公开(公告)号：US20120245183A1

公开(公告)日：2012-09-27

申请号：US13510458

申请日：2010-11-15

申请人： Prabhu Dutt Mishra ,  Shafee Mohammed Abdul ,  Ram Vishwakarma ,  Heinz-Herbert Fiebig ,  Gerhard Kelter

发明人： Prabhu Dutt Mishra ,  Shafee Mohammed Abdul ,  Ram Vishwakarma ,  Heinz-Herbert Fiebig ,  Gerhard Kelter

IPC分类号： A61K31/365 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4523 ,  C07D405/14 ,  C07D313/00 ,  C07D405/12

CPC分类号： C07D313/00

摘要： The present invention provides compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

摘要翻译： 本发明提供由式（1）表示的化合物：其中，R1，R2，R3和R4如说明书中所定义，具有所有比例的所有立体异构体和互变异构形式及其混合物及其药学上可接受的盐，药学上可接受的 溶剂合物，药学上可接受的多晶型物和前药。 本发明还涉及制备式（1）化合物和含有它们的药物组合物的方法。 本发明的化合物和药物组合物可用于治疗癌症。 本发明还提供了一种通过向有需要的哺乳动物施用治疗有效量的所述式（1）化合物或其药物组合物来治疗癌症的方法。

公开(公告)号：US08637670B2

公开(公告)日：2014-01-28

申请号：US13381464

申请日：2009-06-30

申请人： Sanjay Kumar ,  Ram Vishwakarma ,  Ramswaroop Mundada ,  Vijaykumar Deore ,  Pramod Kumar ,  Somesh Sharma

发明人： Sanjay Kumar ,  Ram Vishwakarma ,  Ramswaroop Mundada ,  Vijaykumar Deore ,  Pramod Kumar ,  Somesh Sharma

IPC分类号： C07D471/12 ,  A61K31/122

CPC分类号： C07D471/04

摘要： The present invention provides the compounds of formula (I): The present invention relates to imidazo[4,5-c]quinoline derivatives of formula (I), process for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK) and/or mammalian target of rapamycin (mTOR) and/or tumor necrosis factor-α (TNF-oc) and/or interleukin-6 (IL-6), particularly in the treatment of cancer and inflammation.

摘要翻译： 本发明提供式（I）化合物：本发明涉及式（I）的咪唑并[4,5-c]喹啉衍生物，其制备方法，含有它们的药物组合物及其在治疗疾病中的用途 由磷脂酰肌醇-3-激酶（PBK）和/或哺乳动物雷帕霉素（mTOR）和/或肿瘤坏死因子-α（TNF-α）和/或白细胞介素-6（IL-6）介导，特别是在治疗 癌症和炎症。

公开(公告)号：US08003602B2

公开(公告)日：2011-08-23

申请号：US12226403

申请日：2007-04-10

申请人： Girish Badrinath Mahajan ,  Saji David George ,  Prafull Vasant Ranadive ,  Prabhu Dutt Satyanarayan Mishra ,  Sreekumar Sankaranarayanan Eyyammadichiyil ,  Rajan Mukund Panshikar ,  Satish Namdeo Sawant ,  Sridevi Krishna ,  Meenakshi Sivakumar ,  Koteppa Pari ,  Becky Mary Thomas ,  Zarine Eruch Patel ,  Ram Vishwakarma ,  Chandrakant Govind Naik ,  Lisette D'Souza ,  Prabha Devi

发明人： Girish Badrinath Mahajan ,  Saji David George ,  Prafull Vasant Ranadive ,  Prabhu Dutt Satyanarayan Mishra ,  Sreekumar Sankaranarayanan Eyyammadichiyil ,  Rajan Mukund Panshikar ,  Satish Namdeo Sawant ,  Sridevi Krishna ,  Meenakshi Sivakumar ,  Koteppa Pari ,  Becky Mary Thomas ,  Zarine Eruch Patel ,  Ram Vishwakarma ,  Chandrakant Govind Naik ,  Lisette D'Souza ,  Prabha Devi

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  C07K5/0821

摘要： This invention relates to a novel purified compound PM181104, of formula: of molecular weight 1514 and molecular formula C69H66N18O13S5; which is obtained by fermentation of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269). The invention includes all stereoisomeric forms and all tautomeric forms of the compound PM181104 and pharmaceutically acceptable salts and derivatives such as esters and ethers. The present invention further relates to processes for the production of the novel antibacterial compound(s), to the production of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269), and to pharmaceutical compositions containing the novel compound(s) as an active ingredient and its/their use in medicines for treatment and prevention of diseases caused by bacterial infections.

摘要翻译： 本发明涉及分子量为1514和分子式C69H66N18O13S5的新型纯化的化合物PM181104; 其通过发酵属于Kocuria物种（ZMA B-1 / MTCC 5269）的微生物获得。 本发明包括化合物PM181104的所有立体异构体形式和所有互变异构形式以及药学上可接受的盐和衍生物如酯和醚。 本发明还涉及生产新型抗菌化合物的方法，用于生产属于Kocuria种的微生物（ZMA B-1 / MTCC 5269），以及含有新化合物的药物组合物， 作为活性成分及其在用于治疗和预防由细菌感染引起的疾病的药物中的用途。

公开(公告)号：US20120108627A1

公开(公告)日：2012-05-03

申请号：US13381464

申请日：2009-06-30

申请人： Sanjay Kumar ,  Ram Vishwakarma ,  Ramswaroop Mundada ,  Vijaykumar Deore ,  Pramod Kumar ,  Somesh Sharma

