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1. 发明公开

EP3217968A4 SUBSTITUTED AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR TISSUE SELF-REPAIR AND REGENERATION 无效转让
公开(公告)号：EP3217968A4
公开(公告)日：2018-06-20
申请号：EP15859768
申请日：2015-11-12
申请人： PROMETIC PHARMA SMT LTD
发明人： GAGNON LYNE , LAURIN PIERRE
IPC分类号： A61K31/192 , A61K8/36 , A61P17/02 , A61P19/08 , A61Q19/08 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/52 , C07C59/84
CPC分类号： A61K31/192 , A61K8/36 , A61K8/365 , A61P17/02 , A61P19/08 , A61Q19/08 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/52 , C07C59/84
摘要： Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g. increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue, or cell, promoting wound healing as well as anti-aging applications. Corresponding compositions, methods and uses are also described. Formula I wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)-(CH2)n-CH3 wherein n is 3 or 4; R1 is H, F of OH; R2 is H, F, OH, C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)-(CH2)n-CH3 wherein n is 3 or 4; R3 is H, F, OH, or CH2Ph; R4 is H, F or OH; Q is 1) (CH2),C(0)OH wherein m is 1 or 2 2) CH(CH3)C(0)OH, 3) C(CH3)2C(0)OH, 4) CH(F)-C(0)OH, 5) CF2-C(0)OH or 6) C(0)-C(0)OH.

2. 发明授权

EP2414341B1 OXADIAZOLE DERIVATIVES 有权
公开(公告)号：EP2414341B1
公开(公告)日：2017-09-13
申请号：EP10711881.2
申请日：2010-03-29
申请人： Merck Serono SA
发明人： QUATTROPANI, Anna , MONTAGNE, Cyril , SAUER, Wolfgang , CROSIGNANI, Stefano , BOMBRUN, Agnès
IPC分类号： C07D271/06 , A61K31/4245 , A61P37/00
CPC分类号： A61K31/4245 , A61K31/192 , A61K31/197 , C07C57/30 , C07D271/06

3. 发明授权

EP1368295B1 PROCESS FOR THE MANUFACTURE OF PHENYLACETIC ACID DERIVATIVES 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON PHENYLESSIGSAEURE-DERIVATEN
公开(公告)号：EP1368295B1
公开(公告)日：2017-04-12
申请号：EP02735104.8
申请日：2002-02-07
申请人： F. Hoffmann-La Roche AG
发明人： HOFFMANN-EMERY, Fabienne , SCALONE, Michelangelo , SPURR, Paul
IPC分类号： C07C51/12 , C07C57/30
CPC分类号： C07D213/75 , C07C29/40 , C07C41/26 , C07C51/12 , C07D239/48 , C07C57/30 , C07C57/58 , C07C59/64 , C07C63/14 , C07C61/40 , C07C33/46 , C07C33/20 , C07C43/23

4. 发明授权

EP2054367B1 PROCESS FOR THE PREPARATION OF SODIUM SALT OF IBUPROFEN OF DIFFERENT PARTICLE SIZES 有权转让
标题翻译： VERFAHREN ZUR HERSTELLUNG VON IBUPROFEN-NATRIUMSALZ MIT VERSCHIEDENENPARTIKELGRÖSSEN
公开(公告)号：EP2054367B1
公开(公告)日：2017-03-22
申请号：EP07841187.3
申请日：2007-08-22
申请人： SI Group, Inc.
发明人： PHAN, Hao, V.
IPC分类号： C07C51/41 , C07C51/44 , C07C51/46 , C07C51/47 , C07C57/30
CPC分类号： C07C51/44 , C07C51/412 , C07C51/47 , Y10T428/2982 , C07C57/30
摘要： A free-flowing hydrated sodium salt of ibuprofen of controlled median particle size and water content is provided. It can be produced by adding aqueous NaOH to a non-boiling solution or slurry of ibuprofen in an organic solvent that can be distilled along with water at a temperature in the range of 50 to 120° C. The rate of NaOH addition is at a rate that does not cause the resultant reaction mixture to boil before the addition has been completed. After completing the addition, the water is removed with some of the organic solvent by distillation. After cooling, the hydrated sodium salt of ibuprofen is recovered from the resultant slurry. The process enables the median particle size of the sodium salt of ibuprofen formed to be controlled by selection and use of a predetermined effective concentration of NaOH in the aqueous NaOH solution used.
摘要翻译：提供了控制中值粒径和含水量的自由流动的布洛芬水合钠盐。可以通过向非沸腾溶液或布洛芬的浆液中加入NaOH水溶液来制备，所述有机溶剂可以在50至120℃的温度范围内与水一起蒸馏。加入NaOH的速率为在添加完成之前不会使所得反应混合物沸腾的速率。加完后，用一些有机溶剂通过蒸馏除去水分。冷却后，从所得浆料中回收布洛芬的水合钠盐。该方法可以通过在所用NaOH水溶液中选择和使用预定有效浓度的NaOH来控制形成的布洛芬钠盐的中值粒度。

