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1. 发明专利

JP2008163026A Improved method for producing 8-nitro-2-(1h-tetrazol-5-yl)-4h-1-benzopyran-4-one from 8-nitro-2-cyano-4h-1-benzopyran-4-one and converting resultant product into hydrochloride salt of 8-amino-2-(1h-tetrazol-5-yl)-4h-1-benzopyran-4-one 有权
标题翻译：用于生产8-硝基-2-（1H-四唑-5-基）-4H-1-苯并噻吩-4-酮从8-硝基-2-氰基-4H-1-苯并噻吩-4-酮和转化物质的改进方法产物加入8-氨基-2-（1H-四唑-5-基）-4H-1-苯并噻吩-4-酮的盐酸盐
公开(公告)号：JP2008163026A
公开(公告)日：2008-07-17
申请号：JP2007331615
申请日：2007-12-25
申请人： Cadila Pharmaceuticals Ltd , カディラファーマシューティカルズリミテッド
发明人： MODI INDRAVADAN AMBALAL , KAPADIA BRIJESH NITINBHAI , PARIKH SANJAY NATVARLAL , PANNAIAH RAVI , KHAMAR BAKULESH MAFATLAL
IPC分类号： C07D405/04 , B01J27/138 , C07B61/00
CPC分类号： Y02P20/52
摘要： PROBLEM TO BE SOLVED: To provide an improved method for the conversion of 8-nitro-2-cyano-4H-1-benzopyran-4-one into 8-nitro-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-4-one which uses sodium azide together with a zinc halide in water. SOLUTION: The compound, 8-nitro-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-4-one is further converted into a hydrochloride salt of 8-amino-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-4-one by using stannous chloride in a hydrochloric acid solution. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：为了提供将8-硝基-2-氰基-4H-1-苯并吡喃-4-酮转化为8-硝基-2-（1H-四唑-5-基） -4H-1-苯并吡喃-4-酮，其使用叠氮化钠与卤化锌在水中。解决方案：将8-硝基-2-（1H-四唑-5-基）-4H-1-苯并吡喃-4-酮的化合物进一步转化为8-氨基-2-（1H- 四唑-5-基）-4H-1-苯并吡喃-4-酮，通过在氯化氢溶液中使用氯化亚锡。版权所有（C）2008，JPO＆INPIT

2. 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。

3. 发明申请

WO2010018441A3 PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE TELMISARTAN 审中-公开
标题翻译：制备大量纯TELMISARTAN的方法
公开(公告)号：WO2010018441A3
公开(公告)日：2010-04-08
申请号：PCT/IB2009006505
申请日：2009-08-10
申请人： CADILA PHARMACEUTICALS LTD , KHAMAR BAKULESH MAFATLAL , SIDDIQUI ISHRAT HUSAIN , PONNAIAH RAVI , MODI INDRAVADAN AMBALAL
发明人： KHAMAR BAKULESH MAFATLAL , SIDDIQUI ISHRAT HUSAIN , PONNAIAH RAVI , MODI INDRAVADAN AMBALAL
IPC分类号： C07D235/20
CPC分类号： C07D235/20
摘要： The present invention relates to an improved process for the preparation of substantially pure Telmisartan in polymorphic form A.
摘要翻译：本发明涉及一种用于制备基本上纯的多晶型形式的替米沙坦的改进方法。

