYNTHETICALLY GENERATED PYRROLINE-CARBOXY-LYSINE AND SITE SPECIFIC PROTEIN MODIFICATIONS VIA CHEMICAL DERIVATIZATION OF PYRROLINE-CARBOXY-LYSINE AND PYRROLYSINE RESIDUES 有权
标题翻译：生物合成生产PYRROLINCARBOXYLYSIN和提供特定的蛋白质修饰TO化学衍生PYRROLINCARBOXYLYSIN-和PYRROLYSINRESTEN的
公开(公告)号：EP2356092B1
公开(公告)日：2014-04-16
申请号：EP09744017.6
申请日：2009-10-23
申请人： IRM LLC
发明人： GEIERSTANGER, Bernhard , OU, Weijia , CELLITTI, Susan, E. , UNO, Tetsuo , CROSSGROVE, Tiffany , CHIU, Hsien-Po , GRUNEWALD, Jan , HAO, Xueshi
IPC分类号： C07D207/20 , C07D209/00 , C07K2/00 , C12P13/04 , C12P21/00 , C07K1/107 , C07K1/13
CPC分类号： C12P21/00 , C07D207/20 , C07D207/48 , C07K5/0215

14. 发明公开

EP2678680A2 SMALL MOLECULES FOR ENDOTHELIAL CELL ACTIVATION 审中-公开
标题翻译：用于内皮细胞活化的小分子
公开(公告)号：EP2678680A2
公开(公告)日：2014-01-01
申请号：EP12749763.4
申请日：2012-02-23
申请人： The Regents of the University of California
发明人： CRUZ, Daniel , KWON, Ohyun
IPC分类号： G01N33/50 , G01N33/15 , C12Q1/02
CPC分类号： G01N33/5044 , C07D207/48 , C07D471/04 , C07D487/04 , G01N33/5047 , G01N33/5064
摘要： The present invention provides small molecules for endothelial cell activation and compositions thereof and methods of making and using the same.
摘要翻译：本发明提供了用于内皮细胞活化的小分子及其组合物及其制备和使用方法。

15. 发明公开

EP2639219A1 Ruthenium-based metathesis catalysts and precursors for their preparation 有权
标题翻译： Rutheniumbasierende复分解催化剂和前体生产
公开(公告)号：EP2639219A1
公开(公告)日：2013-09-18
申请号：EP12159506.0
申请日：2012-03-14
申请人： Umicore AG & Co. KG
发明人： Plenio, Herbert , Peeck, Lars
IPC分类号： C07C211/55 , C07F15/00 , C08G61/08
CPC分类号： C07F15/0046 , B01J31/181 , B01J31/2265 , B01J31/2295 , B01J2231/543 , B01J2531/821 , C07C67/30 , C07C67/333 , C07C211/54 , C07C211/55 , C07C2601/10 , C07D207/20 , C07D207/48 , C08G61/08 , C08G2261/418 , C08G2261/419 , C07C69/74
摘要： The invention is directed to ruthenium-based metathesis catalysts of the Hoveyda-Grubbs type. The new N -chelating diarylamino-based ruthenium catalysts described herein are stable in solid state and in solution and reveal rapid initiation behavior. Further, the corresponding N -substituted styrene precursor compounds are disclosed. The catalysts are prepared in a cross-metathesis reaction starting from N -substituted styrene precursors. The new Hoveyda-Grubbs type catalysts are suitable to catalyze ring-closing metathesis (RCM), cross metathesis (CM) and ring-opening metathesis polymerization (ROMP). Low catalyst loadings are sufficient to convert a wide range of substrates via metathesis reactions.

16. 发明公开

EP2490529A1 MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开
标题翻译：变构增效剂mGluR4，组成和方法用于治疗神经机能障碍
公开(公告)号：EP2490529A1
公开(公告)日：2012-08-29
申请号：EP10825779.1
申请日：2010-10-22
申请人： Vanderbilt University
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , NISWENDER, Colleen, M. , GOGLIOTTI, Rocco, D. , SALOVICH, James, M.
IPC分类号： A01N41/10
CPC分类号： A61K45/06 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/538 , C07D207/48 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12
摘要： Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

17. 发明授权

EP1489106B1 ARENE-RUTHENIUM COMPLEXES IMMOBILIZED ON POLYMERS, CATALYSTS CONSISTING OF THE COMPLEXES, AND PROCESSES FOR ORGANIC SYNTHESES WITH THE SAME 有权
标题翻译： ON聚合物固AREN - 钌络合物，催化剂用于有机合成，以便这些复杂和方法
公开(公告)号：EP1489106B1
公开(公告)日：2012-05-09
申请号：EP03710299.3
申请日：2003-03-11
申请人： Japan Science and Technology Agency
发明人： KOBAYASHI, Shu
IPC分类号： B01J31/06
CPC分类号： C08F8/42 , B01J31/1658 , B01J31/2295 , B01J31/24 , B01J2231/324 , B01J2231/543 , B01J2231/643 , B01J2531/821 , C07B2200/11 , C07C29/143 , C07C67/333 , C07C2601/10 , C07D207/48 , C07D211/96 , C07D225/02 , C07D307/28 , C07D307/92 , C07F15/0046 , C07F15/0053 , C07C69/74 , C07C33/22
摘要： Novel arene-ruthenium complexes immobilized on polymers as represented by the following formula: [wherein A is an organic polymer whose aromatic rings on the side chains coordinate to Ru; X1 and X2 are each independently halogeno; and R is an optionally substituted hydrocarbon group], which can be prepared by a simple process and are stable, easy of recovery, and applicable to various organic syntheses by virtue of their high catalytic activities; catalysts consisting of the complexes; and novel processes for organic syntheses including ring-opening metatheses of olefins and reduction of carbonyl by the use of the catalysts.

