公开(公告)号：US20070082926A1

公开(公告)日：2007-04-12

申请号：US10578371

申请日：2004-11-10

申请人： Prasad Deshpande ,  Satish Bhavsar ,  Yati Chugh ,  Ravindra Yeole ,  Noel De Souza ,  Mahesh Vithalbhai

发明人： Prasad Deshpande ,  Satish Bhavsar ,  Yati Chugh ,  Ravindra Yeole ,  Noel De Souza ,  Mahesh Vithalbhai

IPC分类号： A61K31/4709 ,  C07D401/02

CPC分类号： C07D401/04

摘要： A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid and S-(−)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.

摘要翻译： 外消旋（±）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基）-1,4-苯并二氢吡喃的盐酸盐和甲磺酸盐的多晶形式， -2,3-二氢-4-氧代喹啉-3-羧酸，右旋R-（±）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） - 1,4-二氢-4-氧代 - 喹啉-3-羧酸和S - （ - ） - 1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） （I）和（II）的1,4-二氢-4-氧代喹啉-3-羧酸。 还描述了其制备方法。 本发明还涉及包含本发明化合物用于治疗哺乳动物细菌感染的药物组合物的方法和药物组合物。

公开(公告)号：US08729269B2

公开(公告)日：2014-05-20

申请号：US12705258

申请日：2010-02-12

申请人： Prasad Keshav Deshpande ,  Milind Dattatraya Sindkhedkar ,  Mahesh Shriram Phansalkar ,  Ravindra Dattatraya Yeole ,  Shrikant Vinayak Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Subhash Bhagwat ,  Milind Chintaman Shukla ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

发明人： Prasad Keshav Deshpande ,  Milind Dattatraya Sindkhedkar ,  Mahesh Shriram Phansalkar ,  Ravindra Dattatraya Yeole ,  Shrikant Vinayak Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Subhash Bhagwat ,  Milind Chintaman Shukla ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

IPC分类号： C07D411/06 ,  A61K31/454

CPC分类号： C07D491/10 ,  C07D413/10 ,  C07D413/14 ,  C07D495/10 ,  C07D497/10 ,  C07D513/10

摘要： The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

摘要翻译： 本发明提供具有预防和治疗感染性疾病的抗微生物活性的试剂。 因此，本发明提供新的取代的哌啶子基苯基恶唑烷酮衍生物，制备化合物的方法以及含有所述衍生物作为活性成分的抗微生物组合物以及用所述衍生物治疗细菌感染的方法。

公开(公告)号：US07687627B2

公开(公告)日：2010-03-30

申请号：US10935708

申请日：2004-09-07

申请人： Prasad Keshav Deshpande ,  Milind Dattatraya Sindkhedkar ,  Mahesh Shriram Phansalkar ,  Ravindra Dattatraya Yeole ,  Shrikant Vinayak Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Subhash Bhagwat ,  Milind Chintaman Shukla ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

发明人： Prasad Keshav Deshpande ,  Milind Dattatraya Sindkhedkar ,  Mahesh Shriram Phansalkar ,  Ravindra Dattatraya Yeole ,  Shrikant Vinayak Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Subhash Bhagwat ,  Milind Chintaman Shukla ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

IPC分类号： C07D491/113 ,  A61K31/438

CPC分类号： C07D491/10 ,  C07D413/10 ,  C07D413/14 ,  C07D495/10 ,  C07D497/10 ,  C07D513/10

摘要： The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

摘要翻译： 本发明提供具有预防和治疗感染性疾病的抗微生物活性的试剂。 因此，本发明提供新的取代的哌啶子基苯基恶唑烷酮衍生物，制备化合物的方法以及含有所述衍生物作为活性成分的抗微生物组合物以及用所述衍生物治疗细菌感染的方法。

公开(公告)号：US20050065164A1

公开(公告)日：2005-03-24

申请号：US10945504

申请日：2004-09-20

申请人： Noel De Souza ,  Mahesh Patel ,  Prasad Deshpande ,  Shiv Agarwal ,  Kandepu Sreenivas ,  Sheela Nair ,  Yati Chugh ,  Milind Shukla

发明人： Noel De Souza ,  Mahesh Patel ,  Prasad Deshpande ,  Shiv Agarwal ,  Kandepu Sreenivas ,  Sheela Nair ,  Yati Chugh ,  Milind Shukla

IPC分类号： A61K31/47 ,  A61K45/06 ,  C07D215/22 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00 ,  C07D471/02 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496

CPC分类号： A61K31/47 ,  A61K45/06 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  Y10S514/859

摘要： This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

公开(公告)号：US08288416B2

公开(公告)日：2012-10-16

申请号：US12311243

申请日：2007-09-22

申请人： Vijaykumar Jadgishwar Patil ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Deepak Vijaykumar Dekhane ,  Mohammad Usman Shaikh ,  Yati Chugh ,  Rajesh Prabhakar Chavan ,  Mohammad Alam Jafri

发明人： Vijaykumar Jadgishwar Patil ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Deepak Vijaykumar Dekhane ,  Mohammad Usman Shaikh ,  Yati Chugh ,  Rajesh Prabhakar Chavan ,  Mohammad Alam Jafri

IPC分类号： A61K31/445 ,  C07D413/14

CPC分类号： C07D413/10 ,  C07F9/65583

摘要： The present invention relates to oxazolidinones of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof. The invention also relates to processes for the preparation of the compound of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof, and to pharmaceutical compositions containing the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof and to methods for treating or preventing microbial infections using the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof.

