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    SOLID FORMS OF LORCASERIN HYDROCHLORIDE
    2.
    发明公开
    SOLID FORMS OF LORCASERIN HYDROCHLORIDE 审中-公开
    FESTE FORMEN VON LORCASERINHYDROCHORIDE

    公开(公告)号：EP2924024A2

    公开(公告)日：2015-09-30

    申请号：EP15160102.8

    申请日：2015-03-20

    申请人： Medichem, S.A.

    发明人： Duran López, Ernesto ,  Benito Vélez, Mónica

    IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P3/04 ,  A61P25/30 ,  A61P25/24

    CPC分类号： C07D223/16

    摘要： The invention relates to lorcaserin hydrochloride, processes of preparing lorcaserin hydrochloride, mixtures comprising lorcaserin hydrochloride and at least one pharmaceutical excipient and pharmaceutical compositions and therapeutic uses thereof. The invention also relates to cocrystals comprising lorcaserin, processes of preparing thereof, and pharmaceutical compositions and therapeutic uses thereof.

    摘要翻译： 本发明涉及盐酸氯卡色林，盐酸氯卡色林的制备方法，盐酸氯卡色林和至少一种药物赋形剂和药物组合物及其治疗用途的混合物。 本发明还涉及包含氯卡色林的共晶体，其制备方法，以及药物组合物及其治疗用途。

    ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE
    4.
    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.

    发明人： BOSCH I LLADO, Jordi ,  DURAN LOPEZ, Ernesto

    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.

    PROCESS FOR PREPARING A 3-PYRROLE SUBSTITUTED 2-INDOLINONE MALATE SALT
    5.
    发明授权
    PROCESS FOR PREPARING A 3-PYRROLE SUBSTITUTED 2-INDOLINONE MALATE SALT 有权
    制备3-吡咯取代的2-吲哚酮苹果酸盐的方法

    公开(公告)号：EP2313371B1

    公开(公告)日：2012-08-15

    申请号：EP09762051.2

    申请日：2009-06-12

    申请人： Medichem, S.A.

    发明人： MANGION, Bernardino ,  WINTER, Stephen, Benedict, David

    IPC分类号： C07D207/34 ,  C07D403/06

    CPC分类号： C07D403/06 ,  C07D207/34

    摘要： The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5- formyl-2,4-dimethyl-lH-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib.

    摘要翻译： N- [2-（二乙基氨基）乙基] -5-甲酰基-2,4-二甲基-1H-吡咯-3-甲酰胺的苹果酸盐及其用作制备苹果酸的中间体的用途本发明涉及N- [2-（二乙基氨基）乙基] -5-甲酰基-2,4-二甲基-1H-吡咯-3-甲酰胺的苹果酸盐 舒尼替尼的盐以及包含所述舒尼替尼的苹果酸盐的药物组合物。

    CRYSTALLINE FORMS OF A 3-PYRROLE SUBSTITUTED 2-INDOLINONE MALATE SALT
    8.
    发明公开
    CRYSTALLINE FORMS OF A 3-PYRROLE SUBSTITUTED 2-INDOLINONE MALATE SALT 有权
    3-吡咯取代的2-吲哚酮苹果酸盐的结晶形式

    公开(公告)号：EP2342195A2

    公开(公告)日：2011-07-13

    申请号：EP09786058.9

    申请日：2009-07-24

    申请人： Medichem, S.A.

    发明人： WINTER, Stephen, Benedict, David ,  BENITO VELEZ, Monica

    IPC分类号： C07D403/06 ,  A61K31/404 ,  A61P35/00

    CPC分类号： C07D403/06

    摘要： Disclosed are crystalline polymorphic forms of the malic acid salt of (Z)-N-[2- (diethylamino)ethyl]-5-[(5-fluoro-l,2-dihydro-2-oxo-3H-indol-3-yliden)methyl]-2,4- dimethyl-1H-pyrrole-3-carboxamide, sunitinib malate, including crystalline Forms III, IV, V, VI and VII. Also disclosed are processes for preparing crystalline polymorphic forms of sunitinib malate and pharmaceutical compositions comprising sunitinib malate.

    摘要翻译： 公开了（Z）-N- [2-（二乙基氨基）乙基] -5 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-基） 甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺，苹果酸舒尼替尼，包括结晶形式III，IV，V，VI和VII。 还公开了制备苹果酸舒尼替尼的结晶多晶型物和包含苹果酸舒尼替尼的药物组合物的方法。

    Process for preparing varenicline and intermediates for use therein
    10.
    发明公开
    Process for preparing varenicline and intermediates for use therein 审中-公开
    一种用于瓦伦尼克林的制造和中间体其中使用过程

    公开(公告)号：EP2204369A1

    公开(公告)日：2010-07-07

    申请号：EP09180267.8

    申请日：2009-12-22

    申请人： Medichem, S.A.

    发明人： Szabó, András ,  Papp, Attila Ákos ,  Soto, José Javier ,  Winter, Stephen Benedict David

    IPC分类号： C07D471/08 ,  C07C35/22 ,  C07C47/445

    CPC分类号： C07D471/08 ,  C07B2200/07 ,  C07C29/48 ,  C07C35/22 ,  C07C45/52 ,  C07C2602/08 ,  C07C2603/66 ,  C07C47/445

    摘要： The present invention relates to an improved process for preparing varenicline, or pharmaceutically acceptable salts or solvates thereof, and in particular an improved process for preparing varenicline, or pharmaceutically acceptable salts or solvates thereof, employing intermediate compounds 1,2,3,4-tetrahydro-1,4-methano-naphthalene- cis -2,3-diol (a compound of Formula III), and / or indane-1,3-dicarbaldehyde (a compound of Formula IV) as prepared by a process of the present invention.

    摘要翻译： 本发明涉及到改进的方法用于制备瓦伦尼克林，或其药学上可接受的盐或溶剂化物，并且具体地涉及改进的用于制备瓦伦尼克林，或其药学上可接受的盐或溶剂化物，使用中间体化合物1,2,3,4-四氢 作为制备由本发明的方法-1,4-萘顺式-2,3-二醇（式III化合物），和/或茚满-1,3-二甲醛（式IV化合物） ，