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1. 发明申请

WO2013011526A1 PROCESS FOR PREPARATION OF LISDEXAMPHETAMINE AND SALTS THEREOF 审中-公开
标题翻译：制备二苯并咪唑及其盐的方法
公开(公告)号：WO2013011526A1
公开(公告)日：2013-01-24
申请号：PCT/IN2012/000506
申请日：2012-07-18
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD Shekhar Bhaskar , SARIN GURDEEP, Singh , KUMAR, Rajiv
发明人： BHIRUD Shekhar Bhaskar , SARIN GURDEEP, Singh , KUMAR, Rajiv
IPC分类号： C07C237/06 , C07C231/02 , C07C271/22 , C07C269/04
CPC分类号： C07C269/04 , C07C231/12 , C07C269/06 , C07C269/08 , C07C271/22 , C07C303/22 , C07C237/06 , C07C309/04
摘要： An improved, efficient, safe and convenient process for preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate is provided. A process for preparation of diamino protected amide compound namely BOC protected lisdexamphetamine, a key intermediate in the preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate and its purification by crystallization are also provided. Further, novel mixed anhydride intermediate is provided too.
摘要翻译：提供了一种通过使用新的混合酸酐中间体来改进，有效，安全和方便地制备盐酸安非他明及其药学上可接受的盐的方法。还提供了制备二氨基保护的酰胺化合物的方法，即BOC保护的地塞沙芬，其是通过使用新的混合酸酐中间体及其通过结晶进行纯化制备西班牙安非他明及其药学上可接受的盐的关键中间体。此外，还提供了新的混合酸酐中间体。

2. 发明申请

WO2012038974A1 PROCESS FOR PREPARING L-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVE 审中-公开
标题翻译：制备L-苯基-3-二甲氨基酚衍生物的方法
公开(公告)号：WO2012038974A1
公开(公告)日：2012-03-29
申请号：PCT/IN2011/000646
申请日：2011-09-20
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , MISHRA, Sushanta , JAMSHAD, Danish
发明人： BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , MISHRA, Sushanta , JAMSHAD, Danish
IPC分类号： C07C213/08 , C07C215/54 , C07C217/62 , C07C219/22
CPC分类号： C07C213/02 , C07C213/00 , C07C309/73 , C07C215/54
摘要： Provided is a process for the preparing l-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.
摘要翻译：提供了通过新型中间体制备式I的1-苯基-3-二甲基氨基丙烷衍生物的方法（该式应该在此插入）及其药学上可接受的盐。

3. 发明申请

WO2012035553A1 PROCESS FOR PREPARING ANDROSTENONE DERIVATIVES 审中-公开
标题翻译：制备安慰剂衍生物的方法
公开(公告)号：WO2012035553A1
公开(公告)日：2012-03-22
申请号：PCT/IN2011/000625
申请日：2011-09-13
申请人： IND-SWIFT LABORATORIES LIMITED , SARIN GURDEEP, Singh , AAVULA, Sivaji , BHIRUD SHEKHAR, Bhaskar
发明人： SARIN GURDEEP, Singh , AAVULA, Sivaji , BHIRUD SHEKHAR, Bhaskar
IPC分类号： C07J75/00 , C07J73/00 , C07D221/18 , C07J41/00
CPC分类号： C07J73/005
摘要： Provided is a process for preparing androstenone derivatives, specifically 3-oxo-4-aza-5α-androstene-17β-carboxylic acid of Formula I, a key intermediate for dutasteride.
摘要翻译：提供了制备雄酮酮衍生物的方法，特别是式I的3-氧代-4-氮杂-5α-雄甾烯-17β-羧酸，其是度他雄胺的关键中间体。

4. 发明申请

WO2011092719A3 PROCESS FOR PREPARING 1 -PHENYL-3 -DIMETHYLAMINOPROPANE DERIVATIVES 审中-公开
标题翻译：制备1-苯基-3-二甲氨基酚衍生物的方法
公开(公告)号：WO2011092719A3
公开(公告)日：2011-09-22
申请号：PCT/IN2011000060
申请日：2011-01-28
申请人： IND SWIFT LAB LTD , BHIRUD SHEKHAR BHASKAR , JOHAR PERMINDER SINGH , SHARMA EKTA , JAMSHAD DANISH , PRAJAPATY RAMKARAN
发明人： BHIRUD SHEKHAR BHASKAR , JOHAR PERMINDER SINGH , SHARMA EKTA , JAMSHAD DANISH , PRAJAPATY RAMKARAN
IPC分类号： C07C215/54 , C07C211/27 , C07C213/00 , C07C217/62
CPC分类号： C07C215/54 , C07C41/22 , C07C41/26 , C07C43/23 , C07C51/487 , C07C59/64 , C07C43/225
摘要： Process for preparing 1-phenyl-3-dimethylaminopropane derivatives of formula (I), and pharmaceutically acceptable salts thereof from intermediate of formula (II) are provided, wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, SOR2, SO2R2, -SO3H, -NO2, -NR2R2', - CONR2R2 ', and the like; R ' can be selected from hydrogen, alkyl, aryl, aralkyl, alkaryl, heteroaryl, and the like; or R2 and R2 ' can be same or different and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl,-OR3, - COR3, -PO3(R3R1) wherein R1 and R4 can be same or different and can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.
摘要翻译：提供了制备式（I）的1-苯基-3-二甲基氨基丙烷衍生物及其药学上可接受的盐从式（II）中间体制备的方法，其中R 1可以选自-OR 2，卤素，-CH 2 OR 2，-SR 2，SOR 2 ，SO 2 R 2，-SO 3 H，-NO 2，-NR 2 R 2'， - CONR 2 R 2'等; R'可以选自氢，烷基，芳基，芳烷基，烷芳基，杂芳基等; 或R 2和R 2'可以相同或不同，并且可以选自氢，烷基，芳基，芳烷基，杂芳基，-OR3，-CON3，-PO3（R3R1），其中R1和R4可以相同或不同，并且可以选自烷基，芳基，芳烷基，杂芳基等。

