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1. 发明申请

WO2012101475A1 AN IMPROVED PROCESS FOR THE PREPARATION OF ANTIHISTAMINIC DRUGS VIA A NOVEL CARBAMATE INTERMEDIATE 审中-公开
标题翻译：通过新型碳酸氢钠中间体制备抗病毒药物的改进方法
公开(公告)号：WO2012101475A1
公开(公告)日：2012-08-02
申请号：PCT/IB2011/003075
申请日：2011-12-19
申请人： JUBILANT LIFE SCIENCES LIMITED , BISWAS, Sujay , DUBEY, Shailendra, Kumar , MANGLA, Amit , MASAND, Mukesh , VIR, Dharam
发明人： BISWAS, Sujay , DUBEY, Shailendra, Kumar , MANGLA, Amit , MASAND, Mukesh , VIR, Dharam
IPC分类号： C07D295/088 , C07D295/205
CPC分类号： C07D295/205 , C07D295/088
摘要： The present invention relates to a novel racemic or optically active carbamate intermediate of formula (IV A). This novel racemic or optically active carbamate intermediate of formula (IV A) can be used to prepare drugs having antihistaminic activity such as cetirizine (IA), meclizine (IB), chlorcyclizine (IC), clocinizine (ID), buclizine (IE) and enantiomers thereof such as levocetirizine (I). Further, disclosed herein is an improved process for the preparation of levocetirizine via a novel optically active intermediate i.e. compound of formula (IV). Also, disclosed herein is a novel process for the preparation of compound (II) and for crystallization of its salt.
摘要翻译：本发明涉及式（IVA）的新型外消旋或光学活性氨基甲酸酯中间体。式（IVA）的这种新型外消旋或旋光活性氨基甲酸酯中间体可用于制备具有抗组胺活性的药物，如西替立嗪（IA），麦克利嗪（IB），氯氰环己烷（IC），丁草胺（ID）对映异构体，如左西替利嗪（I）。此外，本文公开了通过新型光学活性中间体即式（IV）化合物制备左西替利嗪的改进方法。此外，本文公开了用于制备化合物（II）和其盐的结晶的新方法。

2. 发明申请

WO2006111983A3 NOVEL POLYMORPHIC FORM OF (l-BENZYL-4-[(5,6-DIMETHOXY-l- INDANONE)-2-YL]METHYL PIPERIDINE HYDROCHLORIDE AND PROCESS FOR PREPARING THE SAME 审中-公开
公开(公告)号：WO2006111983A3
公开(公告)日：2006-10-26
申请号：PCT/IN2006/000136
申请日：2006-04-21
申请人： JUBILANT ORGANOSYS LIMITED , DUBEY, Shailendra, Kumar , GUPTH, Poorvi , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
发明人： DUBEY, Shailendra, Kumar , GUPTH, Poorvi , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
IPC分类号： C07D211/32 , A61K31/445 , A61P25/28
摘要： Disclosed herein are novel and stable polymorphic form of Donepezil Hydrochloride, wherein said polymorphic form is designated as J and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic form and use thereof to prepare another forms is also disclosed.

3. 发明申请

WO2012120356A3 PROCESS FOR THE PREPARATION OF (S)-(+)-OR (R)-(-)-10 HYDROXY DIHYDRODIBENZ[B,F]AZEPINES BY ENANTIOSELECTIVE REDUCTION OF 10, 11-DIHYDRO-10-OXO-5H-DIBENZ[B,F]AZEPINES AND POLYMORPHS THEREOF 审中-公开
标题翻译：通过选择性还原10,11-二氢-10-OXO-5H-二苯并[b]的（S） - （+） - 或（R） - （ - ） - 10-羟基二氢苯并[B，F] ，F] AZEPINES和POLYMORPHS
公开(公告)号：WO2012120356A3
公开(公告)日：2013-01-24
申请号：PCT/IB2012000410
申请日：2012-03-06
申请人： JUBILANT LIFE SCIENCES LTD , BISWAS SUJAY , DUBEY SHAILENDRA KUMAR , BANSAL VIKAS , MASAND MUKESH , VIR DHARAM
发明人： BISWAS SUJAY , DUBEY SHAILENDRA KUMAR , BANSAL VIKAS , MASAND MUKESH , VIR DHARAM
IPC分类号： C07D223/22 , A61K31/55 , A61P25/00
CPC分类号： C07D223/28 , C07D223/22 , Y10T428/2982
摘要： The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(-)-10-hydroxy-dihydrodibenz[b, f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The- present invention also provides use of thus prepared (S)-(+)- or (R)-(-)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(-)-10-acetoxy-10,11-dihydro-5H-dibenz[b, f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J1, J2, J3, J4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof. The novel solid state forms of eslicarbazepine are useful for the preparation of derivatives of eslicarbazepine such as eslicarbazepine acetate.
摘要翻译：本发明提供一种制备取代的光学纯的（S） - （+） - 或（R） - （ - ） - 10-羟基 - 二氢二苯并[b，f]吖庚因或其衍生物的新方法，使用硼酸酯或其衍生物的1,4-二氢-10-氧代-5H-二苯并[b，f]吖庚因。本发明还提供如此制备的（S） - （+） - 或（R） - （ - ） - 10-羟基 - 二氢二苯并[b，f]吖庚因用于制备其酯的用途，例如（S） - （ - ） - 10-乙酸基-10,11-二氢-5H-二苯并[b，f]吖庚因-5-甲酰胺或（R） - （+） - 10-乙酰氧基-10,11-二氢-5H-二苯并[ b，f]氮杂-5-甲酰胺。本发明还提供新颖的固态晶形J1，J2，J3，J4和无定形形式的西拉西平及其制备方法。此外，本发明提供了新型固体晶型和无定形形式的醋酸西酞必利及其制备方法。西拉西平的新型固态形式可用于制备西拉西平的衍生物，如醋酸西拉西平。

