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1. 发明申请

WO2011092564A3 PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES 审中-公开
标题翻译：制备纤维素及其中间体的方法
公开(公告)号：WO2011092564A3
公开(公告)日：2011-12-01
申请号：PCT/IB2011000084
申请日：2011-01-20
申请人： FRESENIUS KABI ONCOLOGY LTD , GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
发明人： GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
IPC分类号： C07D319/06 , C07D498/18
CPC分类号： C07D498/18 , C07D319/06
摘要： Intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).
摘要翻译：中间体，其制备方法及其在制备治疗有效的抗肿瘤药物中的用途，特别是式（I）的替西罗莫司。

2. 发明申请

WO2008018091A1 PROCESS FOR PRODUCING SULPHOXIDE COMPOUNDS 审中-公开
标题翻译：生产硫化氧化合物的方法
公开(公告)号：WO2008018091A1
公开(公告)日：2008-02-14
申请号：PCT/IN2007/000335
申请日：2007-08-08
申请人： JUBILANT ORGANOSYS LIMITED , SINGH, Anand , SINGH, Khushwant , DUBEY, Sushil, Kumar
发明人： SINGH, Anand , SINGH, Khushwant , DUBEY, Sushil, Kumar
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Disclosed herein, a process for producing sulphoxide compound of the Formula (I) by asymmetrically oxidizing a prochiral sulphide of the Formula (II) with an effective amount of oxidizing agent in the presence of a chiral transition metal complex without using an organic solvent and base.
摘要翻译：本文公开了一种通过在手性过渡金属络合物的存在下用有效量的氧化剂不对称地氧化式（II）的前手性硫化物而制备式（I）的亚砜化合物的方法，而不使用有机溶剂和碱。

3. 发明申请

WO2008012837A1 PROCESS FOR PRODUCING 10-OXO-L10, 11-DIHYDR0-5H-DIBENZ [B, F] AZEPINE-5-CARBOXAMIDE STARTING FROM 5-CYANOIMINOSTILBENE 审中-公开
标题翻译：从5-氰基咪唑开始制备10-OXO-L10,11-二氢-5H-二苯并[B，F]氮杂卓-5-羧酰胺的方法
公开(公告)号：WO2008012837A1
公开(公告)日：2008-01-31
申请号：PCT/IN2007/000307
申请日：2007-07-24
申请人： JUBILANT ORGANOSYS LIMITED , SINGH, Harnam , GUPTA, Nitin , KUMAR, Parmod , DUBEY, Sushil, Kumar
发明人： SINGH, Harnam , GUPTA, Nitin , KUMAR, Parmod , DUBEY, Sushil, Kumar
IPC分类号： C07D223/26 , C07D223/28
CPC分类号： C07D223/26 , C07D223/28
摘要： Disclosed herein is a process for producing 10-oxo-10,11-dihydro-5H-dibenz[ bf ] azepine-5-carboxamide of formula I via novel intermediates 11-alkoxy-10-halo-10,11-dihydro-5H-dibenzo [ b,f ] azepine-5-carbonitrile [XIX] or 10-alkoxy-5H-dibenz [ b,f ] azepine -5-carbonitrile [XX]. Further the present invention also provides a process for preparation of said intermediates.
摘要翻译：本文公开了通过新中间体11生产式I的10-氧代-10,11-二氢-5H-二苯并[b] az -5-甲酰胺的方法 - 烷氧基-10-卤代-10,11-二氢-5H-二苯并[b，f]吖庚因-5-腈[XIX]或10-烷氧基-5H-二苯并[b， f]吖庚因-5-腈[XX]。此外，本发明还提供了制备所述中间体的方法。

4. 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.

5. 发明申请

WO2006067795A2 NOVEL POLYMORPHIC FORMS OF ATORVASTATIN LACTONE AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：异烟肼的新型多形态及其制备方法
公开(公告)号：WO2006067795A2
公开(公告)日：2006-06-29
申请号：PCT/IN2004/000401
申请日：2004-12-23
申请人： JUBILANT ORGANOSYS LIMITED , BHATRAJU, Sreenivas, Rao , DUA, Annu , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
发明人： BHATRAJU, Sreenivas, Rao , DUA, Annu , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
IPC分类号： A61K31/401
CPC分类号： C07D405/06
摘要： The present invention provides novel crystalline polymorphic Forms and amorphous Form of atorvastatin lactone, characterized by powder X-ray diffraction pattern and Infrared absorption spectrum. The novel processes for their preparation are also disclosed.
摘要翻译：本发明提供了阿托伐他汀内酯的新型结晶多晶型和无定形形式，其特征在于粉末X射线衍射图和红外吸收光谱。还公开了其制备的新方法。

