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。

公开(公告)号：US08076370B2

公开(公告)日：2011-12-13

申请号：US11913380

申请日：2006-05-03

申请人： Biswajit Das ,  Jasbir Singh Arora ,  Shahadat Ahmed ,  Anish Bandyopadhyay ,  Rita Katoch ,  Santosh Haribhau Kurhade ,  Sujata Rathy ,  Soma Ghosh ,  Abhijit Datta Khoje ,  Arti Gujrati ,  Dilip J. Upadhyay

发明人： Biswajit Das ,  Jasbir Singh Arora ,  Shahadat Ahmed ,  Anish Bandyopadhyay ,  Rita Katoch ,  Santosh Haribhau Kurhade ,  Sujata Rathy ,  Soma Ghosh ,  Abhijit Datta Khoje ,  Arti Gujrati ,  Dilip J. Upadhyay

IPC分类号： A61K31/27 ,  A61K31/18 ,  A61K31/155 ,  A61K31/44 ,  A61K31/501 ,  C07D213/72 ,  C07C333/00 ,  C07C303/00 ,  C07C277/00

CPC分类号： C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D231/20 ,  C07D239/42 ,  C07D249/12 ,  C07D277/36 ,  C07D295/096 ,  C07D307/68 ,  C07D333/34 ,  C07D333/38 ,  C07D333/62 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D513/04

摘要： Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.

摘要翻译： 本文提供的是取代的芳族化合物，其是tRNA合成酶抑制剂，因此可以用作抗微生物剂。 本文所述的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性，厌氧菌或真菌生物引起或促成的病症，特别是针对细菌，例如葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫萨拉， 大肠杆菌属，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，棒状杆菌属，芽孢杆菌属或肠杆菌属，以及真菌生物体，例如曲霉属，布氏酵母属，假丝酵母​​属，椰子球菌属，隐球菌属，表皮生长素，亨氏嗜血菌属，组织胞浆菌属，微孢子虫属，拟青霉菌属， ，肺孢子虫（Pneumocystis），毛癣菌（Trichophyton）或三孢子虫（Trichosporium）。 还提供了制备这些化合物的方法，其药物组合物和治疗微生物感染的方法。

公开(公告)号：US20090215764A1

公开(公告)日：2009-08-27

申请号：US11913380

申请日：2006-05-03

申请人： Biswajit Das ,  Jasbir Singh Arora ,  Shahadat Ahmed ,  Anish Bandyopadhyay ,  Rita Katoch ,  Santosh Haribhau Kurhade ,  Sujata Rathy ,  Soma Ghosh ,  Abhijit Datta Khoje ,  Arti Gujrati ,  Dilip J. Upadhyay

发明人： Biswajit Das ,  Jasbir Singh Arora ,  Shahadat Ahmed ,  Anish Bandyopadhyay ,  Rita Katoch ,  Santosh Haribhau Kurhade ,  Sujata Rathy ,  Soma Ghosh ,  Abhijit Datta Khoje ,  Arti Gujrati ,  Dilip J. Upadhyay

IPC分类号： A61K31/535 ,  C07D217/00 ,  A61K31/47 ,  C07D211/00 ,  A61K31/445 ,  C07D265/30 ,  C07D401/02 ,  A61K31/4545

CPC分类号： C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D231/20 ,  C07D239/42 ,  C07D249/12 ,  C07D277/36 ,  C07D295/096 ,  C07D307/68 ,  C07D333/34 ,  C07D333/38 ,  C07D333/62 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D513/04

摘要： Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.

摘要翻译： 本文提供的是取代的芳族化合物，其是tRNA合成酶抑制剂，因此可以用作抗微生物剂。 本文所述的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性，厌氧菌或真菌生物引起或促成的病症，特别是针对细菌，例如葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫萨拉， 大肠杆菌属，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，棒状杆菌属，芽孢杆菌属或肠杆菌属，以及真菌生物体，例如曲霉属，布氏酵母属，假丝酵母​​属，椰子球菌属，隐球菌属，表皮生长素，亨氏嗜血菌属，组织胞浆菌属，微孢子虫属，拟青霉菌属， ，肺孢子虫（Pneumocystis），毛癣菌（Trichophyton）或三孢子虫（Trichosporium）。 还提供了制备这些化合物的方法，其药物组合物和治疗微生物感染的方法。

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：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。