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公开(公告)号：US20080139574A1
公开(公告)日：2008-06-12
申请号：US11998448
申请日：2007-11-29
IPC分类号： A61K31/496 , C07D401/10 , A61P31/04
CPC分类号： C07D401/04 , C07D215/56 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process for preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts and pharmaceutical compositions containing them.
摘要翻译： 本发明涉及通式（I）的新化合物，其互变异构形式，其药学上可接受的盐和含有它们的药物组合物。 本发明还涉及制备通式（I）的化合物，其互变异构形式，其药学上可接受的盐和含有它们的药物组合物的方法。
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公开(公告)号：US20100240709A1
公开(公告)日：2010-09-23
申请号：US12086282
申请日：2006-12-11
申请人： Shanker Jayram Shetty , Gautam D. Patel , Braj Bhushan Lohray , Vidya Bhushan Lohray , Ganes Chakrabarti , Abhijit Chatterjee , Mukul R. Jain , Pankaj Ramanbhai Patel
发明人： Shanker Jayram Shetty , Gautam D. Patel , Braj Bhushan Lohray , Vidya Bhushan Lohray , Ganes Chakrabarti , Abhijit Chatterjee , Mukul R. Jain , Pankaj Ramanbhai Patel
IPC分类号： A61K31/4439 , C07D417/04 , C07D417/14 , A61P29/00
CPC分类号： C07D417/04
摘要： The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
摘要翻译： 本发明涉及通式（I）的新型化合物，其区域异构体，互变异构形式，涉及其合成的新中间体，其药学上可接受的盐和含有它们的药物组合物。 本发明还涉及制备通式（I）的化合物，其区域异构体，其互变异构形式，其药学上可接受的盐含有它们的药物组合物和涉及其合成的新中间体的方法。
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公开(公告)号：US08841413B2
公开(公告)日：2014-09-23
申请号：US12311448
申请日：2007-09-28
申请人： Rajesh H. Bahekar , Braj Bhushan Lohray , Vidya Bhushan Lohray , Mukul R. Jain , Kaushik M. Banerjee , Pankaj Ramanbhai Patel
发明人： Rajesh H. Bahekar , Braj Bhushan Lohray , Vidya Bhushan Lohray , Mukul R. Jain , Kaushik M. Banerjee , Pankaj Ramanbhai Patel
IPC分类号： C07K7/08 , C07K7/06 , C07K14/605
CPC分类号： C07K7/08 , C07K7/06 , C07K14/605
摘要： The present invention provides novel peptidomimetics, of formula (I), which primarily act as glucose dependent insulin secretagogues. Furthermore, it was found that these peptidomimetics showed glucagon receptor antagonistic activity, along with the GLP-1 receptor agonistic activity. A-Z1—Z2—Z3—Z4—Z5—Z6—Z7—Z8—Z9—Z10—Z11—B (I)
摘要翻译： 本发明提供式（I）的新型肽模拟物，其主要作为葡萄糖依赖性胰岛素促分泌剂。 此外，发现这些肽模拟物显示胰高血糖素受体拮抗活性，以及GLP-1受体激动活性。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-B（I）
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公开(公告)号：US20100280024A1
公开(公告)日：2010-11-04
申请号：US12682720
申请日：2008-10-13
IPC分类号： A61K31/536 , C07D215/14 , A61K31/47 , C07D217/00 , C07D265/36 , C07D211/32 , A61K31/445 , C07D403/02 , A61K31/506 , C07D241/04 , A61K31/495 , C07D207/00 , A61K31/40 , C07D295/00 , A61K31/5375 , A61K31/4709 , C07D401/00 , A61K31/4545 , A61P9/12
CPC分类号： C07D215/08 , C07D207/14 , C07D207/16 , C07D209/08 , C07D211/16 , C07D211/22 , C07D213/64 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/26 , C07D217/06 , C07D265/36 , C07D295/185 , C07D401/06 , C07D403/04
摘要： The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
摘要翻译： 本发明涉及式（I）的肾素抑制剂，其药学上可接受的盐和含有它们的药物组合物。 本发明还涉及制备通式（I）的化合物，其互变异构形式，其药学上可接受的盐，含有它们的药物组合物和涉及其合成的新中间体的方法。
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公开(公告)号：US20130225488A1
公开(公告)日：2013-08-29
申请号：US12311448
申请日：2007-09-28
申请人： Rajesh H. Bahekar , Braj Bhushan Lohray , Vidya Bhushan Lohray , Mukul R. Jain , Kaushik M. Banerjee , Pankaj Ramanbhai Patel
发明人： Rajesh H. Bahekar , Braj Bhushan Lohray , Vidya Bhushan Lohray , Mukul R. Jain , Kaushik M. Banerjee , Pankaj Ramanbhai Patel
CPC分类号： C07K7/08 , C07K7/06 , C07K14/605
