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1.发明公开ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE 审中-公开的外消旋酶拆分（2R，S）-2-（乙酰基氨基）-3-甲氧基-N-（苯基甲基）丙酰胺
公开(公告)号：EP2582833A1
公开(公告)日：2013-04-24
申请号：EP11736163.4
申请日：2011-06-15
申请人： Medichem, S.A.
IPC分类号： C12P13/02
CPC分类号： C12P41/006 , C12P13/02 , C12P41/007 , C12Y301/01003
摘要： The present invention is concerned with a process of preparing (R)-lacosamide. The process comprises providing an (R,S)-lacosamide precursor and contacting the same with at least an enzyme in the presence of a solvent. The enzyme either stereoselectively hydrolyzes or acetylates an (R)- or (S)-enantiomer of the (R,S)-lacosamide precursor. The process further comprises where appropriate also concurrently, or successively, employing one or more reagents capable of converting the hydrolysed or acetylated (R)- or (S)-enantiomer to (R)- lacosamide.
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公开(公告)号：EP1623977B1
公开(公告)日：2007-11-07
申请号：EP04731028.9
申请日：2004-05-04
申请人： Medichem, S.A.
发明人： DURAN LOPEZ, Ernesto
IPC分类号： C07D213/55 , C07D417/12
CPC分类号： C07D417/12
摘要： The invention relates to a compound having formula (IV), which is an intermediate compound that is used for the preparation of pioglitazone. The invention also relates to a method of obtaining the novel compound (IV) from a natural product, L-tyrosine, in which the amino group, in the form of an imino-aromatic group, is protected. The invention further relates to a method of obtaining pioglitazone from the aforementioned intermediate compound.
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3.发明公开A DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE WHICH IS FREE OF POTENTIAL GENOTOXICITY AND A PROCESS FOR REDUCING THE RESIDUAL AMOUNT OF P-CHLOROANILINE IN SAID DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE 审中-公开DI（4-氯 - phenyldiguanido）衍生物没有潜在遗传毒性和过程中尽量减少在这DI其余CONTENT P CHLORIDE苯胺（4-氯 - phenyldiguanido）衍生物
公开(公告)号：EP2501676A2
公开(公告)日：2012-09-26
申请号：EP10781885.8
申请日：2010-11-18
申请人： Medichem, S.A.
发明人： SANCHEZ SALGUERO, Laura , BOU BOSCH, Raquel , BOSCH I LLADÓ, Jordi , CAMACHO CARRASCO, Antonio , DURAN LOPEZ, Ernesto , ANDRES MAGNANI, Pablo
IPC分类号： C07C279/18 , C07C277/08 , C07C279/26
CPC分类号： C07C279/265 , C07C277/08
摘要： The invention relates to a process for reducing the residual amount of p-chloroaniline in chlorhexidine. Also, the invention relates to a process for preparing chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. In addition, the invention refers to the said chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. Further, the invention relates to an analytical HPLC method for the determination of potentially genotoxic impurities in samples of chlorhexidine, or of a pharmaceutically acceptable salt thereof. The invention also relates to stabilized chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution, and to a method for stabilizing chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution.
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4.发明授权
公开(公告)号：EP1885727B1
公开(公告)日：2010-03-03
申请号：EP06809025.7
申请日：2006-05-03
申请人： Medichem, S.A.
IPC分类号： C07D491/10
CPC分类号： C07D491/10
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5.发明公开
公开(公告)号：EP1885727A2
公开(公告)日：2008-02-13
申请号：EP06809025.7
申请日：2006-05-03
申请人： Medichem, S.A.
IPC分类号： C07D491/10
CPC分类号： C07D491/10
摘要： The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved to yield (-)-narwedine and which is the biogenic precursor of (-)- galanthamine) and the use thereof as a starting material for producing (-)-galanthamine. The invention further includes processes for preparing (-)-galanthamine and (-)-galanthamine hydrobromide, as well as related novel compounds.
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公开(公告)号：EP2536394A2
公开(公告)日：2012-12-26
申请号：EP11703719.2
申请日：2011-02-18
申请人： Medichem S.A.
