公开(公告)号：US07691889B2

公开(公告)日：2010-04-06

申请号：US11082947

申请日：2005-03-18

申请人： Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A61K31/422 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/454 ,  A61K31/496 ,  C07D263/20 ,  C07D413/02 ,  C07D417/02

CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/14

摘要： Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

摘要翻译： 属于恶唑烷酮类的新型化合物具有强效的抗分支杆菌特性，特别适用于治疗结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然遗传和关西等酸性快速生物。 该化合物及其药学上可接受的盐作为抗菌剂。 还提及了抑制分枝杆菌细胞生长的方法以及治疗结核分枝杆菌，耐药性结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然和关西的分枝杆菌病症的方法，包括施用抗菌分泌杆菌 化合物和/或其药学上可接受的盐的量。 还提及了制备化合物或其药学上可接受的盐的方法。

公开(公告)号：US20080242676A1

公开(公告)日：2008-10-02

申请号：US12137170

申请日：2008-06-11

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A61K31/496 ,  C07D403/02 ,  C12N1/00 ,  C12N1/20 ,  A61P31/04

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

公开(公告)号：US07763602B2

公开(公告)日：2010-07-27

申请号：US12137170

申请日：2008-06-11

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A01N43/00 ,  A01N43/36 ,  A01N43/50 ,  A01N43/62 ,  A01N43/76 ,  A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/445 ,  A61K31/497 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

公开(公告)号：US07691837B2

公开(公告)日：2010-04-06

申请号：US10497615

申请日：2002-09-20

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A01N43/00 ,  A01N43/40 ,  A61K31/33 ,  A61K31/55 ,  A61K31/497 ,  A61K31/435 ,  C07D223/00 ,  C07D243/00 ,  C07D241/04 ,  C07D295/00 ,  C07D213/00

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

公开(公告)号：US20050192275A1

公开(公告)日：2005-09-01

申请号：US11082947

申请日：2005-03-18

申请人： Sudershan Arora ,  Vijaykumar Patil ,  Prathap Nair ,  Prasad Dixit ,  Shankar Ajay ,  Rakesh Sinha

发明人： Sudershan Arora ,  Vijaykumar Patil ,  Prathap Nair ,  Prasad Dixit ,  Shankar Ajay ,  Rakesh Sinha

IPC分类号： A61P31/00 ,  C07D263/20 ,  C07D413/10 ,  C07D413/14 ,  A61K31/541 ,  A61K31/422 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/02 ,  C07D417/02

CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/14

摘要： Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts thereof act as antibacterial agents. Also disclosed is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai, comprising administering an antimycobacterially effective amount of the said compound and/or pharmaceutically acceptable salts thereof. There is also disclosed a process for the manufacture of the said compound or its pharmaceutically acceptable salts.

摘要翻译： 属于恶唑烷酮类的新型化合物具有强效的抗分支杆菌特性，特别适用于治疗结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然遗传和关西等酸性快速生物。 该化合物及其药学上可接受的盐作为抗菌剂。 还公开了一种抑制分枝杆菌细胞生长的方法以及治疗结核分枝杆菌，耐药性结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶发性偶联菌和关西氏菌等分枝杆菌病症的方法，其包括施用抗分枝杆菌有效量 的所述化合物和/或其药学上可接受的盐。 还公开了制备所述化合物或其药学上可接受的盐的方法。

公开(公告)号：US20050107370A1

公开(公告)日：2005-05-19

申请号：US10497615

申请日：2002-09-20

申请人： Sudershan Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Sinha

发明人： Sudershan Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Sinha

IPC分类号： A61P31/06 ,  C07D207/32 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06 ,  C07D417/02 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D413/02 ,  C07D43/02

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。