5. 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。

6. 发明申请

WO2013027227A1 NOVEL POLYMORPHIC FORM I OF RIFAXIMIN 审中-公开
标题翻译：新的多态性我的RIFAXIMIN
公开(公告)号：WO2013027227A1
公开(公告)日：2013-02-28
申请号：PCT/IN2012/000507
申请日：2012-07-18
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , MISHRA, Sushanta
发明人： BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , MISHRA, Sushanta
IPC分类号： C07D498/22
CPC分类号： C07D498/22
摘要： Provided is a novel polymorphic form I of rifaximin and a process for preparation thereof. The novel polymorphic form I is characterized by powder x-ray diffraction pattern at 2Θ 5.2, 7.2, 8.4 and 8.7 degrees±0.2 and water content within the range of 2.0 to 4.5%. A process for preparation of novel polymorphic form I by treating rifaximin with a mixture of ethyl alcohol and water is also provided.
摘要翻译：提供了利福昔明的新型多晶型I及其制备方法。新型多晶型I的特征在于2T 5.2,7.2,8.4和8.7±0.2的粉末x射线衍射图，水含量在2.0〜4.5％的范围内。还提供了通过用乙醇和水的混合物治疗利福昔明来制备新型多晶型I的方法。

7. 发明申请

WO2012004811A1 PROCESS FOR THE PREPARATION OF 5-SUBSTSITUTED INDOLE DERIVATIVE 审中-公开
标题翻译：制备5-SUBSTINDIN INDOLE DERIVATIVE的方法
公开(公告)号：WO2012004811A1
公开(公告)日：2012-01-12
申请号：PCT/IN2011/000447
申请日：2011-07-04
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , SHARMA, Ekta , PRAJAPATY, Ramkaran , GUPTA, Chandan, Kumar
发明人： BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , SHARMA, Ekta , PRAJAPATY, Ramkaran , GUPTA, Chandan, Kumar
IPC分类号： C07D401/06 , C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to an improved and industrially advantageous process for preparation of eletri tan of formula I,or pharmaceutically acceptable salts thereof from bromo indole intermediate of formula II, through isolation of N-acetylated bromo indole intermediate of formula III, to elude carrying forward of impurities to next stage. The present invention relates to process for the preparation of 5-bromo-3-[(R)-l-methyl-pyrrolidin-2- lmeth l -lH-indol of formula II, a key intermediate for the synthesis of eletriptan or pharmaceutically acceptable salts thereof, through novel keto carbamate intermediate. The present invention also relates to novel process for the preparation of a-form of eletriptan hydrobromide.
摘要翻译：本发明涉及通过分离式III的N-乙酰化溴吲哚中间体，从式I的溴吲哚中间体制备式I的电子衍生物或其药学上可接受的盐的改进和工业上有利的方法，以避免携带的杂质到下一阶段。本发明涉及制备式II的5-溴-3 - [（R）-1-甲基 - 吡咯烷-2-基甲基] -1H-吲哚的方法，该化合物是合成依他曲坦或药学上可接受的关键中间体其盐，通过新的酮基氨基甲酸酯中间体。本发明还涉及一种制备α-形式的依他曲坦氢溴酸盐的新方法。

