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1. 发明申请

WO2006109147A1 SUBSTANTIALLY PURE AMORPHOUS FLUVASTATIN, PROCESSES FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：实质性无定形氟尿嘧啶，其制备方法及含有其的药物组合物
公开(公告)号：WO2006109147A1
公开(公告)日：2006-10-19
申请号：PCT/IB2006/000855
申请日：2006-04-12
申请人： GLENMARK PHARMACEUTICALS LIMITED , BHIRUD, Shekhar, Bhaskar , SRIDHARAN, Ramasubramanian , NAIK, Samir, Jaivant
发明人： BHIRUD, Shekhar, Bhaskar , SRIDHARAN, Ramasubramanian , NAIK, Samir, Jaivant
IPC分类号： C07D209/24 , A61K31/405
CPC分类号： C07D209/24
摘要： A process for producing fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form is provided comprising (a) providing a solvent solution comprising substantially non-amorphous fluvastatin or a pharmaceutically acceptable salt thereof in a solvent capable of dissolving the fluvastatin; and (b) recovering fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form. Also provided is an alternative process for producing fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form comprising (a) providing a solvent solution comprising a straight or branched C 1 -C 4 alkyl ester of substantially non-amorphous fluvastatin in a lower alcoholic solvent or cyclic ether solvent capable of dissolving the fluvastatin; (b) hydrolyzing the fluvastatin ester solution with an aqueous solution comprising an alkali metal hydroxide; and (c) recovering fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form.
摘要翻译：提供了以基本上纯的无定形形式生产氟伐他汀或其药学上可接受的盐的方法，其包括（a）在能够溶解氟伐他汀的溶剂中提供包含基本上非结晶性氟伐他汀或其药学上可接受的盐的溶剂溶液; 和（b）以基本上纯的无定形形式回收氟伐他汀或其药学上可接受的盐。还提供了以基本上纯的无定形形式生产氟伐他汀或其药学上可接受的盐的替代方法，其包括（a）提供包含直链或支链C 1 -C 4烷基的溶剂溶液，在可溶解氟伐他汀的低级醇溶剂或环状醚溶剂中的基本上非结晶性氟伐他汀的烷基酯; （b）用包含碱金属氢氧化物的水溶液水解氟伐他汀酯溶液; 和（c）以基本上纯的无定形形式回收氟伐他汀或其药学上可接受的盐。

2. 发明申请

WO2006129190A1 PROCESS FOR THE PREPARATION OF ALMOTRIPTAN 审中-公开
标题翻译：制备ALMOTRIPTAN的方法
公开(公告)号：WO2006129190A1
公开(公告)日：2006-12-07
申请号：PCT/IB2006/001471
申请日：2006-06-02
申请人： GLENMARK PHARMACEUTICALS LIMITED , PRADHAN, Nitin, Sharad, Chandra , PURUSHOTHAM, Vandanapu, Loka, Appala , NAIK, Samir, Jaivant , SRIDHARAN, Ramasubramanian
发明人： PRADHAN, Nitin, Sharad, Chandra , PURUSHOTHAM, Vandanapu, Loka, Appala , NAIK, Samir, Jaivant , SRIDHARAN, Ramasubramanian
IPC分类号： C07D209/16 , C07F7/08 , A61K31/4045 , A61P25/00
CPC分类号： C07D295/26 , C07D209/16 , C07D209/30 , C07F7/1856 , C07F7/1892 , Y02P20/55
摘要： A process for preparing an intermediate of almotriptan is disclosed, the process comprising the step of Heck coupling a 2-halo aniline derivative of Formula (I): wherein X is a halogen with a protected butynol compound of the general formula (III) wherein Prot can be the same or different and is a suitable protecting group, to provide a protected indole derivative of Formula (II).
摘要翻译：公开了制备阿莫曲坦的中间体的方法，该方法包括将式（I）的2-卤代苯胺衍生物Heck偶联的步骤：其中X是具有通式（III）的保护的丁炔化合物的卤素，其中Prot 可以相同或不同，并且是合适的保护基，以提供式（II）的受保护的吲哚衍生物。

3. 发明申请

WO2004018408A1 SYNTHESIS AND PURIFICATION OF NATEGLINIDE 审中-公开
标题翻译： NATEGLINIDE的合成和纯化
公开(公告)号：WO2004018408A1
公开(公告)日：2004-03-04
申请号：PCT/IB2003/003270
申请日：2003-08-12
申请人： GLENMARK PHARMACEUTICALS LIMITED , NAIK, Samir, Jaivant , KULKARNI, Pramila, Vijay , GAIKWAD, Nandkumar, Baburao , SAWANT, Mangesh, Shivram , BHIRUD, Shekhar , BATCHU, Chandrasekhar
发明人： NAIK, Samir, Jaivant , KULKARNI, Pramila, Vijay , GAIKWAD, Nandkumar, Baburao , SAWANT, Mangesh, Shivram , BHIRUD, Shekhar , BATCHU, Chandrasekhar
IPC分类号： C07C231/14
CPC分类号： C07C231/02 , C07C233/63 , C07C2601/14
摘要： Disclosed is a method for the synthesis of [(trans-4-isopropyl cyclohexyl)-carbonyl] D-phenylalanine (nateglinide) (formula I) including the steps of (i) reacting trans-4-isopropyl cyclohexyl carboxylic acid (formula (5)) with an alkyl chloroformate (formula (13)) where R represents an alkyl group, in a ketonic solvent in the presence of a base at a temperature in the range of -20° to 30°C to form the mixed anhydride of formula (14); and (ii) reacting said mixed anhydride with an aqueous alkali salt solution of Dphenylalanine to yield a reaction mixture including [(trans-4-isopropyl cyclohexyl)carbonyl]-D-phenylalanine.
摘要翻译：公开了合成[（反式-4-异丙基环己基） - 羰基] D-苯丙氨酸（那格列奈）（式I）的方法，包括以下步骤：（i）使反式-4-异丙基环己基羧酸（式（5 ）和氯代甲酸烷基酯（式（13）），其中R表示烷基，在酮溶剂中，在碱的存在下，在-20℃至30℃的温度下，形成式（14）; 和（ii）使所述混合酸酐与D-苯丙氨酸的碱金属盐水溶液反应，得到包含[（反式-4-异丙基环己基）羰基] -D-苯丙氨酸的反应混合物。

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