摘要： The present invention provides novel peptidomimetics, of formula (I), which primarily act as glucose dependent insulin secretagogues. Furthermore, it was found that these peptidomimetics showed glucagon receptor antagonistic activity, along with the GLP-1 receptor agonistic activity. A—Z1—Z2—Z3—Z4—Z5—Z6—Z7—Z8—Z9—Z10—Z11—B (I)
摘要翻译： 本发明提供式（I）的新型肽模拟物，其主要作为葡萄糖依赖性胰岛素促分泌素。 此外，发现这些肽模拟物显示胰高血糖素受体拮抗活性，以及GLP-1受体激动活性。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-B（I）
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6.发明申请PEPTIDOMIMETICS WITH GLUCAGON ANTAGONISTIC AND GLP 1 AGONISTIC ACTIVITIES 有权具有GLUCAGON ANTAGONISTIC AND GLP 1 AGONISTIC活动的PEPTIDOMIME公开(公告)号：US20120021972A1
公开(公告)日：2012-01-26
申请号：US12746536
申请日：2008-12-10
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel peptidomimetics, of formula (I), which primarily act as glucose dependent insulin secretagogues. Furthermore, it was found that these peptidomimetics showed glucagon receptor antagonistic activity, along with the GLP-I receptor agonistic activity.
摘要翻译： 本发明提供式（I）的新型肽模拟物，其主要作为葡萄糖依赖性胰岛素促分泌剂。 此外，发现这些肽模拟物显示胰高血糖素受体拮抗活性，以及GLP-1受体激动活性。
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7.发明授权公开(公告)号：US08883963B2
公开(公告)日：2014-11-11
申请号：US12746536
申请日：2008-12-10
IPC分类号： C07K14/605 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel peptidomimetics, of formula (I), which primarily act as glucose dependent insulin secretagogues. Furthermore, it was found that these peptidomimetics showed glucagon receptor antagonistic activity, along with the GLP-I receptor agonistic activity.
摘要翻译： 本发明提供式（I）的新型肽模拟物，其主要作为葡萄糖依赖性胰岛素促分泌剂。 此外，发现这些肽模拟物显示胰高血糖素受体拮抗活性，以及GLP-1受体激动活性。
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公开(公告)号：US20120115907A1
公开(公告)日：2012-05-10
申请号：US13265537
申请日：2010-04-22
申请人： Pravain Thombare , Jigar Desai , Mukul R. Jain
发明人： Pravain Thombare , Jigar Desai , Mukul R. Jain
IPC分类号： A61K31/4468 , C07D401/06 , A61K31/4545 , C07D405/06 , A61K31/453 , A61P9/12 , A61P9/04 , A61P13/12 , A61P9/00 , A61P9/10 , A61P7/00 , A61P25/00 , A61P27/06 , A61P27/02 , A61P15/10 , A61P5/40 , A61P11/00 , A61P17/00 , A61P25/22 , A61P25/28 , C07D211/58
CPC分类号： C07D211/60 , C07D405/12
摘要： The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
摘要翻译： 本发明涉及通式（1）的新型肾素抑制剂，涉及其合成的新中间体，其药学上可接受的盐和含有它们的药物组合物。 本发明还涉及制备通式（1）的化合物，其互变异构形式，其药学上可接受的盐，含有它们的药物组合物和参与其合成的新中间体的方法。
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9.发明授权公开(公告)号：US08835469B2
公开(公告)日：2014-09-16
申请号：US13387885
申请日：2010-07-22
申请人： Rajendra Kharul , Mukul R. Jain , Pankaj R. Patel
发明人： Rajendra Kharul , Mukul R. Jain , Pankaj R. Patel
IPC分类号： C07D413/14 , C07D417/12 , C07D417/14 , A61K31/497 , A61K31/428 , A61K31/496
CPC分类号： C07D417/14 , C07D413/12 , C07D413/14
摘要： The present invention relates to substituted benzamide derivatives of the 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： 本发明涉及式I的取代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萄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用于增加用于治疗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，含有这些化合物的药物组合物及其用途。
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10.发明申请SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST 审中-公开短链基团基于ORAGY活性GLP 1激动剂和GLUCAGON受体拮抗剂公开(公告)号：US20120264685A1
公开(公告)日：2012-10-18
申请号：US13502826
申请日：2010-10-18
申请人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
发明人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
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。
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