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1. 发明申请

US20090209612A1 PROCESS FOR THE PREPARATION OF ATORVASTATIN 审中-公开
标题翻译：制备ATORVASTATIN的方法
公开(公告)号：US20090209612A1
公开(公告)日：2009-08-20
申请号：US11569843
申请日：2005-05-31
申请人： Jitendra A. Sattigeri , Mohammad Salman , Shobhana Rawat , Sachin Sethi
发明人： Jitendra A. Sattigeri , Mohammad Salman , Shobhana Rawat , Sachin Sethi
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/34
摘要： The invention relates to processes for the preparation of atorvastatin. Atorvastatin is known by the chemical name [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid. The hemi-calcium salt of atorvastatin is useful as an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase). The invention also relates to pharmaceutical compositions that include the atorvastatin or a pharmaceutically acceptable salt thereof and to use of said compositions for treating hypolipidemia, hypocholesterolemia and atherosclerosis.
摘要翻译：本发明涉及制备阿托伐他汀的方法。阿托伐他汀以化学名称[R-（R *，R *）] -2-（4-氟苯基） - ，δ-二羟基-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-庚酸。阿托伐他汀的半钙盐可用作3-羟基-3-甲基戊二酰辅酶A还原酶（HMG-CoA还原酶）的抑制剂。本发明还涉及包含阿托伐他汀或其药学上可接受的盐以及所述组合物用于治疗低脂血症，低胆固醇血症和动脉粥样硬化的药物组合物。

2. 发明申请

US20080300251A1 Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors 审中-公开
标题翻译：作为二肽基肽酶-IV抑制剂的3-氮杂双环[3.1.0]己烷的衍生物
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。

3. 发明申请

US20090156465A1 DERIVATIVES OF BETA-AMINO ACID AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译：作为DIPEPTIDYLPEPDDASE-IV抑制剂的β-氨基酸的衍生物
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。

4. 发明申请

US20110166088A1 BENZOTHIAZOLES AND AZA-ANALOGUES THEREOF USE AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：苯并噻唑类及其类似物作为抗菌剂使用
公开(公告)号：US20110166088A1
公开(公告)日：2011-07-07
申请号：US13000561
申请日：2009-06-25
申请人： Jitendra A. Sattigeri , Naresh Kumar , Ajay Yadav , Lalima Sharma , Ian A. Cliffe , Shibu B. Varughese , Shaikh Rizwan Shabbir , V. Samuel Raj , Dilip J. Upadhyay , Pradip K. Bhatnager
发明人： Jitendra A. Sattigeri , Naresh Kumar , Ajay Yadav , Lalima Sharma , Ian A. Cliffe , Shibu B. Varughese , Shaikh Rizwan Shabbir , V. Samuel Raj , Dilip J. Upadhyay , Pradip K. Bhatnager
IPC分类号： A61K31/7068 , C07D417/14 , C07D413/14 , C07H17/02 , A61K31/444 , A61K31/4439 , A61K31/496 , A61K31/5355 , A61K31/513 , A61K31/506 , A61P31/04
CPC分类号： C07D417/14 , C07D417/04 , C07D493/04
摘要： The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Corynebacterium, Bacillus spp., Enterobactericeae,’ (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections. (Formula)
摘要翻译：本发明提供可用作抗菌剂的促旋酶B和/或拓扑异构酶IV对E抑制剂。本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性和厌氧细菌引起的或由其贡献的病症，更具体地针对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，假单胞菌属，醋酸杆菌属，莫氏假单胞菌，衣原体属（Chlamydia spp。），支原体属（Mycoplasma spp。），军团菌属（Legionella spp。），科分枝杆菌属（Ktycobacterium spp。），幽门螺杆菌属（Helicobacter），梭菌属（Clostridium spp。），拟杆菌属（Bacteroides spp。），棒杆菌属（Corynebacterium），芽孢杆菌属（Bacillus spp。），肠杆菌属（Enterobactersisae），（E.coli，Klebsiella spp。，Proteus spp。等等）或其任何组合。还提供了制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗细菌感染的方法。（式）

5. 发明申请

US20120108565A1 PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：吡咯羧酸衍生物作为抗菌剂
公开(公告)号：US20120108565A1
公开(公告)日：2012-05-03
申请号：US13056876
申请日：2009-07-30
申请人： Lalima Sharma , Jitendra A. Sattigeri , Narest Kumar , Ajay Yadav , Rijwan Momim , Shahadat Ahmed , Ian A. Cliffe , Pradip Kumar Bhatnagar , Sanjay Ghosh , V. Samuel Raj , Dilip J. Upadhyay
发明人： Lalima Sharma , Jitendra A. Sattigeri , Narest Kumar , Ajay Yadav , Rijwan Momim , Shahadat Ahmed , Ian A. Cliffe , Pradip Kumar Bhatnagar , Sanjay Ghosh , V. Samuel Raj , Dilip J. Upadhyay
IPC分类号： A61K31/403 , C07D401/14 , C07D403/12 , C07D413/14 , A61K31/427 , A61K31/4439 , A61K31/428 , A61K31/5377 , A61K31/506 , A61P31/04 , A61P11/00 , A61P17/00 , A61P13/00 , A61P19/08 , C07D405/14 , C07D407/14 , C07D403/14 , A61K31/422 , A61K31/454 , A61K31/496 , C07D417/14
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.
摘要翻译：本发明提供可用作抗菌剂的式（I）的DNA促旋酶和/或Topo IV抑制剂。本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性和厌氧细菌引起或由其贡献的病症，特别是针对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，假单胞菌属，醋酸杆菌属，乙型肝炎链球菌，衣原体属，支原体属，军团菌属，分枝杆菌属，幽门螺杆菌属，梭菌属，拟杆菌属，木杆菌属，芽孢杆菌属，肠杆菌属（E.coli，Klebsiella spp。，Proteus spp。）或其任何组合。还提供了制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗细菌感染的方法。

6. 发明授权

US07956198B2 Pharmaceutical compositions 失效
标题翻译：药物组合物
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。

7. 发明申请

US20080248035A1 Pharmaceutical Combination 失效
标题翻译：药物组合
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。

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