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1. 发明申请

WO2009118655A3 HIGHLY PURE PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF KETO IMPURITY 审中-公开
标题翻译：高纯度PALIPERIDONE或其药物接受盐，其实质上不含KETO污染物
公开(公告)号：WO2009118655A3
公开(公告)日：2009-12-03
申请号：PCT/IB2009005479
申请日：2009-03-26
申请人： ACTAVIS GROUP PTC EHF , BAPAT UDAY RAJARAM , JAYAMANI MUNUSAMY , RAVISARAVANAN SIVAJI , SODHA VISHAL AMRUTLAL , VALGEIRSSON JON
发明人： BAPAT UDAY RAJARAM , JAYAMANI MUNUSAMY , RAVISARAVANAN SIVAJI , SODHA VISHAL AMRUTLAL , VALGEIRSSON JON
IPC分类号： C07D471/04 , A61K31/517 , A61P25/18
CPC分类号： C07D471/04
摘要： Provided herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity,3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-y1)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity.
摘要翻译：本文提供的是基本上不含酮杂质的高纯度普利培酮或其药学上可接受的盐，3- [2- [4-（6-氟-1,2-苯并异恶唑-3-基）-1-哌啶基]乙基] 2-甲基-7,8-二氢-6H-吡啶并[1,2-a]嘧啶-4,9-二酮，其制备方法和药物组合物，其包含高度纯的普利培酮或其药学上可接受的盐，其基本上不含的酮杂质。

2. 发明申请

WO2008087557A3 AN IMPROVED PROCESS FOR PREPARATION OF 9-HYDROXY-3-(2-CHLOROETHYL)- 2-METHYL-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE HYDROCHLORIDE 审中-公开
标题翻译：制备9-羟基-3-（2-氯苯乙基）-2-甲基-4H-吡啶并[1,2-A]嘧啶-4-酮氢氯酸盐的改进方法
公开(公告)号：WO2008087557A3
公开(公告)日：2009-02-19
申请号：PCT/IB2008000626
申请日：2008-01-08
申请人： ACTAVIS GROUP PTC EHF , BAPAT UDAY RAJARAM , JAYAMANI MUNUSAMY , RAVISARAVANAN SIVAJI , RAVISANKAR VIGNESHWARA
发明人： BAPAT UDAY RAJARAM , JAYAMANI MUNUSAMY , RAVISARAVANAN SIVAJI , RAVISANKAR VIGNESHWARA
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2- methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield.
摘要翻译：本文描述了改进的，商业上可行的和工业上有利的制备利培酮中间体9-羟基-3-（2-氯乙基）-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮的方法和其盐酸盐。与先前公开的方法相比，该方法提供了较高产率的帕培培酮中间体和缩短的反应时间，由此提供了高纯度和高产率的利培酮及其药学上可接受的酸加成盐的生产。

3. 发明申请

WO2009056990A2 PALIPERIDONE POLYMORPHS 审中-公开
公开(公告)号：WO2009056990A2
公开(公告)日：2009-05-07
申请号：PCT/IB2008003775
申请日：2008-08-20
申请人： ACTAVIS GROUP PTC EHF , BAPAT UDAY RAJARAM , MUNUSAMY JAYAMANI , RAVISARAVANAN SIVAJI , RAVISANKAR VIGNESHWARA , VALGEIRSSON JON
发明人： BAPAT UDAY RAJARAM , MUNUSAMY JAYAMANI , RAVISARAVANAN SIVAJI , RAVISANKAR VIGNESHWARA , VALGEIRSSON JON
IPC分类号： C07D471/04 , A61K31/517 , A61P25/18
CPC分类号： C07D471/04 , A61K9/145 , A61K31/517
摘要： Described herein are novel polymorphic forms of paliperidone, processes for preparing the novel forms and use thereof. Also provided are processes for the preparation of novel polymorphic forms of paliperidone and the use thereof in the preparation of pharmaceutical compositions.
摘要翻译：本文描述的是利培酮的新型多晶型物，其制备方法及其用途。还提供了制备帕培他酮的新型多晶型物的方法及其在制备药物组合物中的用途。

4. 发明申请

WO2008152514A3 PROCESS FOR THE PREPARATION OF ALFUZOSIN AND SALTS THEREOF 审中-公开
标题翻译：制备阿霉素及其盐的方法
公开(公告)号：WO2008152514A3
公开(公告)日：2009-02-19
申请号：PCT/IB2008002340
申请日：2008-05-02
申请人： ACTAVIS GROUP PTC EHF , BAPAT UDAY RAJARAM , POTAMS JOSE PAUL , SUBRAMANIAN NARASIMHAN , VALGEIRSSON JON
发明人： BAPAT UDAY RAJARAM , POTAMS JOSE PAUL , SUBRAMANIAN NARASIMHAN , VALGEIRSSON JON
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： The present invention relates to novel N-[3-[(4-acyl-/aroyl-substituted amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furancarboxamide derivatives, and a process for the preparation thereof. The novel compounds are useful for preparing alfuzosin or a pharmaceutically acceptable salt thereof in high yield and purity.
摘要翻译：本发明涉及新的N- [3 - [（4-酰基 - /芳酰基取代的氨基-6,7-二甲氧基-2-喹唑啉基）甲基氨基]丙基]四氢-2-呋喃甲酰胺衍生物及其制备方法它们。新化合物可用于以高产率和纯度制备阿夫唑嗪或其药学上可接受的盐。

