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1. 发明申请

WO2009066320A2 FUSION PROTEIN SYSTEMS SUITABLE FOR HIGH EXPRESSION OF PEPTIDES 审中-公开
标题翻译：用于表达高表达的融合蛋白质系统
公开(公告)号：WO2009066320A2
公开(公告)日：2009-05-28
申请号：PCT/IN2008/000599
申请日：2008-09-22
申请人： CADILA HEALTHCARE LIMITED , MENDIRETTA, Sanjeev, Kumar , PATEL, Pankaj, R. , BANDYOPADHYAY, Sanjay , SARASWAT, Vibhor , SINGH, Arun, Kumar
发明人： MENDIRETTA, Sanjeev, Kumar , PATEL, Pankaj, R. , BANDYOPADHYAY, Sanjay , SARASWAT, Vibhor , SINGH, Arun, Kumar
IPC分类号： C07K14/435
CPC分类号： C12N15/62 , C07K14/535 , C07K14/62 , C07K14/635 , C12P21/02
摘要： The present invention discloses an improved process for the production of desired recombinant peptides from bacterial cells by using G-CSF as a novel fusion partner for their high level expression in these cells. The invention further provides an expression system comprising the fusion protein wherein the G-CSF is operatively linked to the peptide of interest via an enzymatic or chemical cleavage site which can be used to separate the fusion partner from the said peptide.
摘要翻译：本发明公开了通过使用G-CSF作为这些细胞中高水平表达的新型融合配偶体从细菌细胞中产生所需重组肽的改进方法。本发明还提供了包含融合蛋白的表达系统，其中G-CSF通过酶或化学切割位点可操作地连接到目的肽，其可用于从融合配偶体与所述肽分离。

2. 发明申请

WO2011013141A3 SUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS 审中-公开
公开(公告)号：WO2011013141A3
公开(公告)日：2011-02-03
申请号：PCT/IN2010/000486
申请日：2010-07-22
申请人： CADILA HEALTHCARE LIMITED , KHARUL, Rajendra , JAIN, Mukul, R. , PATEL, Pankaj, R.
发明人： KHARUL, Rajendra , JAIN, Mukul, R. , PATEL, Pankaj, R.
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/427 , A61P3/10
摘要： The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.

3. 发明申请

WO2007102174A3 PROCESS FOR PREPARING HUMAN G-CSF 审中-公开
标题翻译：制备人G-CSF的方法
公开(公告)号：WO2007102174A3
公开(公告)日：2008-01-03
申请号：PCT/IN2007000105
申请日：2007-03-05
申请人： CADILA HEALTHCARE LTD , MENDIRATTA SANJEEV KUMAR , SARASWAT VIBHOR , PATEL PANKAJ R
发明人： MENDIRATTA SANJEEV KUMAR , SARASWAT VIBHOR , PATEL PANKAJ R
IPC分类号： C07K14/535 , C12N1/20 , C12N15/68
CPC分类号： C07K14/535 , C12N1/20
摘要： The present invention discloses an improved process for the production of G-CSF in high yield via a high salt-induced increase in plasmid stability during the production phase.
摘要翻译：本发明公开了一种通过在生产阶段通过高盐诱导的质粒稳定性增加而以高产率生产G-CSF的改进方法。

4. 发明申请

WO2012120532A3 CYCLIC SHORT CHAIN PTH ANALOG PEPTIDES 审中-公开
标题翻译：循环短链PTH模拟肽
公开(公告)号：WO2012120532A3
公开(公告)日：2013-03-14
申请号：PCT/IN2012000078
申请日：2012-02-02
申请人： CADILA HEALTHCARE LTD , BAHEKAR RAJESH H , PRAJAPATI VJAY , JAIN MUKUL R , PATEL PANKAJ R
发明人： BAHEKAR RAJESH H , PRAJAPATI VJAY , JAIN MUKUL R , PATEL PANKAJ R
IPC分类号： C07K14/635 , A61K38/29
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention provides novel cyclic short-chain peptideshaving pharmaceutically beneficial properties. The invention also provides a process for preparing such short chain peptides and pharmaceutical compositions containing the cyclic peptides of the present invention. A-Z 1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z 12-Z13-Z 14-Z 15-B (I)
摘要翻译：本发明提供具有药学上有利性质的新型环状短链肽。本发明还提供了制备这种短链肽的方法和含有本发明的环肽的药物组合物。 A-Z 1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z 12-Z13-Z 14-Z 15-B（I）

