公开(公告)号：US08455479B2

公开(公告)日：2013-06-04

申请号：US12863016

申请日：2009-01-23

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： C07D243/14 ,  C07D403/06 ,  C07D413/12 ,  C07D487/04 ,  A61K31/551 ,  A61P3/10

CPC分类号： C07D243/14 ,  C07D403/06 ,  C07D413/12 ,  C07D487/04

摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).

摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供包含式I化合物的药物组合物以及通过抑制二肽基肽酶IV（DPP-IV）来治疗或预防可被调节或归一化的一种或多种病症的方法。

公开(公告)号：US20120165320A1

公开(公告)日：2012-06-28

申请号：US13380744

申请日：2010-06-22

申请人： Rajseh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajseh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/422 ,  C07D413/14 ,  A61K31/4439 ,  A61K31/5377 ,  A61P25/00 ,  A61K31/403 ,  C07D417/10 ,  A61K31/541 ,  A61K31/551 ,  A61K31/5513 ,  C07D413/10 ,  C07D403/10

CPC分类号： C07D221/22 ,  C07D209/52 ,  C07D401/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08

摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。

公开(公告)号：US20110245258A1

公开(公告)日：2011-10-06

申请号：US13130440

申请日：2009-11-18

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/519 ,  A61P31/04 ,  A61P31/16 ,  A61P31/06

CPC分类号： C07D487/04 ,  C07D263/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

摘要翻译： 本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌 ，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

公开(公告)号：US07030148B2

公开(公告)日：2006-04-18

申请号：US10032392

申请日：2001-12-21

申请人： Selvakumar Natesan ,  Jagattaran Das ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Srinivasa Rao Naga Venkata Mamidi ,  Rajagopalan Ramanujam ,  Baskaran Sundarababu ,  Braj Bhushan Lohray

发明人： Selvakumar Natesan ,  Jagattaran Das ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Srinivasa Rao Naga Venkata Mamidi ,  Rajagopalan Ramanujam ,  Baskaran Sundarababu ,  Braj Bhushan Lohray

IPC分类号： A61K31/421 ,  C07D263/04

CPC分类号： C07D263/20 ,  C07D263/22 ,  C07D263/24 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10

摘要： The present invention relates to novel oxazolidinone compounds of the general formula (I) where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutical acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及通式（I）的新的恶唑烷酮化合物，其中R 1，R 2，R 3，Y 3， 1，Y 2，Y 3，Z如说明书中所定义; 它们的衍生物，它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，它们的药学上可接受的盐，它们的药学上可接受的溶剂合物和含有它们的药物组合物。

公开(公告)号：US07183301B2

公开(公告)日：2007-02-27

申请号：US10632950

申请日：2003-08-01

申请人： Selvakumar Natesan ,  Jagattaran Das ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Srinivasa Rao Naga Venkata Mamidi ,  Rajagopalan Ramanujam ,  Baskaran Sundarababu ,  Braj Bhushan Lohray

发明人： Selvakumar Natesan ,  Jagattaran Das ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Srinivasa Rao Naga Venkata Mamidi ,  Rajagopalan Ramanujam ,  Baskaran Sundarababu ,  Braj Bhushan Lohray

IPC分类号： A61K31/427 ,  C07C277/04

CPC分类号： C07D263/20 ,  C07D263/22 ,  C07D263/24 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10

摘要： The present invention relates to novel oxazolidinone compounds of the general formula (I). where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及通式（I）的新型恶唑烷酮化合物。 其中R 1，R 2，R 3，Y 1，Y 2， Y 3和Z如说明书中所定义; 它们的衍生物，它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的药学上可接受的溶剂化物和含有它们的药物组合物。

公开(公告)号：US06914058B2

公开(公告)日：2005-07-05

申请号：US10342114

申请日：2003-01-14

申请人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

发明人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

IPC分类号： A61K31/4192 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/655 ,  A61P31/00 ,  A61P31/04 ,  C07D249/06 ,  C07D295/12 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10 ,  C07D413/02 ,  C07D413/14 ,  C07D417/02 ,  C07D417/10 ,  C07D417/14

CPC分类号： C07D249/06 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10

摘要： The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotammers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及式（I）的新型三唑化合物，其衍生物，其类似物，其互变异构形式，其区域异构体，其旋转异构体，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药物组合物 。 更具体地，本发明涉及通式（I）的新型三唑衍生物，其类似物，其互变异构体，其区域异构体，其旋转异构体，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂化物和药物 含有它们的组合物。

公开(公告)号：US08906913B2

公开(公告)日：2014-12-09

申请号：US13380744

申请日：2010-06-22

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/5355 ,  C07D413/10 ,  C07D209/52 ,  C07D417/14 ,  C07D491/08 ,  C07D221/22 ,  C07D487/04 ,  C07D413/14 ,  C07D409/04 ,  C07D471/04 ,  C07D417/10 ,  C07D401/10

CPC分类号： C07D221/22 ,  C07D209/52 ,  C07D401/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08

摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。

公开(公告)号：US08841306B2

公开(公告)日：2014-09-23

申请号：US13130440

申请日：2009-11-18

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/33 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D413/12 ,  C07D263/20

CPC分类号： C07D487/04 ,  C07D263/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

摘要翻译： 本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌 ，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

公开(公告)号：US20100311732A1

公开(公告)日：2010-12-09

申请号：US12863016

申请日：2009-01-23

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/5517 ,  C07D243/14 ,  C07D487/04 ,  A61K31/5513 ,  A61P3/10 ,  A61P3/06 ,  A61P9/10 ,  A61P9/12 ,  A61P1/00 ,  A61P1/04 ,  A61P25/28 ,  A61P35/00 ,  A61P35/04 ,  A61P19/10 ,  A61P29/00 ,  A61P15/16 ,  A61P17/00 ,  A61P31/18

CPC分类号： C07D243/14 ,  C07D403/06 ,  C07D413/12 ,  C07D487/04

摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).

摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供包含式I化合物的药物组合物以及通过抑制二肽基肽酶IV（DPP-IV）来治疗或预防可被调节或归一化的一种或多种病症的方法。

公开(公告)号：US07202254B2

公开(公告)日：2007-04-10

申请号：US11120617

申请日：2005-05-03

申请人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

发明人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

IPC分类号： C07D401/10 ,  C07D401/14 ,  A61K31/4439 ,  A61P31/04

CPC分类号： C07D249/06 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10

摘要： The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及式（I）的新型三唑化合物，其衍生物，其类似物，其互变异构形式，其区域异构体，其旋转异构体，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药物组合物 。 更具体地说，本发明涉及通式（I）的新型三唑，