A new process for the preparation of irbesartan
    1.
    发明公开
    A new process for the preparation of irbesartan 审中-公开
    维尔法赫尔·赫斯特伦·冯·厄贝沙坦

    公开(公告)号:EP2194050A1

    公开(公告)日:2010-06-09

    申请号:EP09158339.3

    申请日:2009-04-21

    摘要: A process for the preparation of Irbesartan or a pharmaceutically acceptable salt thereof comprising the step of coupling the 1-pentanamidocyclapentanecarboxamide of formula (V) with 4'-substituted methyl biphenyl-2-carbonitrile or 1-(4'-substituted methyl biphenyl-2-yl)-1H-tetrazole wherein tetrazole can be protected or unprotected to obtain the N-[(2'-cyanobiphenyl-4-yl)methyl]-1-pentanamidocyclopentanecarboxamide or N -[1-({[2'-(1 H- tetrazol-1-yl)biphenyl-4-yl]methylamino)methyl)cydopentyl]pentanamide wherein tetrazole can be protected or unprotected that is further processed to Irbesartan or a pharmaceutical acceptable salt thereof.

    摘要翻译: 一种制备厄贝沙坦或其药学上可接受的盐的方法,其包括将式(V)的1-戊酰氨基环戊烷甲酰胺与4'-取代的甲基联苯-2-腈或1-(4'-取代的甲基联苯基-2 - ((2'-氰基联苯-4-基)甲基] -1-戊酰氨基环戊烷甲酰胺或N - [1 - ({[2' - (1 甲基)环戊基]戊酰胺,其中四唑可被保护或未被保护,进一步加工成厄贝沙坦或其药学上可接受的盐。

    Process for the preparation of optically enriched clopidogrel
    5.
    发明公开
    Process for the preparation of optically enriched clopidogrel 审中-公开
    Herstellungsverfahrenfüroptisch angereichertes Clopidogrel

    公开(公告)号:EP2107061A1

    公开(公告)日:2009-10-07

    申请号:EP08153990.0

    申请日:2008-04-02

    IPC分类号: C07D495/04

    CPC分类号: C07D495/04

    摘要: The invention relates to a process for the preparation of substantially optically pure or optically enriched clopidogrel or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to a process for the preparation of a pharmaceutical formulation comprising substantially optically pure clopidogrel, or a pharmaceutically acceptable salt or solvate thereof, in combination with at least one pharmaceutically acceptable carrier.

    摘要翻译: 本发明涉及制备基本上光学纯的或光学富集的氯吡格雷或其药学上可接受的盐或溶剂化物的方法。 本发明还涉及一种制备药物制剂的方法,其包含与至少一种药学上可接受的载体组合的基本上光学上纯的氯吡格雷或其药学上可接受的盐或溶剂合物。

    Process for the preparation of optically pure omeprazole via salt formation with a chiral amine
    6.
    发明公开
    Process for the preparation of optically pure omeprazole via salt formation with a chiral amine 审中-公开
    Herstellungsverfahrenfüroptisch reines Omeprazol via Salzbildung mit einem chiralen Amin

    公开(公告)号:EP2048144A1

    公开(公告)日:2009-04-15

    申请号:EP07019823.9

    申请日:2007-10-10

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12 C07D453/04

    摘要: The present invention relates to a process for the preparation of substantially optically pure omeprazole, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to a process for preparing a pharmaceutical composition comprising the substantially optically pure omeprazole or the pharmaceutically acceptable salt or solvate thereof and to intermediates useful for the preparation of optically pure omeprazole.

    摘要翻译: 本发明涉及制备基本上光学纯的奥美拉唑或其药学上可接受的盐或溶剂化物的方法。 本发明还涉及一种制备药物组合物的方法,该药物组合物包含基本上光学纯的奥美拉唑或其药学上可接受的盐或溶剂合物,以及可用于制备光学纯奥美拉唑的中间体。

    A process for a preparation of marbofloxacin and intermediate thereof
    8.
    发明公开
    A process for a preparation of marbofloxacin and intermediate thereof 审中-公开
    用于生产麻保沙星及其中间体

    公开(公告)号:EP2332916A3

    公开(公告)日:2011-08-03

    申请号:EP10156733.7

    申请日:2010-03-17

    IPC分类号: C07D215/58

    CPC分类号: C07D215/58

    摘要: The present invention describes a novel process for the preparation of marbofloxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula III, NR 1 R 2 R 3 R 4 wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula II,

    wherein R is selected from H, alkyl, arylalkyl, alkali metal cation, , NH 4 cation, NR 1 R 2 R 3 R 4 cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.

    A process for a preparation of marbofloxacin and intermediate thereof
    9.
    发明公开
    A process for a preparation of marbofloxacin and intermediate thereof 审中-公开
    维多利亚·祖尔·赫尔斯

    公开(公告)号:EP2332916A2

    公开(公告)日:2011-06-15

    申请号:EP10156733.7

    申请日:2010-03-17

    IPC分类号: C07D215/58

    CPC分类号: C07D215/58

    摘要: The present invention describes a novel process for the preparation of marbofloxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula III, NR 1 R 2 R 3 R 4 wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula II,

    wherein R is selected from H, alkyl, arylalkyl, alkali metal cation, , NH 4 cation, NR 1 R 2 R 3 R 4 cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.

    摘要翻译: 本发明描述了制备马氟沙星及其中间体的新方法,其包括式III的氢氧化铵,NR 1 R 2 R 3 R 4的反应,其中R 1,R 2,R 3和R 4独立地选自 H,烷基,烷基芳基,芳基和/或杂芳基与式II化合物反应,其中R选自H,烷基,芳烷基,碱金属阳离子,NH 4阳离子,NR 1 R 2 R 3 R 4阳离子; X是卤素,例如氯,溴,氟,哌嗪基,其可以是取代或未取代的,R'选自H,甲酰基或COOA烷基。

    Pharmaceutical formulation of duloxetine hydrochloride
    10.
    发明公开
    Pharmaceutical formulation of duloxetine hydrochloride 审中-公开
    Pharmazutische Zubereitung Enhaltend Duloxetin Hydrochlorid

    公开(公告)号:EP2308864A1

    公开(公告)日:2011-04-13

    申请号:EP10186667.1

    申请日:2007-02-16

    摘要: The present invention relates to polymorphic forms of duloxetine hydrochloride, especially (duloxetine HCl), which are characterized by an X-ray diffraction pattern with peaks (2θ):9.6, 13.9, 18.0, 18.8, 19.2, 20.8, 27.4, 27.9 (designated form A) or an X-ray diffraction pattern with characteristic peaks (2θ): 12.0, 14.8, 19.8, 21.3, 21.6, 22.1, 22.4, 23.1, 24.1 (designated form T). The present invention also pertains to processes for the preparation of form A and form T, which involves dissolving duloxetine hydrochloride in particular solvents and cooling the solution to obtain crystals, that are dried.

    摘要翻译: 本发明涉及度洛西汀盐酸盐,特别是(度洛西汀盐酸盐)的多晶型物,其特征在于具有峰(2°):9.6,13.9,18.0,18.8,19.2,20.8,27.4,27.9(的X射线衍射图 指定形式A)或具有特征峰(2¸):12.0,14.8,19.8,21.3,21.6,22.1,22.4,23.1,24.1(以T表示)的X射线衍射图。 本发明还涉及制备形式A和形式T的方法,其包括将度洛西汀盐酸盐溶解在特定溶剂中并冷却溶液以获得待干燥的晶体。