4. 发明申请

WO0205746A3 THE PROCESS OF MANUFACTURING PHARMACEUTICAL GRADE TANNATES 审中-公开
标题翻译：制造药物级别的过程
公开(公告)号：WO0205746A3
公开(公告)日：2002-05-02
申请号：PCT/IB0101252
申请日：2001-07-13
申请人： CADILA PHARMACEUTICALS LTD , KHAMAR BAKULESH MAFATLAL , SRINIVASAN CHIDAMBARAM VENKATE , MITRA JAYATI
发明人： KHAMAR BAKULESH MAFATLAL , SRINIVASAN CHIDAMBARAM VENKATE , MITRA JAYATI
IPC分类号： A61K47/12 , C07C69/88
CPC分类号： A61K47/12
摘要： Antihistamines are available in the form of free bases as well as salts i.e. hydrochloride, maleate, tannate etc. Frequently, it is necessary to utilise antihistamines in the form of tannate salt because such salts are generally quite stable and may be administered in such from without untoward side effects. Tannic acid, also known as tannin, is a well known naturally occurring substance. Tannic acid, which is available commercially, usually contain about 5 % of water, has a molecular weight of about 1700 and is typically produced from Turkish or Chinese nutgall. Antihistamine tannates, presently manufactured commercially, are relatively impure. Such tannates are prepared by the reaction of antihistamine free base with tannic acid and using a volatile solvent, isopropanol (IPA). The yield is only fair (around 70 %) and decomposition products e.g. 2-5 % along with significant amount of volatile solvent, isopropanol (6-10 %) remains with the product, which cannot be removed. According to present invention, for specific types of tannates, isopropanol (IPA) is removed by adding water while stirring and dispersing the wet cake of tannate. It is then filtered and the tannate residue is dried to obtain pharmaceutical grade tannate. Tannates like chlorpheniramine tannate and pyrilamine tannates have been prepared by this method.
摘要翻译：抗组胺药以游离碱和盐酸盐，马来酸盐，鞣酸盐等盐的形式提供。通常，有必要利用鞣酸盐形式的抗组胺剂，因为这些盐通常是相当稳定的，可以不经不良副作用。丹宁酸，也称为单宁，是众所周知的天然存在物质。市售的丹宁酸通常含有约5％的水，其分子量约为1700，通常由土耳其或中国的nutgall生产。目前商业上制造的抗组胺药丹宁酸是相对不纯的。通过抗组胺游离碱与鞣酸反应并使用挥发性溶剂异丙醇（IPA）制备此类鞣酸。产量仅为公平（约70％），分解产物例如 2-5％以及显着量的挥发性溶剂，异丙醇（6-10％）仍然残留在产品中，不能除去。根据本发明，对于特定类型的鞣酸酯，通过加水来除去异丙醇（IPA），同时搅拌并分散丹宁酸的湿饼。然后将其过滤并将丹宁酸残余物干燥以获得药物级单宁酸盐。通过这种方法制备了丹宁酸盐，如丹宁酸氯苯那敏和吡拉明丹宁酸盐。

5. 发明公开

EP2555617A4 NOVEL HYPOGLYCEMIC COMPOUNDS 审中-公开
标题翻译：新化合物低血糖的治疗
公开(公告)号：EP2555617A4
公开(公告)日：2013-08-14
申请号：EP11765149
申请日：2011-04-01
申请人： CADILA PHARMACEUTICALS LTD
发明人： KHAMAR BAKULESH MAFATLAL , SINGH CHANDAN , MODI RAJIV INDRAVADAN
IPC分类号： A01N33/26 , A61K31/4985 , C07D209/52 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D473/04 , C07D487/04
CPC分类号： C07D473/04 , A61K31/4985 , A61K47/65 , C07D209/52 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04

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

WO2010035119A3 VACCINE ADJUVANTS 审中-公开
公开(公告)号：WO2010035119A3
公开(公告)日：2010-05-20
申请号：PCT/IB2009006950
申请日：2009-09-26
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , MODI RAJIV INDRAVADAN , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , MODI RAJIV INDRAVADAN , KHAMAR BAKULESH MAFATLAL
IPC分类号： C12N5/16
CPC分类号： A61K31/56 , A61K39/00 , A61K39/0011 , A61K39/12 , A61K39/39 , A61K2039/5152 , A61K2039/5252 , A61K2039/53 , A61K2039/55511 , C12N2730/10134 , C12N2760/20134 , C12N2770/28134
摘要： The invention provides novel adjuvants and pharmaceutical composition comprising of an adjuvant alone. The invention also provides novel vaccine compositions comprising of an antigen and a novel adjuvant. The novel adjuvant as per present invention is farnesoid-X-receptor (FXR) antagonist. The invention also relates to an adjuvant for variety of antigens. The adjuvant improves antibody production specific to incorporated antigen. The adjuvant also induces cell mediated immune response.
摘要翻译：本发明提供了新颖的佐剂和药物组合物，其包含单独的佐剂。本发明还提供了包含抗原和新型佐剂的新型疫苗组合物。根据本发明的新型佐剂是法呢甾-X-受体（FXR）拮抗剂。本发明还涉及用于多种抗原的佐剂。该佐剂改善针对掺入抗原的抗体产生。佐剂也诱导细胞介导的免疫应答。