6. 发明申请

WO2006027789A1 PROCESS FOR PRODUCING 11-[4-[2-(2-HYDROXYETHOXY)ETHYL]-1-PIPERAZINYL]DIBENZO[b,f][1,4]THIAZEPINE AND A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：制备11- [4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基]二苯并[b，f] [1,4]噻吩及其药物可接受的盐的方法
公开(公告)号：WO2006027789A1
公开(公告)日：2006-03-16
申请号：PCT/IN2004/000281
申请日：2004-09-08
申请人： JUBILANT ORGANOSYS LIMITED , PATHAK, Shailendra , SHARMA, Jitendra , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
发明人： PATHAK, Shailendra , SHARMA, Jitendra , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
IPC分类号： C07D281/02
CPC分类号： C07D281/16
摘要： A process for producing 11-[4-[2-(2-hydroxyethoxy)ethyl]-l-piperazinyl]dibenzo [b,f][1,4]thiazepine [I] and a pharmaceutically suitable acid addition salt is disclosed. Accordingly, thiosalicylic acid [XVI] is reacted with o-halonitrobenzene [XVII] using a phase transfer catalyst to obtain 2-nitro-2'-carboxydiphenylsulphide [XI]. It is hydrogenated in the presence of a noble metal catalyst to obtain 2-amino-2' carboxydiphenyl sulphide [X]. The 2-amino-2'-carboxydiphenylsulphide [X] is reacted with halide or oxyhalide of the phosphorous to obtain in situ iminohalide [VI], which further reacts as such with 1-hydroxyethoxyethylpiperazine or condenses with piperazine to obtain 11-piperazinyldi.benzo[b,f][1,4]thiazepine [XIX] which further reacts with 2- chloroethoxyethanol or reacts with 1-(2-hydroxyethyl)piperazine to give 11-[4-(2-hydroxyethyl)piperazine-1-yl]dibenzo[b,f][ 1,4]thiazepine [XXXI] which further converts to an intermediate 11-[4-(2-substitutedethyl)piperazin-1- yl)dibenzo[b,f][1,4]thiazepine wherein the substituent at the 2-position is selected from mesyloxy or tosyloxy or halo group [XXXII] followed by reaction with ethylene glycol to give quetiapine [1].
摘要翻译：公开了制备11- [4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基]二苯并[b，f] [1,4]硫氮杂] [I]和药学上合适的酸加成盐的方法。因此，使用相转移催化剂将硫代水杨酸[XVI]与邻硝基苯[XVII]反应，得到2-硝基-2'-羧基二苯基硫化物[XI]。在贵金属催化剂存在下氢化得到2-氨基-2'-羧基二苯基硫醚[X]。将2-氨基-2'-羧基二苯基硫化物[X]与磷的卤化物或卤氧化物反应，得到原位亚氨基卤[VI]，其进一步与1-羟基乙氧基乙基哌嗪反应或与哌嗪缩合，得到11-哌嗪基二苯并 [b，f] [1,4]硫氮杂[XIX]，其进一步与2-氯乙氧基乙醇反应或与1-（2-羟乙基）哌嗪反应，得到11- [4-（2-羟乙基）哌嗪-1-基] 二苯并[b，f] [1,4]硫氮杂[XXXI]，其进一步转化为中间体11- [4-（2-取代乙基）哌嗪-1-基）二苯并[b，f] [1,4] 2位上的取代基选自甲磺酰氧基或甲苯磺酰氧基或卤代基[ⅩⅩⅫ]，随后与乙二醇反应得到喹硫平[1]。