5. 发明申请

WO03068142A2 NOVEL ANTI-FUNGAL AGENTS 审中-公开
标题翻译：新型抗真菌药剂
公开(公告)号：WO03068142A2
公开(公告)日：2003-08-21
申请号：PCT/IN0300024
申请日：2003-02-11
申请人： FDC LTD , CHANDAVARKAR MOHAN A , KULKARNI VITHAL MADHAVRAO , SHIVKUMAR PRANAVKUMAR , SHETTY RAVINDRA S , BAPAT UDAY RAJARAM
发明人： CHANDAVARKAR MOHAN A , KULKARNI VITHAL MADHAVRAO , SHIVKUMAR PRANAVKUMAR , SHETTY RAVINDRA S , BAPAT UDAY RAJARAM
IPC分类号： A61P31/00 , C07D403/06 , A61K
CPC分类号： C07D403/06
摘要： The invention relates to novel antifungal compounds and its pharmaceutically acceptable salts., having as part of its structure, imidazolyl or benzimidazolyl derivatives. The imidazolyl derivative may be substituted at 2 position from among the group consisting of aroyl, p-chloroaroyl, phenyl hydroxy methine or p-chloro phenyl hydroxy methine or with n-butyl at 2 position and chlorine at 4 and 5 position. In the alternative , when it is a benzimadazolyl derivative, with hydrogen at 6 position, the substituent at 2 position may be selected from among methyl, ethyl, isopropyl, 2-oxoprop-1-yl, n-propyl, methoxy methyl, propen-1-yl, phenyl, p-chlorophenyl, p-toluyl, benzyl, 4-pyridyl, p-methoxy phenyl, 3-pyridyl, o-methoxy phenyl, styryl, 2-cyano methyl, p-hydroxy phenyl, p-amino phenyl, p-toluyl sulfonyl methyl or p-(t-butyl) phenyl group and if hydrogen is at 2 position, the substituent at the 6 position is selected from among nitro, trifluoromethyl or methoxy group.
摘要翻译：本发明涉及作为其结构部分的咪唑基或苯并咪唑衍生物的新型抗真菌化合物及其药学上可接受的盐。咪唑基衍生物可以在由芳酰基，对氯芳酰基，苯基羟基次甲基或对氯苯基羟基次甲基组成的组中的2位或与2位的正丁基和4和5位的氯取代。在另一种情况下，当是6位的氢时的苯并恶唑基衍生物时，2位上的取代基可以选自甲基，乙基，异丙基，2-氧代丙-1-基，正丙基，甲氧基甲基，苯基，对氯苯基，对甲苯基，苄基，4-吡啶基，对甲氧基苯基，3-吡啶基，邻甲氧基苯基，苯乙烯基，2-氰基甲基，对羟基苯基，对氨基苯基，对甲苯磺酰基甲基或对 - （叔丁基）苯基，如果氢在2位，6位上的取代基选自硝基，三氟甲基或甲氧基。

6. 发明申请

WO2012017391A3 NOVEL COMPOUNDS AS DPP-IV INHIBITORS AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：新化合物作为DPP-IV抑制剂及其制备方法
公开(公告)号：WO2012017391A3
公开(公告)日：2016-05-26
申请号：PCT/IB2011053443
申请日：2011-08-03
申请人： CADILA PHARMACEUTICALS LTD , KHAMAR BAKULESH MAFATLAL , JOSHI NIRAV KISHORBHAI , SINGH CHANDAN HARDHAN , BAPAT UDAY RAJARAM , GADHIYA BIPIN DHANJIBHAI , SAGAR NIRAV SURESHBHAI , MODI INDRAVADAN AMBALAL
发明人： KHAMAR BAKULESH MAFATLAL , JOSHI NIRAV KISHORBHAI , SINGH CHANDAN HARDHAN , BAPAT UDAY RAJARAM , GADHIYA BIPIN DHANJIBHAI , SAGAR NIRAV SURESHBHAI , MODI INDRAVADAN AMBALAL
IPC分类号： A01N43/42 , A61K31/47 , C07D295/00
CPC分类号： C07D487/04 , C07D207/16 , C07D209/52 , C07K1/10 , C07K5/0202
摘要： The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶抑制剂的新化合物的制备方法，并由下列结构式描述：式VI。其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是2型糖尿病。

