公开(公告)号：US20090156465A1

公开(公告)日：2009-06-18

申请号：US12159562

申请日：2006-12-12

申请人： Jitendra A. Sattigeri ,  Shahadat Ahmed ,  Murugaiah M.S. Andappan ,  Sachin Sethi ,  Lalima Sharma ,  Chanchal Kumar Pal ,  Sachin Ramesh Kandalkar ,  Dipak C. Mahajan ,  Kaushal Kishore ,  Sumati Bhatia ,  Anil G. Gadhave ,  Vinay S. Bansal ,  Joseph Alexanand Davis

发明人： Jitendra A. Sattigeri ,  Shahadat Ahmed ,  Murugaiah M.S. Andappan ,  Sachin Sethi ,  Lalima Sharma ,  Chanchal Kumar Pal ,  Sachin Ramesh Kandalkar ,  Dipak C. Mahajan ,  Kaushal Kishore ,  Sumati Bhatia ,  Anil G. Gadhave ,  Vinay S. Bansal ,  Joseph Alexanand Davis

IPC分类号： A61K38/28 ,  C07D413/02 ,  A61K31/5377 ,  C07D241/36 ,  A61K31/4995 ,  A61K31/702 ,  A61K31/397 ,  A61P3/00 ,  A61P3/10 ,  A61P37/00 ,  A61P35/00 ,  A61P1/00 ,  A61P15/08

CPC分类号： C07D409/12 ,  C07C237/20 ,  C07C2603/74 ,  C07D209/44 ,  C07D209/52 ,  C07D211/58 ,  C07D401/12 ,  C07D405/12 ,  C07D487/08

摘要： The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

摘要翻译： 本发明涉及作为二肽基肽酶-IV抑制剂的β-氨基酸衍生物及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及治疗糖尿病，特别是2型糖尿病以及糖尿病前期，糖尿病性血脂异常，代谢性酸中毒，酮症，饱腹感和肥胖症的方法。 这些抑制剂也可用于治疗由各种代谢，神经，抗炎和自身免疫性疾病如炎症性疾病，多发性硬化，类风湿性关节炎所表现的病症; 病毒，癌症和胃肠道疾病。 本发明的化合物也可用于治疗由于多囊卵巢综合征引起的不育症。

公开(公告)号：US20080300251A1

公开(公告)日：2008-12-04

申请号：US12065754

申请日：2006-09-01

申请人： Jitendra A. Sattigeri ,  Murugaiah M.S. Andappan ,  Kaushal Kishore ,  Sachin Sethi ,  Sachin Ramesh Kandalkar ,  Chanchal Kumar Pal ,  Dipak C. Mahajan ,  Shahadat Ahmed ,  Santhosh Sadashiv Parkale ,  T. Srinivasan ,  Lalima Sharma ,  Vinay S. Bansal ,  Anita Chugh ,  Joseph Alexanand Davis

发明人： Jitendra A. Sattigeri ,  Murugaiah M.S. Andappan ,  Kaushal Kishore ,  Sachin Sethi ,  Sachin Ramesh Kandalkar ,  Chanchal Kumar Pal ,  Dipak C. Mahajan ,  Shahadat Ahmed ,  Santhosh Sadashiv Parkale ,  T. Srinivasan ,  Lalima Sharma ,  Vinay S. Bansal ,  Anita Chugh ,  Joseph Alexanand Davis

IPC分类号： A61K31/498 ,  C07D221/02 ,  A61K31/439 ,  C07D215/00 ,  A61K31/4709 ,  C07D239/24 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P3/00 ,  A61K31/506 ,  C07D217/00 ,  A61K31/4725 ,  C07D241/36

CPC分类号： C07D403/12 ,  C07D209/52 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