7. 发明申请

WO2005077928A1 IMPROVED PROCESS FOR PRODUCING SIMVASTATIN 审中-公开
标题翻译：改进生产SIMVASTATIN的方法
公开(公告)号：WO2005077928A1
公开(公告)日：2005-08-25
申请号：PCT/IN2005/000043
申请日：2005-02-11
申请人： JUBILANT ORGANOSYS LIMITED , BHADWAL, Paramvir , JAIN, Pratima , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar , KHANNA, Jag, Mohan
发明人： BHADWAL, Paramvir , JAIN, Pratima , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar , KHANNA, Jag, Mohan
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： Disclosed herein is an industrially feasible process for producing HMG-CoA reductase inhibitor, simvastatin, via an improved acylation process using lovastatin ammonium salt as a starting material. The process comprising treating lovastatin ammonium salt with a base to obtain the compound of formula [III], lactonizing the compound of the formula [III] to obtain compound of formula [IV], selectively protecting the hydroxyl group of the compound of formula [IV] to obtain compound of formula [V], acylating the compound of formula [V] with dimethylbutyrylchloride using potassium halide in presence of a solvent to obtain compound of formula [VI], deprotecting compound of formula [VI] followed by hydrolysis to obtain simvastatin ammonium salt of formula [VII] which is lactonized to obtain simvastatin.
摘要翻译：本文公开了通过使用洛伐他汀铵盐作为起始原料的改进的酰化方法来生产HMG-CoA还原酶抑制剂辛伐他汀的工业上可行的方法。该方法包括用碱处理洛伐他汀铵盐以获得式[III]化合物，将式[Ⅲ]化合物内酯化得到式[Ⅳ]化合物，选择性保护式[Ⅳ]化合物的羟基 ]得到式[Ⅴ]化合物，在溶剂存在下，使用卤化钾，用二甲基丁酰氯酰化式[Ⅴ]化合物，得到式[Ⅵ]化合物，将式[Ⅵ]化合物脱保护，然后水解得到辛伐他汀式[Ⅶ]铵盐，其被内酯化以获得辛伐他汀。

8. 发明申请

WO02088149A3 A PROCESS FOR MANUFACTURE OF FOSINOPRIL SODIUM 审中-公开
标题翻译：一种制造FOSINOPRIL SODIUM的方法
公开(公告)号：WO02088149A3
公开(公告)日：2003-06-05
申请号：PCT/IN0100144
申请日：2001-08-17
申请人： LUPIN LAB LTD , DUBEY SUSHIL KUMAR , LAHIRI SASWATA , SINGH ANIL VIR
发明人： DUBEY SUSHIL KUMAR , LAHIRI SASWATA , SINGH ANIL VIR
IPC分类号： C07B57/00 , C07B61/00 , C07F9/572
CPC分类号： C07F9/5721
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.
摘要翻译：本发明公开了一种在两个步骤中合成作为高纯度的单一所需异构体的福辛普利的方法，包括（a）以四种非对映异构体的混合物制备福辛普利，和（b）通过形成从所述混合物中分离所需的异构体的碱金属盐，随后结晶。

9. 发明申请

WO2011092564A4 PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES 审中-公开
标题翻译：制备TEMSIROLIMUS及其中间体的方法
公开(公告)号：WO2011092564A4
公开(公告)日：2012-01-19
申请号：PCT/IB2011000084
申请日：2011-01-20
申请人： FRESENIUS KABI ONCOLOGY LTD , GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
发明人： GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
IPC分类号： C07D319/06 , C07D498/18
CPC分类号： C07D498/18 , C07D319/06
摘要： Intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).
摘要翻译：中间体，它们的制备方法以及它们在制备治疗有效的抗肿瘤剂，特别是式（I）的坦罗莫司酯中的用途。

10. 发明申请

WO2010084516A1 PROCESS FOR PRODUCING OPTICALLY ACTIVE N-ALKYL-PIPERIDINE-2-CARBOXANILIDE 审中-公开
标题翻译：生产光学活性N-烷基 - 哌啶-2-羧酸酰亚胺的方法
公开(公告)号：WO2010084516A1
公开(公告)日：2010-07-29
申请号：PCT/IN2010/000039
申请日：2010-01-22
申请人： JUBILANT ORGANOSYS LIMITED , THANKI, Bhavin, Prabhudas , SINGH, Harinder , SINGH, Anand, Kumar , SINGH, Khushwant , DUBEY, Sushil, Kumar
发明人： THANKI, Bhavin, Prabhudas , SINGH, Harinder , SINGH, Anand, Kumar , SINGH, Khushwant , DUBEY, Sushil, Kumar
IPC分类号： C07D211/60
CPC分类号： C07D211/60
摘要： Disclosed herein is a process for producing optically active 1-n-propyl-2',6'-dimethyl-2-piperidinecarboxanilide. The process comprises of reacting n -propyl pipecolate ester with 2,6-dimethylanilino magnesium halide. The 1-n-propyl-2',6'-dimethyl-2-piperidinecarboxanilide obtained according to the process is having chiral purity of more than 97%.
摘要翻译：本文公开了一种光学活性1-正丙基-2'，6'-二甲基-2-哌啶甲酰苯胺的制备方法。该方法包括使正丙基哌可酸酯与2,6-二甲基苯胺基卤化镁反应。根据该方法获得的1-正丙基-2'，6'-二甲基-2-哌啶甲酰苯胺具有大于97％的手性纯度。

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