5. 发明授权

EP1996329B1 A HIGH THROUGHPUT PROCESS FOR MANUFACTURING MOLECULAR SIEVES 有权
标题翻译： PRODUCING分子SEVEN高通量方法
公开(公告)号：EP1996329B1
公开(公告)日：2016-08-03
申请号：EP07749406.0
申请日：2007-01-29
申请人： ExxonMobil Chemical Patents Inc.
发明人： JOHNSON, Ivy, D. , LAI, Wenyih, Frank
IPC分类号： B01J37/10 , B01J29/06 , C01B39/02
CPC分类号： C07B37/04 , B01J20/3028 , B01J29/04 , B01J29/06 , B01J29/40 , B01J29/7023 , B01J29/7038 , B01J29/80 , B01J29/86 , C01B37/02 , C01B39/02 , C01B39/04 , C01B39/40 , C07C2/66 , C07C6/126 , C07C29/36 , C07C51/235 , C09B67/0073 , C09B67/0096 , C10G45/64 , Y02P20/52 , C07C15/02 , C07C15/107 , C07C15/085 , C07C57/30 , C07C33/20

6. 发明授权

EP1590314B1 2-ARYL-ACETIC ACIDS, THEIR DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
标题翻译： 2ARYLESSIGSÄUREVERBINDUNGEN，其衍生物和药物组合物
公开(公告)号：EP1590314B1
公开(公告)日：2015-08-05
申请号：EP04707926.4
申请日：2004-02-04
申请人： Dompé farmaceutici s.p.a.
发明人： MORICONI, Alessio , ALLEGRETTI, Marcello , BERTINI, Riccardo , CESTA, Maria, Candida , BIZZARRI, Cinzia , COLOTTA, Francesco
IPC分类号： C07D207/32 , C07D295/12 , C07D209/42 , C07C63/04 , A61P43/00
CPC分类号： C07D207/337 , C07C57/30 , C07C57/58 , C07C311/09 , C07C311/21 , C07C311/51 , C07D209/26 , C07D209/42 , C07D295/13 , C07D471/04

7. 发明公开

EP2251316A4 METHOD FOR PRODUCING OPTICALLY ACTIVE ESTER AND METHOD FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID 有权
标题翻译：工艺生产光学活性酯和方法生产光学活性羧酸
公开(公告)号：EP2251316A4
公开(公告)日：2015-04-22
申请号：EP09719934
申请日：2009-03-04
申请人： UNIV TOKYO SCI EDUC FOUND
发明人： SHIINA ISAMU , NAKATA KENYA
IPC分类号： C07C67/08 , C07B57/00 , C07C51/493 , C07C57/30 , C07C69/612
CPC分类号： C07C67/08 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C51/493 , C07C2603/26 , C07C59/68 , C07C59/84 , C07C57/30 , C07C59/64 , C07C57/58 , C07C69/736 , C07C69/612 , C07C69/65 , C07C69/738 , C07C69/734 , C07C69/616
摘要： Disclosed is a method for producing an optically active ester by highly selectively esterifying one enantiomer of a racemic carboxylic acid, while producing an optically active carboxylic acid which is the other enantiomer. An optically active ester is produced while producing an optically active carboxylic acid at the same time by reacting a racemic carboxylic acid with a specific alcohol or phenol derivative in the presence of benzoic anhydride or a derivative thereof and a catalyst such as tetramisole or benzotetramisole, thereby selectively esterifying one enantiomer of the racemic carboxylic acid.