CPC分类号： C07C271/28 , A61K31/27
摘要： The invention relates to retigabine with improved color quality, and to processes for preparing the same. In addition, the invention relates to a process for drying wet retigabine. Also, the invention relates to stabilized or substantially stabilized retigabine in solid state or pharmaceutical formulation comprising the same. Further, the invention also relates to an improved process for preparing retigabine.
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7.发明公开SOLID FORMS OF AN N-(PHENYLMETHYL)PROPANAMIDE DERIVATIVE AND PROCESSES OF PREPARATION 审中-公开FESTE FORMEN EINES N-（PHENYLMETHYL）Propanamid-DERIVATS UND HERSTELLUNGSVERFAHRENDAFÜR
公开(公告)号：EP2462107A1
公开(公告)日：2012-06-13
申请号：EP10755114.5
申请日：2010-08-05
申请人： Medichem, S.A.
IPC分类号： C07C237/22
CPC分类号： C07C237/22
摘要： Disclosed are solid Forms, and corresponding mixtures, of the anti-epileptic agent lacosamide (I). Also disclosed is a mixture of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)- enantiomer of lacosamide.
摘要翻译： 本发明涉及抗癫痫剂拉科酰胺（I）的固体形式。 本发明还涉及拉莫糖的固体形式的混合物。 本发明还涉及以聚集体形式结晶的lacosamide对映异构体的混合物及其在提供对映异构体富集的lacosamide，优选lacosamide的（R） - 对映异构体富集的lacosamide）中的用途。
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8.发明公开
公开(公告)号：EP2456750A2
公开(公告)日：2012-05-30
申请号：EP10754901.6
申请日：2010-07-20
申请人： Medichem, S.A.
IPC分类号： C07C211/42 , A61K31/135 , A61P25/16
CPC分类号： C07C211/42 , C07C2602/08
摘要： The invention relates to rasagiline mesylate with improved flowability and compressibility and with advantageously reduced stickiness, to processes for the preparation thereof, and to the use thereof for milling and for preparing pharmaceutical formulations. Also, the invention relates to a method for improving the flowability and / or alleviating the stickiness of rasagiline mesylate having a very poor flowability and / or showing undesirable stickiness.
摘要翻译： 本公开总体上涉及具有改善的流动性和有利地降低的粘性的甲磺酸雷沙吉兰，其制备方法及其用于研磨和用于制备药物制剂的用途。 还公开了改善具有非常差的流动性和/或显示不期望的粘性的甲磺酸雷沙吉兰的流动性和/或减轻粘性的方法。
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9.发明公开
公开(公告)号：EP2064205A2
公开(公告)日：2009-06-03
申请号：EP07825063.6
申请日：2007-09-07
申请人： Medichem, S.A.
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： A process for preparing substituted pyrrolidine compounds, including (5)-2-{l-[2- (2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst.
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10.发明公开INTERMEDIATE COMPOUND WHICH IS USED FOR THE PREPARATION OF PIOGLITAZONE 有权ZWISCHENPRODUKTFÜRDIE HERSTELLUNG VON PIOGLITAZON
公开(公告)号：EP1623977A1
公开(公告)日：2006-02-08
申请号：EP04731028.9
申请日：2004-05-04
申请人： Medichem, S.A.
发明人： DURAN LOPEZ, Ernesto
IPC分类号： C07D213/55 , C07D417/12 , A61K31/44 , A61P3/10
CPC分类号： C07D417/12
摘要： The present invention relates to a novel compound of formula (IV)
which is an intermediate that can be used for the preparation of pioglitazone. It also relates to a method of obtaining the novel compound (IV) starting from the natural product L-tyrosine, in which the amino group is protected in the form of aromatic imino group, and a method of obtaining pioglitazone from the said intermediate.摘要翻译： 本发明涉及一种新的式（Ⅳ）化合物，它是可用于制备吡格列酮的中间体。 它还涉及从天然产物L-酪氨酸开始获得新颖化合物（Ⅳ）的方法，其中氨基被保护为芳族亚氨基的形式，以及从所述中间体获得吡格列酮的方法。
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