4. 发明申请

WO2007054978A2 PROCESS FOR PREPARING PAROXETINE HYDROCHLORIDE HEMIHYDRATE 审中-公开
标题翻译：制备环氧氯丙烷硫酸氢盐的方法
公开(公告)号：WO2007054978A2
公开(公告)日：2007-05-18
申请号：PCT/IN2006000446
申请日：2006-11-10
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
发明人： DUBEY SHAILENDRA KUMAR , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
IPC分类号： C07D405/02
CPC分类号： C07D405/12
摘要： Disclosed herein a process for the preparation of crystalline paroxetine hydrochloride in hemihydrate form employing a selective solvent system to achieve stable and non- hygroscopic form which is easy to prepare and convenient to operate on commercial scale.
摘要翻译：本文公开了以半水合物形式制备结晶帕罗西汀盐酸盐的方法，其采用选择性溶剂体系以实现易于制备和方便在商业规模下操作的稳定和非吸湿性形式。

5. 发明申请

WO2006070396A1 PROCESS FOR PRODUCING 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON2-YL)METHYL] PIPERIDINE OR ITS SALT THEREOF VIA NOVEL INTERMEDIATE 审中-公开
标题翻译：通过新型中间体生产1-苄基-4 - [（5,6-二甲氧基-1-吲哚-2-基）甲基]哌啶或其盐的方法
公开(公告)号：WO2006070396A1
公开(公告)日：2006-07-06
申请号：PCT/IN2004/000433
申请日：2004-12-30
申请人： JUBILANT ORGANOSYS LIMITED , DUBEY, Shailendra, Kumar , SHARMA, Amit, Kumar , RANI, Beena, S. , PAUL, Soumendu , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar , KHANNA, Jag, Mohan
发明人： DUBEY, Shailendra, Kumar , SHARMA, Amit, Kumar , RANI, Beena, S. , PAUL, Soumendu , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar , KHANNA, Jag, Mohan
IPC分类号： C07D211/70 , C07D211/82
CPC分类号： C07D213/89 , C07D211/22
摘要： Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.
摘要翻译：本文公开了使用新型中间体生产1-苄基-4 - [（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶或其盐的方法。

6. 发明申请

WO2005076749A3 A NOVEL PROCESS FOR THE PREPARATION OF 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE 审中-公开
标题翻译：制备1-苄基-4 - [（5,6-二甲氧基-1-吲哚-2-基）甲基]哌嗪的新工艺
公开(公告)号：WO2005076749A3
公开(公告)日：2006-06-08
申请号：PCT/IN2005000044
申请日：2005-02-11
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
发明人： DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
IPC分类号： C07D211/02 , C07D211/32 , C07D211/70
CPC分类号： C07D211/02 , C07D211/32 , C07D211/70
摘要： Disclosed herein is the novel process for producing 1-benzyl-4-(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (donepezil) of formula [I] by treating novel starting compound 1,2,3,6-tetrahydropyridine derivative of formula [V] with 5,6-dimethoxy-1-indanone of formula [IV] to obtain an intermediate 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]-1,2,3,6-tetrahydro pyridine of formula [II] and reducing the same to produce 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine of formula [I]. The invention further comprising the process for preparation of the novel compound of formula [V].
摘要翻译：本文公开了通过处理新的起始化合物1,2,3（1）的新型制备式[I]的1-苄基-4-（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶（多奈哌齐）式[Ⅴ]的6-四氢吡啶衍生物与式[Ⅳ]的5,6-二甲氧基-1-二氢茚酮得到中间体1-苄基-4 - [（5,6-二甲氧基-1-茚满酮基）甲基 ] -1,2,3,6-四氢吡啶并将其还原，得到式（I）的1-苄基-4 - [（5,6-二甲氧基-1-茚满-2-基）甲基]哌啶 [一世]。本发明还包括制备式[Ⅴ]新化合物的方法。