摘要翻译： 本发明涉及式I的恶唑烷酮及其药学上可接受的盐，药学上可接受的溶剂化物或其多晶型物。 本发明还涉及制备式I化合物及其药学上可接受的盐，药学上可接受的溶剂合物或多晶型物的方法，以及含有式I化合物及其药学上可接受的盐，药学上可接受的溶剂化物或多晶型物的药物组合物，以及 使用式I化合物及其药学上可接受的盐，药学上可接受的溶剂合物或多晶型物治疗或预防微生物感染的方法。

公开(公告)号：US07538221B2

公开(公告)日：2009-05-26

申请号：US10578371

申请日：2004-11-10

申请人： Prasad Keshav Deshpande ,  Satish Baliram Bhavsar ,  Yati Chugh ,  Ravindra Dattatrya Yeole ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

发明人： Prasad Keshav Deshpande ,  Satish Baliram Bhavsar ,  Yati Chugh ,  Ravindra Dattatrya Yeole ,  Noel John De Souza ,  Mahesh Vithalbhai Patel

IPC分类号： C07D215/38 ,  A61K31/44

CPC分类号： C07D401/04

摘要： A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (±)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(+)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid and S-(−)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.

摘要翻译： 外消旋（±）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基）-1,4-苯并二氢吡喃的盐酸盐和甲磺酸盐的多晶形式， -2,3-二氢-4-氧代 - 喹啉-3-羧酸，右旋R - （+）-1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） - 1,4-二氢-4-氧代 - 喹啉-3-羧酸和S - （ - ） - 1-环丙基-6-氟-8-甲氧基-7-（4-氨基-3,3-二甲基哌啶-1-基） （I）和（II）的1,4-二氢-4-氧代 - 喹啉-3-羧酸。 还描述了其制备方法。 本发明还涉及包含本发明化合物用于治疗哺乳动物细菌感染的药物组合物的方法和药物组合物。

公开(公告)号：US07405228B2

公开(公告)日：2008-07-29

申请号：US10616888

申请日：2003-07-10

申请人： Mahesh V Patel ,  Prasad K Deshpande ,  Milind D Sindkhedkar ,  Shrikant V Gupte ,  Yati Chugh ,  Nitin Shetty ,  Milind C Shukla ,  Ravindra D Yeole ,  Noel J De Souza

发明人： Mahesh V Patel ,  Prasad K Deshpande ,  Milind D Sindkhedkar ,  Shrikant V Gupte ,  Yati Chugh ,  Nitin Shetty ,  Milind C Shukla ,  Ravindra D Yeole ,  Noel J De Souza

IPC分类号： A61K31/421 ,  A61K31/454 ,  C07D413/10 ,  C07D401/10

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

摘要翻译： 本发明提供了用于预防和治疗感染性疾病的高抗微生物活性的试剂。 因此，本发明提供新的氰基 - （取代） - 亚甲基哌啶基苯基恶唑烷酮衍生物，制备该化合物的方法，以及含有所述衍生物作为活性成分的抗微生物组合物以及用所述衍生物治疗细菌感染的方法。

公开(公告)号：US07626032B2

公开(公告)日：2009-12-01

申请号：US12150075

申请日：2008-04-24

申请人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Yati Chugh ,  Milind Chintaman Shukla

发明人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Yati Chugh ,  Milind Chintaman Shukla

IPC分类号： C07D211/56

CPC分类号： A61K31/47 ,  A61K45/06 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  Y10S514/859

摘要： This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

摘要翻译： 本发明涉及新一代三靶向，手性，广谱抗微生物7-取代的哌啶子基 - 喹诺酮羧酸衍生物，其旋光异构体，非对映异构体或对映异构体，以及其药学上可接受的盐，水合物，前药，多晶型物和假多晶型物 ，准备，组合和使用。

公开(公告)号：US07393957B2

公开(公告)日：2008-07-01

申请号：US10945504

申请日：2004-09-20

申请人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Yati Chugh ,  Milind Chintaman Shukla

发明人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Yati Chugh ,  Milind Chintaman Shukla

IPC分类号： C07D215/38 ,  A61K31/47

CPC分类号： A61K31/47 ,  A61K45/06 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  Y10S514/859

摘要： This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

摘要翻译： 本发明涉及新一代三靶向，手性，广谱抗微生物7-取代的哌啶子基 - 喹诺酮羧酸衍生物，其旋光异构体，非对映异构体或对映异构体，以及其药学上可接受的盐，水合物，前药，多晶型物和假多晶型物 ，准备，组合和使用。

公开(公告)号：US20050143421A1

公开(公告)日：2005-06-30

申请号：US10935708

申请日：2004-09-07

申请人： Prasad Deshpande ,  Milind Sindkhedkar ,  Mahesh Phansalkar ,  Ravindra Yeole ,  Shrikant Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Bhagwat ,  Milind Shukla ,  Noel De Souza ,  Mahesh Patel

发明人： Prasad Deshpande ,  Milind Sindkhedkar ,  Mahesh Phansalkar ,  Ravindra Yeole ,  Shrikant Gupte ,  Yati Chugh ,  Nitin Shetty ,  Sachin Bhagwat ,  Milind Shukla ,  Noel De Souza ,  Mahesh Patel

IPC分类号： C07D413/10 ,  C07D413/14 ,  C07D491/10 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D513/10 ,  C07D413/02 ,  A61K31/422 ,  A61K31/454

CPC分类号： C07D491/10 ,  C07D413/10 ,  C07D413/14 ,  C07D495/10 ,  C07D497/10 ,  C07D513/10

摘要： The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

摘要翻译： 本发明提供具有预防和治疗感染性疾病的抗微生物活性的试剂。 因此，本发明提供新的取代的哌啶子基苯基恶唑烷酮衍生物，制备化合物的方法以及含有所述衍生物作为活性成分的抗微生物组合物以及用所述衍生物治疗细菌感染的方法。