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1. 发明申请

WO2006114676A8 A PROCESS FOR THE PREPARATION OF RUPATADINE 审中-公开
标题翻译：制备RUPATADINE的方法
公开(公告)号：WO2006114676A8
公开(公告)日：2007-11-22
申请号：PCT/IB2006000964
申请日：2006-04-22
申请人： CADILA PHARMACEUTICALS LTD , KHAMAR BAKULESH MAFATLAL , MODI INDRAVADAN AMBALAL , SHUKLA MANISH CHANDRAKANT , PARIKH KRUNAL KASHYAPBHAI , DANGE SURYABHAN PRABHAKAR , PONNIAH RAVI , DESAI SANJAY JAGDISH , VENKATRAMAN J
发明人： KHAMAR BAKULESH MAFATLAL , MODI INDRAVADAN AMBALAL , SHUKLA MANISH CHANDRAKANT , PARIKH KRUNAL KASHYAPBHAI , DANGE SURYABHAN PRABHAKAR , PONNIAH RAVI , DESAI SANJAY JAGDISH , VENKATRAMAN J
IPC分类号： C07D221/06 , A61K31/435
CPC分类号： C07D401/14
摘要： Rupatadine is synthesized by phase transfer catalysed N-alkylation of Desloratadine in biphasic s
摘要翻译：卢帕定是通过相转移催化的N-二烷基化的地氯雷他定N-烷基化合成的

2. 发明申请

WO2008001188A3 AN IMPROVED PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE ARIPIPRAZOLE 审中-公开
标题翻译：用于制备主要纯的阿维替唑的改进方法
公开(公告)号：WO2008001188A3
公开(公告)日：2009-04-23
申请号：PCT/IB2007001732
申请日：2007-06-26
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , SONDAGAR KEVAL RAMESHKUMAR , KAGATHARA NIRAV KESHAVLAL , SHUKLA MANISH CHANDRAKANT , PONNAIAH RAVI
发明人： MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , SONDAGAR KEVAL RAMESHKUMAR , KAGATHARA NIRAV KESHAVLAL , SHUKLA MANISH CHANDRAKANT , PONNAIAH RAVI
IPC分类号： C07D401/12
CPC分类号： C07D215/227
摘要： The invention relates to an improved process for preparing substantially pure aripiprazole (HPLC >99.8 %), wherein 7,7'-[tetramethylenebis(oxy)]bis(3,4- dihydroquinolin-2(lH)-one) is present in pure aripiprazole in
摘要翻译：本发明涉及制备基本上纯的阿立哌唑（HPLC> 99.8％）的改进方法，其中7,7' - [四亚甲基双（氧基）]双（3,4-二氢喹啉-2（1H） - 酮）以纯的阿立哌唑<0.01％（w / w）。

3. 发明申请

WO2008001188A8 AN IMPROVED PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE ARIPIPRAZOLE 审中-公开
标题翻译：一种改进的制备大量纯化ARIPIPRAZOLE的方法
公开(公告)号：WO2008001188A8
公开(公告)日：2008-05-02
申请号：PCT/IB2007001732
申请日：2007-06-26
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , SONDAGAR KEVAL RAMESHKUMAR , KAGATHARA NIRAV KESHAVLAL , SHUKLA MANISH CHANDRAKANT , PONNAIAH RAVI
发明人： MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL , SONDAGAR KEVAL RAMESHKUMAR , KAGATHARA NIRAV KESHAVLAL , SHUKLA MANISH CHANDRAKANT , PONNAIAH RAVI
IPC分类号： C07D403/02
CPC分类号： C07D215/227
摘要： The invention relates to an improved process for preparing substantially pure aripiprazole (HPLC >99.8 %), wherein 7,7'-[tetramethylenebis(oxy)]bis(3,4- dihydroquinolin-2(lH)-one) is present in pure aripiprazole in
摘要翻译：本发明涉及用于制备基本上纯的阿立哌唑（HPLC> 99.8％）的改进方法，其中7,7' - [四亚甲基双（氧基）]双（3,4-二氢喹啉-2（1H） - 酮）以纯阿立哌唑<0.01％（w / w）。