7. 发明申请

WO2012120356A2 PROCESS FOR THE PREPARATION OF (S)-(+)-OR (R)-(-)-10 HYDROXY DIHYDRODIBENZ[B,F]AZEPINES BY ENANTIOSELECTIVE REDUCTION OF 10, 11-DIHYDRO-10-OXO-5H-DIBENZ[B,F]AZEPINES AND POLYMORPHS THEREOF 审中-公开
标题翻译：通过选择性还原10,11-二氢-10-OXO-5H-二苯并[b]的（S） - （+） - 或（R） - （ - ） - 10-羟基二氢苯并[B，F] ，F] AZEPINES和POLYMORPHS
公开(公告)号：WO2012120356A2
公开(公告)日：2012-09-13
申请号：PCT/IB2012/000410
申请日：2012-03-06
申请人： JUBILANT LIFE SCIENCES LIMITED , BISWAS,. Sujay , DUBEY, Shailendra Kumar , BANSAL, Vikas , MASAND, Mukesh , VIR, Dharam
发明人： BISWAS,. Sujay , DUBEY, Shailendra Kumar , BANSAL, Vikas , MASAND, Mukesh , VIR, Dharam
IPC分类号： C07D223/22
CPC分类号： C07D223/28 , C07D223/22 , Y10T428/2982
摘要： The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(-)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(-)- 10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(-)- 10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide, or (R)-(+)-10-acetoxy- 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J 1 , J 2 , J 3 , J 4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof. The novel solid state forms of eslicarbazepine are useful for the preparation of derivatives of eslicarbazepine such as eslicarbazepine acetate.
摘要翻译：本发明提供一种制备取代的光学纯的（S） - （+） - 或（R） - （ - ） - 10-羟基 - 二氢二苯并[b，f]吖庚因或其衍生物的新方法，使用硼酸酯或其衍生物的1,4-二氢-10-氧代-5H-二苯并[b，f]吖庚因。本发明还提供如此制备的（S） - （+） - 或（R） - （ - ） - 10-羟基 - 二氢二苯并[b，f]吖庚因用于制备其酯的用途，例如（S） - （ - ） - 10-乙酰氧基-10,11-二氢-5H-二苯并[b，f]吖庚因-5-甲酰胺或（R） - （+） - 10-乙酰氧基-10,11-二氢-5H-二苯并[ b，f]氮杂-5-甲酰胺。本发明还提供新颖的固态晶形J1，J2，J3，J4和无定形形式的西拉西平及其制备方法。此外，本发明提供了新型固体晶型和无定形形式的醋酸西酞必利及其制备方法。西拉西平的新型固态形式可用于制备西拉西平的衍生物，如醋酸西拉西平。

