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1. 发明授权

EP1713788B1 VERFAHREN ZUR HERSTELLUNG VON ENANTIOMERENREINEN AMINOALKOHOLEN 有权
标题翻译：用于生产氨基醇对映纯
公开(公告)号：EP1713788B1
公开(公告)日：2009-03-04
申请号：EP05700995.3
申请日：2005-01-18
申请人： BASF SE
发明人： STÜRMER, Rainer
IPC分类号： C07D333/14 , C07D333/20
CPC分类号： C07D333/16
摘要： The invention relates to a method for producing the enantiomer-pure aminoalcohol of formula (I), by (i) reducing the ketone of formula (3) to the racemic alcohol of formula (4), (ii) enantioselectively acylating the racemic alcohol of formula (4) with succinic anhydride in the presence of a lipase to the succinic acid semi-ester of formula (7), (iii) removing the succinic acid semi-ester of formula (7) from the unreacted enantiomer of formula (4), and (iv) reacting the enantiomer-pure alcohol of formula (4) with methylamine to give the enantiomer-pure alcohol of formula (1).

2. 发明公开

EP1713788A1 VERFAHREN ZUR HERSTELLUNG VON ENANTIOMERENREINEN AMINOALKOHOLEN 有权
标题翻译：用于生产氨基醇对映纯
公开(公告)号：EP1713788A1
公开(公告)日：2006-10-25
申请号：EP05700995.3
申请日：2005-01-18
申请人： BASF Aktiengesellschaft
发明人： STÜRMER, Rainer
IPC分类号： C07D333/14 , C07D333/20
CPC分类号： C07D333/16
摘要： The invention relates to a method for producing the enantiomer-pure aminoalcohol of formula (I), by (i) reducing the ketone of formula (3) to the racemic alcohol of formula (4), (ii) enantioselectively acylating the racemic alcohol of formula (4) with succinic anhydride in the presence of a lipase to the succinic acid semi-ester of formula (7), (iii) removing the succinic acid semi-ester of formula (7) from the unreacted enantiomer of formula (4), and (iv) reacting the enantiomer-pure alcohol of formula (4) with methylamine to give the enantiomer-pure alcohol of formula (1).

3. 发明公开

EP1989193A1 PROCESS FOR OBTAINING ENANTIOMERS OF DULOXETINE PRECURSORS 有权
标题翻译：程序用于获得度洛西汀前体对映体
公开(公告)号：EP1989193A1
公开(公告)日：2008-11-12
申请号：EP07711690.3
申请日：2007-02-27
申请人： Laboratorios Del. Dr. Esteve, S.A.
发明人： BUSCHMANN, Helmut Heinrich , TORRENS JOVER, Antoni , LORMANN, Matthias , DAHMEN, Stefan
IPC分类号： C07D333/12 , C07D333/14 , C07D333/24
CPC分类号： C07D333/24 , C07D333/12 , C07D333/14 , Y02P20/55
摘要： The present invention is directed to a process for the preparation of an enantiomerically enriched compound of formula (II) wherein, R1, R2 and R3 are each independently selected from hydrogen, halogen, substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl; X is -C(=O)-Z or -Y, wherein -Y is selected from -CH2-OR4, -CH2-halogen or -CH2-NR6R7; wherein Z is selected from -NR6R7 or -OR5, wherein R5 is selected from hydrogen, substituted or unsubstituted lower alkyl or ester activating group; R4 is selected from hydrogen, hydroxyl protecting group or hydroxyl activating group; R6 and R7 are each independently selected from hydrogen, amino protecting group, amido protecting group or substituted or unsubstituted lower alkyl; or a pharmaceutically acceptable salt, complex or solvate thereof; which comprises an enantioselective addition with a thienyl zinc reagent, in the presence of a chiral ligand.