8. 发明申请

WO2011154977A1 'PROCESS FOR THE PREPARATION OF COLESEVELAM HYDROCHLORIDE" 审中-公开
标题翻译： “制备COLESEVELAM HYDROCHLORIDE的方法”
公开(公告)号：WO2011154977A1
公开(公告)日：2011-12-15
申请号：PCT/IN2011/000382
申请日：2011-06-08
申请人： IND-SWIFT LABORATORIES LIMIT , BHIRUD Shekhar Bhaskar , JOHAR, Perminder Singh , SHARMA, Ekta , SHARMA, Veerender
发明人： BHIRUD Shekhar Bhaskar , JOHAR, Perminder Singh , SHARMA, Ekta , SHARMA, Veerender
IPC分类号： C08G73/02
CPC分类号： C08G73/022
摘要： The present invention provides an industrially advantageous and efficient process for the preparation of colesevelam hydrochloride using dried colesevelam and a source of chloride ion which includes hydrogen chloride gas, solvent saturated with hydrogen chloride gas; hydrochloride salt of a suitable amine having formula NR 1 R 2 R 3 . HCl (wherein R 1 R 2 and R 3 can be same or different and can be individually selected amongst hydrogen, substituted or unsubstituted alkyl or aryl or alkaryl, aralkyl, heteroaryl); sulfur compounds; carboxylic acid chloride having formula R 1 COCI ( wherein R 1 is as defined above; silyl chloride of formula R 1 R 2 R 3 SiC1 (wherein R 1 R 2 and R 3 are as defined above); metal chlorides such as TiCI 4 ; TiCl 3 ; BCI 3 ; AlCl 3 ; PCI 3 ; PCl 5 ; or alkali metal chloride in combination with a sulfuric acid and the like or in combination thereof.
摘要翻译：本发明提供了一种工业上有利且有效的制备盐酸利多韦姆的方法，该方法是使用干燥的考来普兰和氯离子源，包括氯化氢气体，氯化氢气体饱和的溶剂; 盐酸盐，其具有式NR1R2R3的合适的胺。 HCl（其中R 1 R 2和R 3可以相同或不同，并且可以分别选自氢，取代或未取代的烷基或芳基或烷芳基，芳烷基，杂芳基）; 硫化合物; 具有式R 1 COCI（其中R 1如上定义）的羧酸酰氯;式R 1 R 2 R 3 SiCl（其中R 1 R 2和R 3如上定义）的甲硅烷基氯;金属氯化物如TiCl 4; TiCl 3; BCl 3; AlCl 3; PCI 3; PCl5;或碱金属氯化物与硫酸等的组合或其组合。

9. 发明申请

WO2011080756A1 PROCESS FOR THE PREPARATION OF 1-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVES 审中-公开
标题翻译：制备1-苯基-3-二甲基亚胺基衍生物的方法
公开(公告)号：WO2011080756A1
公开(公告)日：2011-07-07
申请号：PCT/IN2010/000855
申请日：2010-12-27
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , SHARMA, Ekta , JAMSHAD, Danish , PRAJAPATY, Ramkaran
发明人： BHIRUD, Shekhar, Bhaskar , JOHAR, Perminder, Singh , SHARMA, Ekta , JAMSHAD, Danish , PRAJAPATY, Ramkaran
IPC分类号： C07D213/02 , C07D215/42 , C07D217/52 , C07D219/24 , C07D229/46
CPC分类号： C07C59/64 , C07B2200/07 , C07C213/00 , C07C235/34 , C07C255/13 , C07C255/37 , C07C255/41 , C07C317/46 , C07C215/54
摘要： A process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives of formula (I) and its pharmaceutically acceptable salts thereof from cyano intermediate of formula (II), wherein R 1 can be selected from -OR 2 , halo, -CH 2 OR 2 , -SR 2 , -SOR 2 , SO 2 R 2 , -SO 3 H, -NO 2 , -NR 2 R 2 ', -CONR 2 R 2 ', carboxylic esters, sulfonate esters or phosphate esters, R 2 and R 2 ' can be same or different, and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl, -COR 2 ", -P0 3 (R 2 ") 2 wherein R 2 " can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.
摘要翻译：从式（II）的氰基中间体制备式（I）的1-苯基-3-二甲基氨基丙烷衍生物及其药学上可接受的盐的方法，其中R 1可以选自-OR 2，卤代，-CH 2 OR 2，-SR 2 ，-SOR 2，SO 2 R 2，-SO 3 H，-NO 2，-NR 2 R 2'，-CONR 2 R 2'，羧酸酯，磺酸酯或磷酸酯，R 2和R 2'可以相同或不同，并且可以选自氢，烷基，芳基，芳烷基，杂芳基，-COR 2“，-PO 3（R 2”）2，其中R 2“可以选自烷基，芳基，芳烷基，杂芳基等。

10. 发明申请

WO2010140168A1 IMPROVED PROCESS FOR PREPARING TEMOZOLOMIDE 审中-公开
标题翻译：改进制备TEMOZOLOMIDE的方法
公开(公告)号：WO2010140168A1
公开(公告)日：2010-12-09
申请号：PCT/IN2010/000365
申请日：2010-06-02
申请人： IND-SWIFT LABORATORIES LIMITED , BHIRUD, Shekhar Bhaskar , SARIN, Gurdeep Singh , GUPTA, Neeraj , TIWARI, Parveen Kumar , CHIDAMBARAM, Venkateswaran Srinivasan , WADHWA, Lalit
发明人： BHIRUD, Shekhar Bhaskar , SARIN, Gurdeep Singh , GUPTA, Neeraj , TIWARI, Parveen Kumar , CHIDAMBARAM, Venkateswaran Srinivasan , WADHWA, Lalit
IPC分类号： C07D487/04 , C07D233/90 , C07C225/06
CPC分类号： C07D487/04 , C07D233/90
摘要： A process for preparing temozolomide by employing mild reaction and easy isolation of temozolomide is provided.
摘要翻译：提供了采用轻度反应和容易分离替莫唑胺来制备替莫唑胺的方法。

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