8. 发明申请

WO2009066146A3 STABLE SOLUTIONS OF SPARINGLY SOLUBLE ACTIVES 审中-公开
标题翻译：稳定可溶活性的稳定解决方案
公开(公告)号：WO2009066146A3
公开(公告)日：2009-12-30
申请号：PCT/IB2008003096
申请日：2008-11-15
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , OMRAY ASHOK SITARAM , PATRAVALE VANDANA , SHAH KARTIK YOGESH , PATEL PRASHANT YOGESH
发明人： MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , OMRAY ASHOK SITARAM , PATRAVALE VANDANA , SHAH KARTIK YOGESH , PATEL PRASHANT YOGESH
IPC分类号： A61K9/48
CPC分类号： A61K9/4858 , A61K31/137 , A61K31/167 , A61K31/4402 , A61K31/485
摘要： The present invention relates to a stable pharmaceutical composition comprising soft gelatin capsules containing at least one sparingly soluble active drug (singly or in combination with sparingly soluble and/or soluble drugs) and a solvent system, wherein the solvent system comprises of solvent, co-solvent, solubilizer(s), surfactant, aqueous solution of alkali and crystal growth inhibitor. The present invention further relates to process for preparing a stable pharmaceutical composition of sparingly soluble active drug(s) in soft gelatin capsules.
摘要翻译：本发明涉及稳定的药物组合物，其包含含有至少一种微溶性活性药物（单独或与微溶性和/或可溶性药物组合）和溶剂体系的软明胶胶囊，其中所述溶剂体系包含溶剂，溶剂，增溶剂，表面活性剂，碱水溶液和晶体生长抑制剂。本发明进一步涉及在软明胶胶囊中制备微溶活性药物的稳定药物组合物的方法。

9. 发明申请

WO2007113650A3 A NOVEL AND IMPROVED PROCESS FRO THE PREPARATION OF NATEGLINIDE AND ITS POLYMORPH FORM-H 审中-公开
标题翻译：一种新的和改进的方法来制备N-内酰胺及其多聚甲醛
公开(公告)号：WO2007113650A3
公开(公告)日：2009-04-16
申请号：PCT/IB2007000869
申请日：2007-04-04
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , VENKATASUBBU SHYLAJA , GAJULA MADHUSUDANA RAO , GURUSAMY RENUGADEVI , PONNIAH RAVI , VARMA RAJIV
发明人： MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , VENKATASUBBU SHYLAJA , GAJULA MADHUSUDANA RAO , GURUSAMY RENUGADEVI , PONNIAH RAVI , VARMA RAJIV
IPC分类号： C07C229/00
CPC分类号： C07C233/63 , C07C2601/14
摘要： Nateglinide is prepared by an improved process comprising reaction of trans-4-isopropyl cyclohexane carbonyl chloride with N,O-bis- trimethylsilyl protected D-phenyl alanine to give after aqueous workup, crude nateglinide which is converted to Nateglinide form- H using a mixture of cyclohexane / ethyl acetate. trans-4-isopropyl cyclohexane carbonyl chloride is prepared from trans-4- isopropyl cyclohexane carboxylic acid using oxalyl chloride.
摘要翻译：那格列奈通过改进的方法制备，包括反式-4-异丙基环己烷碳酰氯与N，O-双三甲基甲硅烷基保护的D-苯基丙氨酸反应，在水处理后，使用混合物转化为那格列奈形式H的粗那格列奈的环己烷/乙酸乙酯。使用草酰氯由反式-4-异丙基环己烷羧酸制备反式-4-异丙基环己烷碳酰氯。

10. 发明申请

WO2008053312A8 PROCESS FOR PREPARING AMORPHOUS ATORVASTATIN HEMI CALCIUM SALT AND ITS INTERMEDIATE 审中-公开
标题翻译：制备不定形ATORVASTATIN HEMI钙盐及其中间体的方法
公开(公告)号：WO2008053312A8
公开(公告)日：2008-08-21
申请号：PCT/IB2007003251
申请日：2007-10-29
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , JAIN PRATIMA , RAJPUT AMARSINGH L , TEKADE PRABHAKAR MOTIRAM , JOSHI ATUL CHHOTALAL , PONNAIAH RAVI , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , JAIN PRATIMA , RAJPUT AMARSINGH L , TEKADE PRABHAKAR MOTIRAM , JOSHI ATUL CHHOTALAL , PONNAIAH RAVI , KHAMAR BAKULESH MAFATLAL
IPC分类号： C07D207/327
CPC分类号： C07D207/34 , C07D405/06
摘要： The invention relates to the HMG-CoA reductase inhibitor in particular to Atorvastatin Hemi-calcium. The present invention is directed to novel processes for preparing amorphous form of Atorvastatin hemi calcium and their intermediate in high purity.
摘要翻译：本发明涉及特别是阿托伐他汀半钙的HMG-CoA还原酶抑制剂。本发明涉及制备无定形形式的阿托伐他汀半钙及其高纯度中间体的新方法。

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