5. 发明申请

WO2011048614A2 SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP-1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST 审中-公开
标题翻译：基于短链活性GLP-1激动剂和GLUCAGON受体拮抗剂的短链多肽
公开(公告)号：WO2011048614A2
公开(公告)日：2011-04-28
申请号：PCT/IN2010/000683
申请日：2010-10-18
申请人： CADILA HEALTHCARE LIMITED , BAHEKAR, Rajesh , JAIN, Mukul R. , PATEL, Pankaj R.
发明人： BAHEKAR, Rajesh , JAIN, Mukul R. , PATEL, Pankaj R.
IPC分类号： C07K14/435
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel short chain peptidomimetics, which act as GLP-1 receptors agonist and glucagon receptor antagonist. These dual acting peptidomimetics exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme, GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes ( in vitro ). Due to increased metabolic stability, other than parenteral route of administration, these short chain peptidomimetics can be delivered by oral routes of administration, for the treatment or prevention of diabetes and related metabolic disorders, such as obesity, hyperlipidemia and eating disorders.
摘要翻译：本发明提供新的短链肽模拟物，其作为GLP-1受体激动剂和胰高血糖素受体拮抗剂。这些双重作用的肽模拟物表现出增加的蛋白水解切割的稳定性，特别是对DPP-IV（二肽基肽酶-IV）酶，GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性。由于代谢稳定性增加，除了肠胃外给药途径之外，这些短链肽模拟物可以通过口服给药途径递送，用于治疗或预防糖尿病和相关的代谢紊乱，例如肥胖，高脂血症和进食障碍。

6. 发明申请

WO2010128521A3 SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST 审中-公开
标题翻译：短链激酶（PTH）受体激动剂
公开(公告)号：WO2010128521A3
公开(公告)日：2011-03-10
申请号：PCT/IN2010000264
申请日：2010-04-26
申请人： CADILA HEALTHCARE LTD , BAHEKAR RAJESH , JAIN MUKUL R , PATEL PANKAJ R
发明人： BAHEKAR RAJESH , JAIN MUKUL R , PATEL PANKAJ R
IPC分类号： C07K14/635 , A61K38/29
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/ PTH-I) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma upto 24 hours (in vitro), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment / prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B
摘要翻译：本发明提供了主要作为甲状旁腺激素（PTH / PTH-1）受体激动剂的新型短链肽。这些短链肽表现出增加的蛋白水解切割的稳定性。发现大多数短链肽在大鼠血浆中稳定至24小时（体外），显示出对GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性增加。由于增加的代谢稳定性，除了肠胃外给药途径之外，一些短链肽也可以通过口服给药途径递送，用于治疗/预防甲状旁腺功能减退症和以骨量减少为特征的疾病如骨质疏松症，绝经后骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B

7. 发明申请

WO2013054338A1 2-THIO-IMIDAZOLE DERIVATIVES AS TGR5 MODULATORS 审中-公开
标题翻译：作为TGR5调节剂的2-硫咪唑衍生物
公开(公告)号：WO2013054338A1
公开(公告)日：2013-04-18
申请号：PCT/IN2012/000471
申请日：2012-07-04
申请人： CADILA HEALTHCARE LIMITED , AGARWAL, Sameer , JAIN, Mukul R , PATEL, Pankaj R
发明人： AGARWAL, Sameer , JAIN, Mukul R , PATEL, Pankaj R
IPC分类号： C07D233/84 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4178 , A61K31/4164 , A61P3/04
CPC分类号： C07D233/84 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of the general Formula I their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, their N-oxide, metabolites, polymorphs, use of these compounds in medicine for treating diabetes (TGR5 modulators) and the intermediates involved in their preparation.
摘要翻译：本发明涉及通式I的化合物，其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，非对映异构体，前药，其N-氧化物，代谢物，多晶型物，这些化合物在治疗糖尿病的药物中的用途（TGR5调节剂）涉及中间体的制备。