8. 发明申请

WO2009013764A3 PROCESS FOR PRODUCING 6(R)-[2-(8'(S)-2 ",2 "-DIMETHYLBUTYRYLOXY-2'(S),6'(R)-DIMETHYL-1,2,6,7', 8',8A'(R)- HEXAHYDRONAPHTHYL-L'(S))ETHYL]-4(R)-HYDROXY-3,4,5,6- TETRAHYDRO-2H-PYRAN-2-ONE 审中-公开
标题翻译：制备6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - 二甲基-1,2,6,7'，8 '，8A'（R） - 十六氢萘基-L'（S））乙基] -4（R） - 羟基-3,4,5,6-四氢-2H-吡喃-2-酮
公开(公告)号：WO2009013764A3
公开(公告)日：2009-03-19
申请号：PCT/IN2008000467
申请日：2008-07-24
申请人： JUBILANT ORGANOSYS LTD , SINGH HARNAM , DUBEY SHAILENDRA KUMAR , GUPTA NITIN , DUBEY SUSHIL KUMAR
发明人： SINGH HARNAM , DUBEY SHAILENDRA KUMAR , GUPTA NITIN , DUBEY SUSHIL KUMAR
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： Disclosed herein is an improved process for producing HMG-CoA reductase inhibitor, 6(R)-[2-(8 '(S)-2 ",2 ''-dimethylbutyryloxy-2'(S),6 '(R)-dimethyl- 1', 2', 6', 7', 8',8a'(R)-hexahydronaphthyl-r(S))ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-one, the process comprising hydrolyzing (lS,3R,7S,8S,8aR)-8-{2-[(2R,4R)- 4-hydroxy-6-oxotetrahydro-2H-?yran-2-yl]ethyl}-3,7-dimethyl-l,2,3,7,8,8a- hexahydronaphthalen-1-yl (2S)-2-methylbutanoate in presence of a base and antioxidant, lactonizing and selectively protecting the hydroxyl group of the resultant compound, followed by acylation with an acylating agent to obtain 6(R)-[2-(8'(S)- 2",2''-dimethylbutyryloxy-2 '(S),6 '(R)-dimethyl- 1',2',6',7',8',8a'(R)- hexahydronaphthyl-r(S))ethyl]-4(R)-substituted)-3,4,5,6-tetrahydro-2H-pyran-2-one and further deprotection to obtain 6(R)-[2-(8'(S)-2",2"-dimethylbutyryloxy- 2'(S),6'(R)-dimethyl-1',2',6',7',8',8a'(R)-hexahydronaphthyl-1'(S))ethyl]-4(R)- hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
摘要翻译：本文公开了一种生产HMG-CoA还原酶抑制剂，6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - （R） - 六氢萘基-r（S））乙基] -4（R） - 羟基-3,4,5,6-四氢 - （1S，3R，7S，8S，8aR）-8- {2 - [（2R，4R）-4-羟基-6-氧代四氢-2H-哒嗪-2 - 基]乙基} -3,7-二甲基-1,2,3,7,8,8a-六氢萘-1-基（2S）-2-甲基丁酸酯在碱和抗氧化剂存在下，内酯化和选择性保护羟基然后用酰化剂酰化，得到6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - 二甲基-1'，2'，6'，7'，8'，8a'（R） - 六氢萘基-r（S））乙基] -4（R） - 取代的）四氢-2H-吡喃-2-酮，进一步脱保护，得到6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） -1'，2'，6'，7'，8'，8a'（R） - 六氢萘基-1'（S））乙基] -4（R） - 羟基-3,4,5,6-四氢 - -2H-吡喃-2-酮。

9. 发明申请

WO2007054978A3 PROCESS FOR PREPARING PAROXETINE HYDROCHLORIDE HEMIHYDRATE 审中-公开
公开(公告)号：WO2007054978A3
公开(公告)日：2007-05-18
申请号：PCT/IN2006/000446
申请日：2006-11-10
申请人： JUBILANT ORGANOSYS LIMITED , DUBEY, Shailendra, Kumar , KUMAR, Pramod , DUBEY, Sushil, Kumar
发明人： DUBEY, Shailendra, Kumar , KUMAR, Pramod , DUBEY, Sushil, Kumar
IPC分类号： C07D405/12
摘要： Disclosed herein a process for the preparation of crystalline paroxetine hydrochloride in hemihydrate form employing a selective solvent system to achieve stable and non- hygroscopic form which is easy to prepare and convenient to operate on commercial scale.

10. 发明申请

WO2006111983A2 NOVEL POLYMORPHIC FORM OF (l-BENZYL-4-[(5,6-DIMETHOXY-l- INDANONE)-2-YL]METHYL PIPERIDINE HYDROCHLORIDE AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：（1-苄基-4 - [（5,6-二甲氧基-1-吲哚酮）-2-基]甲基哌啶盐酸氢盐的新型多晶型及其制备方法
公开(公告)号：WO2006111983A2
公开(公告)日：2006-10-26
申请号：PCT/IN2006000136
申请日：2006-04-21
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , GUPTH POORVI , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
发明人： DUBEY SHAILENDRA KUMAR , GUPTH POORVI , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
CPC分类号： C07D211/32
摘要： Disclosed herein are novel and stable polymorphic form of Donepezil Hydrochloride, wherein said polymorphic form is designated as J and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic form and use thereof to prepare another forms is also disclosed.
摘要翻译：本文公开了多奈哌齐盐酸盐的新颖且稳定的多晶型物，其中所述多晶型物称为J，其特征在于它们的粉末X射线衍射图，红外吸收光谱，热重分析和差示扫描量热法。还公开了制备所述多晶形式及其用途以制备另一种形式的方法。

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