公开(公告)号：EP2468751A2

公开(公告)日：2012-06-27

申请号：EP11195387.3

申请日：2011-12-22

申请人： Medichem, S.A.

发明人： Boch i Lladó, Jordi ,  Duran López, Ernestp

IPC分类号： C07D491/04

CPC分类号： C07D491/04

摘要： This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1 H- dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.

摘要翻译： 本发明提供了制备5-氯-2-甲基-2,3,3a，12b-四氢-1H-二苯并[2,3：6,7]氧杂环庚烯并[4,5-c]吡咯的改进方法， 阿塞那平。 这些方法允许以良好的产率和高立体选择性以工业规模制备阿替那非。

公开(公告)号：EP2228371A1

公开(公告)日：2010-09-15

申请号：EP10155234.7

申请日：2006-12-22

申请人： Medichem, S.A.

发明人： Chamorro, Iolanda

IPC分类号： C07D313/12

CPC分类号： C07D313/12

摘要： The invention covers a process for preparing olopatadine free base and/or its hydrochloride salt by performing a Wittig reaction, wherein said Wittig reaction comprises the use of at least one of hexyllithium, sodium hydride and combinations thereof. The process of invention achieves olapatadine free base and/or its hydrochloride salt having less than approximately 0.5% by area percentage HPLC of olapatadine trans isomer and a reduced level of bromide impurities.

摘要翻译： 本发明涵盖了通过进行Wittig反应来制备奥洛他定游离碱和/或其盐酸盐的方法，其中所述维t希反应包括使用己基锂，氢化钠及其组合中的至少一种。 本发明的方法实现了奥拉帕定游离碱和/或其盐酸盐，其具有低达约0.5％的奥拉他定反式异构体的HPLC百分比，并且降低了溴化物杂质含量。

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.

发明人： TOJO SUAREZ, Gabriel ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADO, Jordi

IPC分类号： C07D491/10

CPC分类号： C07D491/10

公开(公告)号：EP2142540A2

公开(公告)日：2010-01-13

申请号：EP08719386.8

申请日：2008-03-28

申请人： Medichem S.A.

发明人： PUIG SERRANO, Jordi ,  CAMPS, Pelayo

IPC分类号： C07D453/02

CPC分类号： C07D403/10

摘要： The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.

公开(公告)号：EP2118056A2

公开(公告)日：2009-11-18

申请号：EP08702212.5

申请日：2008-01-10

申请人： Medichem, S.A.

发明人： WINTER, Stephen ,  BOSCH, Jordi ,  PUIG SERRANO, jordi ,  SOTO, Jose, Javier

IPC分类号： C07D207/16

CPC分类号： C07D207/16

摘要： The present invention relates to a process for preparing vildagliptin of formula (I) with high chemical and enantiomeric purity and compositions comprising vildagliptin. In addition, the present invention relates to (2S,2'S)-1,1'-[[(3-hydroxytricyclo[3.3.1.13'7]dec-1- y1)imino]bis(1-oxo-2,1-ethanediyl)]di(2-pyrrolidinecarbonitrile) of formula (II), processes for preparing, and compositions comprising a compound for formula (II). Furthermore, the invention relates to processes for determining the purity of vildagliptin using a compound of formula (II).

公开(公告)号：EP1971573B1

公开(公告)日：2009-10-14

申请号：EP06850451.3

申请日：2006-12-22

申请人： Medichem S.A.

发明人： GAVALDA I ESCUDE, Ana ,  BOSCH I LLADO, Jordi ,  VIDAL I FERRAN, Anton ,  GARCIA GARCIA, Eva

IPC分类号： C07D205/08 ,  C07D263/24

CPC分类号： C07D205/08

摘要： The invention relates, in general, to an improved process for the preparation of the compounds (3R,4S)-4-(4-(benzyloxy)phenyl)-l-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3- oxopropyl]azetidin-2-one and (3R,4S)-l-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]- 4-(4-hydroxyphenyl)-azetidin-2-one, which are key intermediates for the synthesis of ezetimibe, as well as the use of these intermediates for the preparation of ezetimibe.

公开(公告)号：EP1971570A2

公开(公告)日：2008-09-24

申请号：EP06851235.9

申请日：2006-12-22

申请人： Medichem, S.A.

发明人： ARNALOT AGUILAR, Carmen ,  BOSCH I LLADÓ, Jordi

IPC分类号： C07C213/02 ,  C07C213/08 ,  C07C217/32 ,  A61K31/135 ,  A61P9/10 ,  A61P9/12

CPC分类号： C07C213/02 ,  C07C213/08 ,  C07C213/10 ,  C07C217/32

摘要： The invention relates to an improved process for preparing metoprolol and its salts.

公开(公告)号：EP1948593A2

公开(公告)日：2008-07-30

申请号：EP06850464.6

申请日：2006-10-27

申请人： Medichem, S.A.

发明人： AUQUER PEDEMONTE, Ignasi

IPC分类号： C07C303/40 ,  C07C311/37 ,  A61K31/18 ,  A61P13/08

CPC分类号： C07C303/40 ,  C07B2200/07 ,  C07C311/37

摘要： The invention relates, in general, to the preparation of (R)(-)tamsulosin free base by reaction of (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide or an addition salt thereof with 1 -(2-bromoethoxy)-2-ethoxybenzene in a polar aprotic solvent in the presence of an organic base. More particularly, the invention relates to a process for preparing pure solid crystalline (R)(-)tamsulosin in its free base form as a precursor for the production of (R)(-)tamsulosin hydrochloride.

公开(公告)号：EP1426356B1

公开(公告)日：2008-04-16

申请号：EP01969812.5

申请日：2001-09-14

申请人： Medichem S.A.

发明人： BOSCH I LLADO, Jordi ,  CAMPS GARCIA, Pelayo ,  CONTRERAS LASCORZ, Juan ,  ONRUBIA MIGUEL, Ma Carmen

IPC分类号： C07C233/11 ,  C07C231/02 ,  C07D241/04

CPC分类号： C07C237/22 ,  C07D241/04

摘要： The invention relates to intermediate compounds that are used for the preparation of mirtazapine and the production methods thereof. The inventive method is used to produce (+/-)-3-phenyl-1-methylpiperazine which is an important intermediate for the production of mirtazapine. Said method consists in subjecting novel compounds having general formula (I), wherein Z is a leaving group that can undergo nucleophilic displacement, to a cyclization reaction in the presence of a reducing agent. The invention also relates to a method of producing novel compounds having formula (I).

公开(公告)号：EP1879865A1

公开(公告)日：2008-01-23

申请号：EP06795321.6

申请日：2006-04-13

申请人： Medichem S.A.

发明人： BENITO VELEZ, Monica ,  MOLINS I GRAU, Elies ,  ARNALOT AGUILAR, Carmen ,  MANGION, Bernardino

IPC分类号： C07D215/22 ,  A61K31/496 ,  A61P25/18

CPC分类号： C07D215/22

摘要： The invention relates to polymorphic crystalline forms of aripiprazole, synthetic processes for their preparation and pharmaceutical compositions containing the same. These crystalline forms of aripiprazole can be readily milled and can be easily combined with various pharmaceutical adjuvants without effecting changes to their crystalline structure when, for example, pressed into tablet or capsule form.