摘要翻译： 本发明涉及作为二肽基肽酶-IV抑制剂的新型3-氮杂双环[3.1.0]己烷衍生物及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及治疗糖尿病，特别是2型糖尿病以及糖尿病前期，糖尿病性血脂异常，代谢性酸中毒，酮症，饱腹感和肥胖症的方法。 这些抑制剂也可用于治疗由各种代谢，神经，抗炎和自身免疫性疾病如炎症性疾病，多发性硬化，类风湿性关节炎所表现的病症; 病毒，癌症和胃肠道疾病。 本发明的化合物也可用于治疗由于多囊卵巢综合征引起的不育症。

公开(公告)号：US07956198B2

公开(公告)日：2011-06-07

申请号：US12092930

申请日：2006-11-08

申请人： Jitendra A. Sattigeri ,  Vinay S. Bansal

发明人： Jitendra A. Sattigeri ,  Vinay S. Bansal

IPC分类号： C07D207/00

CPC分类号： C07D207/34 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/554 ,  A61K31/70 ,  A61K45/06 ,  C07D405/06 ,  A61K2300/00

摘要： This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof. Also provided herein are the pharmaceutical compositions comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof and optionally together with at least one pharmaceutically acceptable carrier, and methods for the treatment or prophylaxis of cardiovascular diseases, Alzheimer's disease, obesity, diabetes or inflammatory diseases comprising administering to a mammal in need thereof therapeutically effective amounts of combination pharmaceutical composition comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixtures thereof.

摘要翻译： 本发明涉及包含至少一种新的取代的吡咯衍生物和一种或多种血脂异常剂，抗肥胖剂，抗高血糖药，抗炎剂或其混合物的组合产品或药物。 本文还提供了包含至少一种新的取代的吡咯衍生物和一种或多种血脂变剂，抗肥胖剂，抗高血糖药，抗炎剂或其混合物以及任选地与至少一种药学上可接受的载体的药物组合物，以及用于 治疗或预防心血管疾病，阿尔茨海默氏病，肥胖症，糖尿病或炎性疾病，包括向有需要的哺乳动物施用治疗有效量的组合药物组合物，其包含至少一种新的取代的吡咯衍生物和一种或多种血脂异常剂，抗肥胖剂，抗高血糖药 药剂，抗炎剂或其混合物。

公开(公告)号：US20080248035A1

公开(公告)日：2008-10-09

申请号：US12092930

申请日：2006-11-08

申请人： Jitendra A. Sattigeri ,  Vinay S. Bansal

发明人： Jitendra A. Sattigeri ,  Vinay S. Bansal

IPC分类号： A61K39/395 ,  A61K31/40 ,  A61K31/47 ,  A61K31/44 ,  A61K31/4439 ,  A61K38/16 ,  A61P25/00 ,  A61P29/00 ,  A61P3/00 ,  A61P9/00 ,  A61K31/554 ,  A61K31/397 ,  A61K31/445 ,  A61K31/70

CPC分类号： C07D207/34 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/554 ,  A61K31/70 ,  A61K45/06 ,  C07D405/06 ,  A61K2300/00

摘要： This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof. Also provided herein are the pharmaceutical compositions comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof and optionally together with at least one pharmaceutically acceptable carrier, and methods for the treatment or prophylaxis of cardiovascular diseases, Alzheimer's disease, obesity, diabetes or inflammatory diseases comprising administering to a mammal in need thereof therapeutically effective amounts of combination pharmaceutical composition comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixtures thereof.

摘要翻译： 本发明涉及包含至少一种新的取代的吡咯衍生物和一种或多种血脂异常剂，抗肥胖剂，抗高血糖药，抗炎剂或其混合物的组合产品或药物。 本文还提供了包含至少一种新的取代的吡咯衍生物和一种或多种血脂变剂，抗肥胖剂，抗高血糖药，抗炎剂或其混合物以及任选地与至少一种药学上可接受的载体的药物组合物，以及用于 治疗或预防心血管疾病，阿尔茨海默氏病，肥胖症，糖尿病或炎性疾病，包括向有需要的哺乳动物施用治疗有效量的组合药物组合物，其包含至少一种新的取代的吡咯衍生物和一种或多种血脂异常剂，抗肥胖剂，抗高血糖药 药剂，抗炎剂或其混合物。