18. 发明授权

EP2081890B1 ARYLSULFONYL PYRROLIDINES AS 5-HT6 INHIBITORS 有权
标题翻译：芳基磺酰基吡咯烷作为5-HT6抑制剂
公开(公告)号：EP2081890B1
公开(公告)日：2011-01-12
申请号：EP07847099.4
申请日：2007-11-02
申请人： F. Hoffmann-La Roche AG
发明人： LOPEZ-TAPIA, Francisco Javier , LOWRIE, Jr., Lee Edwin , NITZAN, Dov
IPC分类号： C07D207/08 , C07D207/09 , C07D403/12 , A61K31/40 , A61K31/404 , A61K31/416 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , C07D207/36 , C07D207/48
CPC分类号： C07D207/36 , C07D207/08 , C07D207/48 , C07D403/12
摘要： This invention relates to substituted pyrrolidine compounds of the formula I wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.
摘要翻译：本发明涉及式I的取代的吡咯烷化合物，其中m，n，Ar，R1和R2如本文所定义。公开了制备该化合物和使用该化合物的方法。

19. 发明授权

EP1506169B1 VERFAHREN ZUR HERSTELLUNG VON SULFONSÄUREDIAMIDEN 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VONSULFONSÄUREDIAMIDEN
公开(公告)号：EP1506169B1
公开(公告)日：2009-12-23
申请号：EP03730050.6
申请日：2003-05-15
申请人： BASF SE
发明人： HAMPRECHT, Gerhard , PUHL, Michael , REINHARD, Robert , SAGASSER, Ingo , SCHMIDT, Thomas , GÖTZ, Norbert , ZIERKE, Thomas
IPC分类号： C07C307/02 , C07C303/34
CPC分类号： C07D295/26 , C07C303/34 , C07C307/00 , C07C2601/14 , C07D207/48 , C07D211/96 , C07D239/46
摘要： The invention relates to a method for the production of sulphamic acid halogenides of primary or secondary amines, comprising the following steps: i) reaction of a primary or secondary amine A1 with at least equimolar amounts of SO3 or an S03 source in the presence of at least equimolar amounts of a tertiary amine A2, respectively in relation to amine A1, and ii) reaction of the reaction mixture obtained in step i) with at least the stochiometrically required amount of phosphorus halogenide. The invention also relates to a method for the production of sulphamic acid diamides, comprising the production of sulphamic acid halogenides by carrying out steps i) and ii) and by subsequently reacting the sulphamic acid halogenides thus obtained with ammonia.The invention further relates to the use of said method in the production of herbicidal active ingredients with a sulphodiamide structure. The invention also relates to novel sulphamic acid chlorides.
摘要翻译：本发明涉及生产伯胺或仲胺的氨基磺酰氯的方法，其包括以下步骤：i）伯或仲胺A1与至少等摩尔量的SO 3或SO 3源在分别相对于胺A1为最少等摩尔量的叔胺A2，和ii）使步骤i）中获得的反应混合物与至少化学计量需要量的卤化磷反应。本发明还涉及生产氨基磺酸二酰胺的方法，该方法包括通过进行步骤i）和ii）产生氨基磺酰卤，并随后使由此获得的氨基磺酸酰卤与氨反应。本发明进一步涉及所述方法在制备具有磺基二酰胺结构的除草活性成分中的用途。本发明还涉及新型氨基磺酰氯。

20. 发明公开

EP2081890A1 ARYLSULFONYL PYRROLIDINES AS 5-HT6 INHIBITORS 有权
标题翻译： ARYLSULFONYLPYRROLIDINE AS 5-HT 6抑制剂
公开(公告)号：EP2081890A1
公开(公告)日：2009-07-29
申请号：EP07847099.4
申请日：2007-11-02
申请人： F. Hoffmann-La Roche AG
发明人： LOPEZ-TAPIA, Francisco Javier , LOWRIE, Jr., Lee Edwin , NITZAN, Dov
IPC分类号： C07D207/08 , C07D207/09 , C07D403/12 , A61K31/40 , A61K31/404 , A61K31/416 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , C07D207/36 , C07D207/48
CPC分类号： C07D207/36 , C07D207/08 , C07D207/48 , C07D403/12
摘要： This invention relates to substituted pyrrolidine compounds of the formula I wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.

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