ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE
    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

    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.

    INTERMEDIATE COMPOUND WHICH IS USED FOR THE PREPARATION OF PIOGLITAZONE
    2.
    发明授权
    INTERMEDIATE COMPOUND WHICH IS USED FOR THE PREPARATION OF PIOGLITAZONE 有权
    中间体吡格列酮生产

    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.

    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.

    SOLID FORMS OF AN N-(PHENYLMETHYL)PROPANAMIDE DERIVATIVE AND PROCESSES OF PREPARATION
    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。

    NEW FORM OF THE AMINOINDAN MESYLATE DERIVATIVE RASAGINLINE MESYLATE
    8.
    发明公开
    NEW FORM OF THE AMINOINDAN MESYLATE DERIVATIVE RASAGINLINE MESYLATE 审中-公开
    氨基甲酰胺衍生物RASAGILIN-MESYLAT

    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.

    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。

    INTERMEDIATE COMPOUND WHICH IS USED FOR THE PREPARATION OF PIOGLITAZONE
    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.

    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。