4. 发明公开

EP1296940A1 AMIDINE DERIVATIVES AS SELECTIVE ANTAGONISTS OF NMDA RECEPTORS 有权
标题翻译： AMIDINDERIVATE ALS SELEKTIVE NMDA-REZEPTORANTAGONISTEN
公开(公告)号：EP1296940A1
公开(公告)日：2003-04-02
申请号：EP01938439.5
申请日：2001-06-14
申请人： MERCK SHARP & DOHME LTD.
发明人： CURTIS, Neil Roy , KULAGOWSKI, Janusz Jozef , THOMAS, Steve , WATT, Alan Paul
IPC分类号： C07C257/14 , C07D333/14 , C07D307/52 , C07D213/36 , A61K31/155 , A61P25/00
CPC分类号： C07D213/40 , C07C257/14 , C07C2601/14
摘要： A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.
摘要翻译：作为对NM2受体的拮抗剂的一类苯乙烯基脒衍生物，对于含有NR2B亚基的那些受体是选择性的，在治疗和/或预防神经和神经退行性疾病中尤其是神经性疼痛和头痛，特别是偏头痛显示与其他类别的NMDA受体拮抗剂相关的少见的和相关的副作用。

5. 发明公开

EP2040697A2 POLYMORPHIC FORM OF DULOXETINE HYDROCHLORIDE 审中-公开
标题翻译：盐酸度洛西汀的多晶型
公开(公告)号：EP2040697A2
公开(公告)日：2009-04-01
申请号：EP07805049.9
申请日：2007-07-03
申请人： Ranbaxy Laboratories Limited
发明人： BISWAS, Sujoy , KARANJAI, Keya
IPC分类号： A61K31/381 , C07D333/14
CPC分类号： C07D333/14
摘要： The present invention relates to Form I of duloxetine hydrochloride and its preparation.

6. 发明公开

EP1826204A1 Process for obtaining enantiomers of duloxetine precursors 审中-公开
标题翻译： Verfahren zur Herstellung enantomerer Ausgangsverbindungen von Duloxetin
公开(公告)号：EP1826204A1
公开(公告)日：2007-08-29
申请号：EP06380038.7
申请日：2006-02-28
申请人： LABORATORIOS DEL DR. ESTEVE, S.A.
发明人： Torrens Jover, Antoni , Buschmann, Helmut Henrich , Dahmen, Stefan , Lormann, Matthias
IPC分类号： C07D333/12 , C07D333/14 , C07D333/24
CPC分类号： C07D333/24 , C07D333/12 , C07D333/14 , Y02P20/55
摘要： The present invention is directed to a process for the preparation of an enantiomerically enriched compound of formula II

wherein,
R 1 , R 2 and R 3 are each independently selected from hydrogen, halogen, substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl;
X is -C(=O)-Z or -Y, wherein -Y is selected from -CH 2 -OR 4 , -CH 2 -halogen or - CH 2 -NR 6 R 7 ;
wherein
Z is selected from -NR 6 R 7 or -OR 5 , wherein R 5 is selected from hydrogen, substituted or unsubstituted lower alkyl or ester activating group;
R 4 is selected from hydrogen, hydroxyl protecting group or hydroxyl activating group;
R 6 and R 7 are each independently selected from hydrogen, amino protecting group, amido protecting group or substituted or unsubstituted lower alkyl;

which comprises an enantioselective addition with a thienyl zinc reagent, in the presence of a chiral ligand.
摘要翻译：本发明涉及一种制备对映体富集的式II化合物的方法，其中R 1，R 2和R 3各自独立地选自氢，卤素，取代或未取代的低级烷基或取代或未取代的芳基; X是-C（= O）-Z或-Y，其中-Y选自-CH 2 -OR 4，-CH 2 - 卤素或-CH 2 -NR 6 R 7; 其中Z选自-NR 6 R 7或-OR 5，其中R 5选自氢，取代或未取代的低级烷基或酯活化基团; R 4选自氢，羟基保护基或羟基活化基团; R 6和R 7各自独立地选自氢，氨基保护基，酰氨基保护基或取代或未取代的低级烷基; 其包括在手性配体存在下用噻吩锌试剂进行对映选择性加成。

7. 发明公开

EP0238401A3 Sulfon amides derived from diaryl methanes, processes for their preparation and pharmaceutical preparation containing them 失效
标题翻译：二胺衍生的磺胺类，其制备方法和含有它们的药物制剂
公开(公告)号：EP0238401A3
公开(公告)日：1987-12-02
申请号：EP87400556
申请日：1987-03-12
申请人： SANOFI
发明人： Roger, Pierre , Fournier, Jean-Paul , Martin, Alain , Choay, Jean
IPC分类号： C07C143/78 , C07D333/14 , C07D333/22 , A61K31/195 , A61K31/20 , A61K31/275 , A61K31/165 , A61K31/22 , A61K31/38
CPC分类号： C07D295/13 , C07D333/18 , C07D333/22