8. 发明申请

WO2011013141A2 SUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS 审中-公开
标题翻译：取代的苯甲酰胺衍生物作为葡糖激酶（GK）激活剂
公开(公告)号：WO2011013141A2
公开(公告)日：2011-02-03
申请号：PCT/IN2010000486
申请日：2010-07-22
申请人： CADILA HEALTHCARE LTD , KHARUL RAJENDRA , JAIN MUKUL R , PATEL PANKAJ R
发明人： KHARUL RAJENDRA , JAIN MUKUL R , PATEL PANKAJ R
IPC分类号： C07D413/12
CPC分类号： C07D417/14 , C07D413/12 , C07D413/14
摘要： The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
摘要翻译：本发明涉及通式I的取代的苯甲酰胺衍生物及其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，非对映异构体，前药，代谢物和多晶型物，并且可用于治疗由葡糖激酶介导的疾病状态。本文公开的化合物可用于降低血糖水平和增加用于治疗II型糖尿病的胰岛素分泌。本发明还涉及制备本发明化合物的方法，含有该化合物的药物组合物及其用途。

9. 发明申请

WO2010128521A2 SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST 审中-公开
标题翻译：短链激酶（PTH）受体激动剂
公开(公告)号：WO2010128521A2
公开(公告)日：2010-11-11
申请号：PCT/IN2010/000264
申请日：2010-04-26
申请人： CADILA HEALTHCARE LIMITED , BAHEKAR, Rajesh , JAIN, Mukul R. , PATEL, Pankaj R.
发明人： BAHEKAR, Rajesh , JAIN, Mukul R. , PATEL, Pankaj R.
IPC分类号： C07K14/435
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/ PTH-I) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma upto 24 hours ( in vitro ), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes ( in vitro ). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment / prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z 1 -Z 2 -Z 3 -Z 4 -Z 5 -Z 6 -Z 7 -Z 8 -Z 9 -Z 10 -Z 11 -Z 12 -Z 13 -Z 14 -Z 15 -B
摘要翻译：本发明提供了主要作为甲状旁腺激素（PTH / PTH-1）受体激动剂的新型短链肽。这些短链肽表现出增加的蛋白水解切割的稳定性。发现大多数短链肽在大鼠血浆中稳定至24小时（体外），显示出对GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性增加。由于增加的代谢稳定性，除了肠胃外给药途径之外，一些短链肽也可以通过口服给药途径递送，用于治疗/预防甲状旁腺功能减退症和以骨量减少为特征的疾病，如骨质疏松症，绝经后骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B

10. 发明申请

WO2009066320A3 GCSF FUSION PROTEIN SYSTEMS SUITABLE FOR HIGH EXPRESSION OF PEPTIDES 审中-公开
标题翻译： GCSF融合蛋白质系统适用于高表达肽
公开(公告)号：WO2009066320A3
公开(公告)日：2009-09-24
申请号：PCT/IN2008000599
申请日：2008-09-22
申请人： CADILA HEALTHCARE LTD , MENDIRETTA SANJEEV KUMAR , PATEL PANKAJ R , BANDYOPADHYAY SANJAY , SARASWAT VIBHOR , SINGH ARUN KUMAR
发明人： MENDIRETTA SANJEEV KUMAR , PATEL PANKAJ R , BANDYOPADHYAY SANJAY , SARASWAT VIBHOR , SINGH ARUN KUMAR
IPC分类号： C12N15/62
CPC分类号： C12N15/62 , C07K14/535 , C07K14/62 , C07K14/635 , C12P21/02
摘要： The present invention discloses an improved process for the production of desired recombinant peptides from bacterial cells by using G-CSF as a novel fusion partner for their high level expression in these cells. The invention further provides an expression system comprising the fusion protein wherein the G-CSF is operatively linked to the peptide of interest via an enzymatic or chemical cleavage site which can be used to separate the fusion partner from the said peptide.
摘要翻译：本发明公开了通过使用G-CSF作为这些细胞中高水平表达的新型融合配偶体从细菌细胞中产生所需重组肽的改进方法。本发明还提供了包含融合蛋白的表达系统，其中G-CSF通过酶或化学切割位点可操作地连接到目的肽，其可用于从融合配偶体与所述肽分离。

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