发明人： Sanjay Kumar ,  Ram Vishwakarma ,  Ramswaroop Mundada ,  Vijaykumar Deore ,  Pramod Kumar ,  Somesh Sharma

IPC分类号： A61K31/4745 ,  A61P35/00 ,  A61P35/02 ,  A61P17/06 ,  A61P17/00 ,  A61P17/14 ,  A61P19/04 ,  A61P27/02 ,  A61P1/00 ,  A61P29/00 ,  A61P19/10 ,  A61P19/02 ,  A61P9/10 ,  A61P9/00 ,  A61P7/00 ,  A61P25/00 ,  A61P1/04 ,  A61P37/00 ,  A61P37/06 ,  A61P11/06 ,  A61P11/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention provides the compounds of formula (I): The present invention relates to imidazo[4,5-c]quinoline derivatives of formula (I), process for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK) and/or mammalian target of rapamycin (mTOR) and/or tumor necrosis factor-α (TNF-oc) and/or interleukin-6 (IL-6), particularly in the treatment of cancer and inflammation.

摘要翻译： 本发明提供式（I）化合物：本发明涉及式（I）的咪唑并[4,5-c]喹啉衍生物，其制备方法，含有它们的药物组合物及其在治疗疾病中的用途 由磷脂酰肌醇-3-激酶（PBK）和/或哺乳动物雷帕霉素（mTOR）和/或肿瘤坏死因子-α（TNF-α）和/或白细胞介素-6（IL-6）介导，特别是在治疗 癌症和炎症。

公开(公告)号：US20090076094A1

公开(公告)日：2009-03-19

申请号：US12226403

申请日：2007-04-10

申请人： Girish Badrinath Mahajan ,  Saji David George ,  Prafull Vasant Ranadive ,  Prabhu Dutt Satyanarayan Mishra ,  Sreekumar Sankaranarayanan Eyyammadichiyil ,  Rajan Mukund Panshikar ,  Satish Namdeo Sawant ,  Sridevi Krishna ,  Meenakshi Sivakumar ,  Koteppa Pari ,  Becky Mary Thomas ,  Zarine Eruch Patel ,  Ram Vishwakarma ,  Chandrakant Govind Naik ,  Lisette D'Souza ,  Prabha Devi

发明人： Girish Badrinath Mahajan ,  Saji David George ,  Prafull Vasant Ranadive ,  Prabhu Dutt Satyanarayan Mishra ,  Sreekumar Sankaranarayanan Eyyammadichiyil ,  Rajan Mukund Panshikar ,  Satish Namdeo Sawant ,  Sridevi Krishna ,  Meenakshi Sivakumar ,  Koteppa Pari ,  Becky Mary Thomas ,  Zarine Eruch Patel ,  Ram Vishwakarma ,  Chandrakant Govind Naik ,  Lisette D'Souza ,  Prabha Devi

IPC分类号： A61K31/4439 ,  C07D417/14 ,  A61P31/04 ,  C12P17/16

CPC分类号： A61K38/12 ,  C07K5/0821

摘要： This invention relates to a novel purified compound PM181104, of formula: of molecular weight 1514 and molecular formula C69H66N18O13S5; which is obtained by fermentation of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269). The invention includes all stereoisomeric forms and all tautomeric forms of the compound PM181104 and pharmaceutically acceptable salts and derivatives such as esters and ethers. The present invention further relates to processes for the production of the novel antibacterial compound(s), to the production of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269), and to pharmaceutical compositions containing the novel compound(s) as an active ingredient and its/their use in medicines for treatment and prevention of diseases caused by bacterial infections.

摘要翻译： 本发明涉及分子量为1514和分子式C69H66N18O13S5的新型纯化的化合物PM181104; 其通过发酵属于Kocuria物种（ZMA B-1 / MTCC 5269）的微生物获得。 本发明包括化合物PM181104的所有立体异构体形式和所有互变异构形式以及药学上可接受的盐和衍生物如酯和醚。 本发明还涉及生产新型抗菌化合物的方法，用于生产属于Kocuria种的微生物（ZMA B-1 / MTCC 5269），以及含有新化合物的药物组合物， 作为活性成分及其在用于治疗和预防由细菌感染引起的疾病的药物中的用途。

公开(公告)号：US08637683B2

公开(公告)日：2014-01-28

申请号：US13510458

申请日：2010-11-15

申请人： Prabhu Dutt Mishra ,  Shafee Mohammed Abdul ,  Ram Vishwakarma ,  Heinz-Herbert Fiebig ,  Gerhard Kelter

发明人： Prabhu Dutt Mishra ,  Shafee Mohammed Abdul ,  Ram Vishwakarma ,  Heinz-Herbert Fiebig ,  Gerhard Kelter

IPC分类号： C07D313/00

CPC分类号： C07D313/00

摘要： The present invention provides compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

摘要翻译： 本发明提供由式（1）表示的化合物：其中R1，R2，R3和R4如说明书中所定义，具有所有比例的所有立体异构体和互变异构体形式及其混合物及其药学上可接受的盐，药学上可接受的 溶剂合物，药学上可接受的多晶型物和前药。 本发明还涉及制备式（1）化合物和含有它们的药物组合物的方法。 本发明的化合物和药物组合物可用于治疗癌症。 本发明还提供了一种通过向有需要的哺乳动物施用治疗有效量的所述式（1）化合物或其药物组合物来治疗癌症的方法。