4. 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。

5. 发明申请

WO2009034434A3 AN IMPROVED PROCESS FOR THE PREPARATION OF O-DESMETHYLVENLAFAXINE 审中-公开
标题翻译：一种改进的制备O-脱甲基戊二胺的方法
公开(公告)号：WO2009034434A3
公开(公告)日：2009-12-30
申请号：PCT/IB2008002323
申请日：2008-09-09
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , MUKTAWAT SANJAY , SINGH UDAI PRATAP , CHANDRASEKARAN RAMASUBBU , PONNAIAH RAVI , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , MUKTAWAT SANJAY , SINGH UDAI PRATAP , CHANDRASEKARAN RAMASUBBU , PONNAIAH RAVI , KHAMAR BAKULESH MAFATLAL
IPC分类号： C07C209/00
CPC分类号： C07C213/08 , C07C217/74
摘要： The present invention provides a novel process for the preparation of O-desmethyl venlafaxine from venlafaxine or its salt. Venlafaxine or its salt is O-demethylated to provide O- desmethylvenlafaxine in high yield and purity by reacting venlafaxine or its salt with trimethyl silyl halide and metal sulfide at elevated temperature, using high boiling ethereal solvent(s). O- desmethylvenlafaxine is isolated by aqueous quenching followed by pH adjustment and isolated at pH ~9.5 to 10. The process avoids formation of high molecular weight sulfur compounds. O- desmethyl venlafaxine is produced in high yield (> 85 %) and purity (> 99.0), wherein each impurity is
摘要翻译：本发明提供了一种由文拉法辛或其盐制备O-去甲基文拉法辛的新方法。文拉法辛或其盐通过使用高沸点醚溶剂在升高的温度下使文拉法辛或其盐与三甲基甲硅烷基卤化物和金属硫化物反应，O-去甲基化以提供高收率和纯度的O-去甲基文拉法辛。 O-去甲基文拉法辛通过水淬，然后调节pH并在pH约9.5至10下分离。该方法避免了高分子量硫化合物的形成。以高产率（> 85％）和纯度（> 99.0）产生O-去甲基文拉法辛，其中每种杂质<0.1％。

6. 发明申请

WO2008114119A3 P38 INHIBITORS 审中-公开
标题翻译： P38抑制剂
公开(公告)号：WO2008114119A3
公开(公告)日：2009-12-23
申请号：PCT/IB2008000633
申请日：2008-03-18
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , GHOSH PRASANTA KUMAR , BHARDWAJ DEVESH , DESAI NIRAV M , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , GHOSH PRASANTA KUMAR , BHARDWAJ DEVESH , DESAI NIRAV M , KHAMAR BAKULESH MAFATLAL
IPC分类号： A01N47/28 , A61K31/17
CPC分类号： A61K35/74
摘要： The invention relates to novel p38 MAPK inhibitor which involves Mycobacterium w and/or its constituents in pharmaceutically acceptable carriers and their uses. Mycobacterium w and/or its constituents when administered to mammal results in p38 inhibition The inhibition is found to last more than 28 days. It is also found to induce inhibition of TNF-alfa. it suppresses cytokines in a pattern identical to Glucocorticoids. In transforms cells it also induces apoptosis. P38 mediated conditions include inflammation, cell differentiation, cell proliferation, cell inhibition, cell cycle regulation, anti-inflammatory reactions, immune modulation, vascularization, response to external stimuli and angiogenesis. The use of Mycobacterium w (Mw) and / or constituents of Mycobacterium w for inhibition of p38 protein kinase i.e. (i) to induce apoptosis in transformed cells (ii) for inhibition of TNF-alfa (iii) for inhibition of cytokines.
摘要翻译：本发明涉及新颖的p38MAPK抑制剂，其涉及在药学上可接受的载体中的分枝杆菌和/或其成分及其用途。当对哺乳动物施用时，分枝杆菌w和/或其成分导致p38抑制。发现抑制持续超过28天。还发现诱导TNF-α的抑制。它以与糖皮质激素相似的模式抑制细胞因子。在转化细胞时，它也诱导细胞凋亡。 P38介导的病症包括炎症，细胞分化，细胞增殖，细胞抑制，细胞周期调节，抗炎反应，免疫调节，血管化，对外部刺激的反应和血管生成。使用分枝杆菌w（Mw）和/或组织分枝杆菌w来抑制p38蛋白激酶，即（i）诱导转化细胞凋亡（ii）抑制TNF-α（iii）抑制细胞因子。

7. 发明申请

WO2008062288A3 POLY-TLR ANTAGONIST 审中-公开
公开(公告)号：WO2008062288A3
公开(公告)日：2009-04-23
申请号：PCT/IB2007003581
申请日：2007-11-21
申请人： CADILA PHARMACEUTICALS LTD , MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL
发明人： MODI INDRAVADAN AMBALAL , KHAMAR BAKULESH MAFATLAL
IPC分类号： A01N37/18 , A61K38/00
CPC分类号： C07K14/35 , A61K35/74
摘要： Mycobacterium w or its components are found to have poly TLR antagonistic activity to induced TLRs by varieties of TLR ligands. The induced TLR against which inhibitory effect is seen includes TLR 3, 4, 5, 6, 7, 8, 9. They also display antagonistic activities to effects of TLR ligands. They are also useful in management of diseases wherein TLRs are over expressed, like sepsis, multiple sclerosis, optic neuritis, Chronic obstructive pulmonary diseases multiple myeloma etc.
摘要翻译：发现分枝杆菌或其组分具有多种TLR配体诱导TLR的多TLR拮抗活性。可以看到抑制作用的诱导TLR包括TLR3,4,5,6,7,8,9。它们还显示对TLR配体作用的拮抗活性。它们也可用于治疗TLR过度表达的疾病，如败血症，多发性硬化，视神经炎，慢性阻塞性肺疾病多发性骨髓瘤等。

8. 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。

9. 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。

10. 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。

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