8. 发明公开

EP2739610A1 PROCESS FOR THE MANUFACTURE OF IVABRADINE AND OF INTERMEDIATES OF SYNTHESIS THEREOF 失效
标题翻译：用于生产伊伐布雷定和中间体的合成
公开(公告)号：EP2739610A1
公开(公告)日：2014-06-11
申请号：EP12772396.3
申请日：2012-07-31
申请人： Laboratorio Chimico Internazionale S.p.A.
发明人： NARDI, Antonio , DE ANGELIS, Bruno , CEREA, Paolangelo , RAFECAS, Jane, Llorenc , TESSON, Nicolas
IPC分类号： C07D223/16 , C07C213/10
CPC分类号： C07D223/16 , C07C53/134 , C07C57/30 , C07C209/46 , C07C211/04 , C07C213/10 , C07C215/50 , C07C2602/06 , Y02P20/582
摘要： The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.

9. 发明公开

EP2737900A1 NDM INHIBITOR 审中-公开
标题翻译： NDM-抑制剂
公开(公告)号：EP2737900A1
公开(公告)日：2014-06-04
申请号：EP12817790.4
申请日：2012-07-26
申请人： Meiji Seika Pharma Co., Ltd.
发明人： MORINAKA, Akihiro , MAEBASHI, Kazunori , IDA, Takashi , HIKIDA, Muneo , YAMADA, Mototsugu , ABE, Takao
IPC分类号： A61K31/194 , A61K31/351 , A61K31/40 , A61K31/407 , A61K31/4164 , A61K31/4406 , A61K31/445 , A61K31/5375 , A61K45/00 , A61P31/04 , A61P43/00 , C07C57/26 , C07C57/48 , C07C59/46 , C07C217/22 , C07D309/06
CPC分类号： C07C69/593 , A61K31/194 , A61K31/216 , A61K31/225 , A61K31/351 , A61K31/40 , A61K31/4015 , A61K31/407 , A61K31/4164 , A61K31/4174 , A61K31/4406 , A61K31/45 , A61K31/5375 , A61K45/06 , C07C57/13 , C07C57/26 , C07C57/30 , C07C57/42 , C07C57/48 , C07C57/50 , C07C59/46 , C07C59/64 , C07C63/66 , C07C69/608 , C07C69/612 , C07C69/618 , C07C69/732 , C07C217/18 , C07C233/65 , C07C235/20 , C07C237/22 , C07C279/08 , C07D207/12 , C07D211/46 , C07D213/55 , C07D233/64 , C07D295/108 , C07D309/06 , Y02A50/473 , A61K2300/00
摘要： An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):

10. 发明公开

EP2562152A1 A METHOD FOR PREPARING 2,5-DIMETHYLPHENYLACETIC ACID 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON 2,5-DIMETHYLPHENYL-ESSIGSÄURE
公开(公告)号：EP2562152A1
公开(公告)日：2013-02-27
申请号：EP11860849.6
申请日：2011-06-07
申请人： Lianhe Chemical Technology Co., Ltd. , Jiangsu Lianhe Chemical Technology Co., Ltd
发明人： WANG, Ping , FAN, Xiaobin , LIN, Xingjun , HE, Zhaohui
IPC分类号： C07C51/10 , C07C57/30
CPC分类号： C07C51/10 , C07C17/32 , Y02P20/542 , C07C57/30 , C07C22/04
摘要： Provided is a method for preparing 2,5-dimethylphenylacetic acid, wherein p-xylene is mixed with paraformaldehyde and concentrated hydrochloric acid in a solvent of ion liquid to obtain 2,5-dimethyl benzyl chloride by the chloromethylation reaction. Then, 2,5-dimethyl benzyl chloride is introduced into a reactor with an acid binding agent and a solvent, the carbonylation and hydrolysis reaction is conducted in the presence of a catalyst to obtain 2,5-dimethylphenylacetic acid. The present process has new route, less synthesis steps, simple operation, lower cost, increased yield, and is friendly to the environment. Therefore, the method is suitable for industrial production.
摘要翻译：提供了制备2,5-二甲基苯乙酸的方法，其中对二甲苯与多聚甲醛和浓盐酸在离子液体的溶剂中混合，通过氯甲基化反应得到2,5-二甲基苄基氯。然后，用酸结合剂和溶剂将2,5-二甲基苄基氯引入反应器中，羰基化和水解反应在催化剂存在下进行，得到2,5-二甲基苯基乙酸。本工艺具有新途径，综合步骤少，操作简单，成本低廉，产量增加，环境友好。因此，该方法适用于工业生产。

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