7. 发明申请

WO2010082110A2 NOVEL PROCESS FOR PREPARING PURE 6-FLUORO-3-PIPERIDIN-4-YL-1,2-BENZISOXAZOLE HYDROCHLORIDE AND ITS CONVERSION TO PALIPERIDONE 审中-公开
标题翻译：制备纯的6-氟-3-哌啶-4-基-1,2-苯并恶唑盐酸盐的新方法及其对哌啶酮的转化
公开(公告)号：WO2010082110A2
公开(公告)日：2010-07-22
申请号：PCT/IB2010000041
申请日：2010-01-12
申请人： CADILA PHARMACEUTICALS LTD , SODAGAR KEVAL RAMESHCHANDRA , MALIK VINEET , KAPADIA BRIJESH NITINKUMAR , JAIN SUDHIR HUKAMCHAND , PARIKH SANJAY NATVARLAL , SHARMA ARUN OMPRAKASH , BAPAT UDAY RAJARAM , KHAMAR BAKULESH MAFATIAL
发明人： SODAGAR KEVAL RAMESHCHANDRA , MALIK VINEET , KAPADIA BRIJESH NITINKUMAR , JAIN SUDHIR HUKAMCHAND , PARIKH SANJAY NATVARLAL , SHARMA ARUN OMPRAKASH , BAPAT UDAY RAJARAM , KHAMAR BAKULESH MAFATIAL
IPC分类号： C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to novel process for providing substantially pure 6-Fluoro-3- piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to Paliperidone having dimer compound of structural formula-1 A is less than 0.2 % and HPLC purity > 99.7%.
摘要翻译：本发明涉及提供基本上纯的6-氟-3-哌啶-4-基-1,2-苯并异恶唑盐酸盐的新方法，并且其具有结构式-A的二聚体化合物的帕利哌酮的转化率小于0.2％且HPLC纯度 > 99.7％。

8. 发明申请

WO2011132140A3 PROCESS FOR THE CONVERSION OF (2R)-6-FLUORO-2-[(2S)-OXIRAN-2-YL]-3,4-DIHYDRO-2H-CHROMENE TO (2R)-6-FLUORO-2-[(2R)-OXIRAN-2-YL]-3,4-DIHYDRO-2H-CHROMENE 审中-公开
标题翻译：（2R）-6-氟-2 - [（2S） - 氧代-2-基] -3,4-二氢-2H-吡喃转化为（2R）-6-氟-2 - [（2R ） - 环氧乙烷-2-基] -3,4-二氢-2H-色烯
公开(公告)号：WO2011132140A3
公开(公告)日：2012-03-08
申请号：PCT/IB2011051685
申请日：2011-04-19
申请人： CADILA PHARMACEUTICALS LTD , KHAMAR BAKULESH MAFATLAL , KAGATHARA NIRAV KESHAVLAL , MUGALE BALAJI , KORIKANA SIVAPRASAD , BAPAT UDAY RAJARAM , MODI INDRAVADAN AMBALAL
发明人： KHAMAR BAKULESH MAFATLAL , KAGATHARA NIRAV KESHAVLAL , MUGALE BALAJI , KORIKANA SIVAPRASAD , BAPAT UDAY RAJARAM , MODI INDRAVADAN AMBALAL
IPC分类号： C07D311/58 , C07D407/04
CPC分类号： C07D311/58
摘要： The present invention relates to a novel process for the conversion of (2R)-6-fluoro- 2-[(2S)-oxiran-2-yl]-3,4-dihydro-2H-chromene (formula lll-A) to (2R)-6-fluoro-2-[(2R)-oxiran- 2-yl]-3,4-dihydro-2H-chromene (formula lll-B). The compound of formula lll-A and formula lll-B are key intermediates for preparing Nebivolol.
摘要翻译：本发明涉及将（2R）-6-氟-2 - [（2S） - 环氧乙烷-2-基] -3,4-二氢-2H-色烯（式III-A）转化为（2R）-6-氟-2 - [（2R） - 环氧乙烷-2-基] -3,4-二氢-2H-色烯（式III-B）。式III-A和式III-B的化合物是制备奈比洛尔的关键中间体。

9. 发明申请

WO2010064134A2 PROCESS OF SYNTHESIS OF PALIPERIDONE 审中-公开
标题翻译： PALIPERIDONE合成方法
公开(公告)号：WO2010064134A2
公开(公告)日：2010-06-10
申请号：PCT/IB2009007652
申请日：2009-12-04
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , SODAGAR KEVAL RAMESHCHANDRA , VINEET MALIK , JAIN SUDHIR HUKAMCHAND , PARIKH SANJAY NATVARLAL , SHARMA ARUN OMPRAKASH , BAPAT UDAY RAJARAM , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , SODAGAR KEVAL RAMESHCHANDRA , VINEET MALIK , JAIN SUDHIR HUKAMCHAND , PARIKH SANJAY NATVARLAL , SHARMA ARUN OMPRAKASH , BAPAT UDAY RAJARAM , KHAMAR BAKULESH MAFATLAL
IPC分类号： C07D487/02
CPC分类号： C07D471/04
摘要： The invention relates to an improved process for preparation of 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one, an intermediate used in the synthesis of paliperidone and process for converting the same to Paliperidone.
摘要翻译：本发明涉及制备3-（2-氯乙基）-9-羟基-2-甲基-6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮的改进方法，一种，用于合成帕潘立酮的中间体及其转化为哌啶酮的方法。

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