8. 发明公开

EP0238401A2 Nouveaux sulfonamides dérivés de diarylméthanes et leurs procédés de préparation et les compositions pharmaceutiques les contenant 失效
标题翻译：二芳基甲烷磺酰胺衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0238401A2
公开(公告)日：1987-09-23
申请号：EP87400556.4
申请日：1987-03-12
申请人： SANOFI
发明人： Roger, Pierre , Fournier, Jean-Paul , Martin, Alain , Choay, Jean
IPC分类号： C07C311/19 , C07C311/14 , C07D333/14 , C07D333/22 , A61K31/195 , A61K31/20 , A61K31/275 , A61K31/165 , A61K31/22 , A61K31/38
CPC分类号： C07D295/13 , C07D333/18 , C07D333/22
摘要： L'invention a pour objét de nouveaux composés répondant à la formule I
dans laquelle:

- W représente C = 0, CH 2 ou CHOH,
- Z représente

- R 1 et R 2 représentent notamment C1 ou F,
- R, R' et R" représentent notamment H,
- X représente notamment CH 2 ,
- Y représente notamment COOH,
- u et v sont deux nombres entiers de 0 à 2
- p et q valent 0 ou 1
- n et m sont deux nombres entiers variant de 0 à 10 et t vaut 0 ou 1,
- le nombre total d'atomes de carbone de la chaine - (CH 2 ) n ( 1 CH) t - X - 1 CH - (CH 2 )m Y, variant de 2 à 20, ainsi que leurs sels physiologiquement acceptables obtenus avec des acides organiques ou minéraux.

Ces composés sont utiles pour la préparation de médicaments possédant notamment des propriétés anti-inflammatoires.

9. 发明授权

EP1989193B1 PROCESS FOR OBTAINING ENANTIOMERS OF DULOXETINE PRECURSORS 有权
标题翻译：程序用于获得度洛西汀前体对映体
公开(公告)号：EP1989193B1
公开(公告)日：2011-06-22
申请号：EP07711690.3
申请日：2007-02-27
申请人： Laboratorios del. Dr. Esteve, S.A.
发明人： BUSCHMANN, Helmut Heinrich , TORRENS JOVER, Antoni , LORMANN, Matthias , DAHMEN, Stefan
IPC分类号： C07D333/12 , C07D333/14 , C07D333/24
CPC分类号： C07D333/24 , C07D333/12 , C07D333/14 , Y02P20/55
摘要： The present invention is directed to a process for the preparation of an enantiomerically enriched compound of formula (II) wherein, R1, R2 and R3 are each independently selected from hydrogen, halogen, substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl; X is -C(=O)-Z or -Y, wherein -Y is selected from -CH2-OR4, -CH2-halogen or -CH2-NR6R7; wherein Z is selected from -NR6R7 or -OR5, wherein R5 is selected from hydrogen, substituted or unsubstituted lower alkyl or ester activating group; R4 is selected from hydrogen, hydroxyl protecting group or hydroxyl activating group; R6 and R7 are each independently selected from hydrogen, amino protecting group, amido protecting group or substituted or unsubstituted lower alkyl; or a pharmaceutically acceptable salt, complex or solvate thereof; which comprises an enantioselective addition with a thienyl zinc reagent, in the presence of a chiral ligand.

10. 发明授权

EP1296940B1 AMIDINE DERIVATIVES AS SELECTIVE ANTAGONISTS OF NMDA RECEPTORS 有权
标题翻译：脒作为选择性NMDA受体拮抗剂
公开(公告)号：EP1296940B1
公开(公告)日：2008-07-02
申请号：EP01938439.5
申请日：2001-06-14
申请人： MERCK SHARP & DOHME LTD.
发明人： CURTIS, Neil Roy , KULAGOWSKI, Janusz Jozef , THOMAS, Steve , WATT, Alan Paul
IPC分类号： C07C257/14 , C07D333/14 , C07D307/52 , C07D213/36 , A61K31/155 , A61P25/00
CPC分类号： C07D213/40 , C07C257/14 , C07C2601/14
摘要： A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.

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