公开(公告)号：US08097594B2

公开(公告)日：2012-01-17

申请号：US12379539

申请日：2009-02-24

申请人： Milind Dattatraya Sindkhedkar ,  Vijaya Narayan Desai ,  Rajesh Maganlal Loriya ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Rajesh Onkardas Bora ,  Santosh Devidas Diwakar ,  Ganesh Rajaram Jadhav ,  Shivaji Sampatrao Pawar

发明人： Milind Dattatraya Sindkhedkar ,  Vijaya Narayan Desai ,  Rajesh Maganlal Loriya ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Rajesh Onkardas Bora ,  Santosh Devidas Diwakar ,  Ganesh Rajaram Jadhav ,  Shivaji Sampatrao Pawar

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07D493/04

摘要： The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-γ lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.

摘要翻译： 本发明提供具有抗微生物活性的化合物，其用于预防和治疗由微生物感染引起的疾病。 因此，本发明涉及具有抗微生物活性的新型半合成11,12-γ内酯大环内酯和酮内酯，以及制备化合物的方法以及含有所述化合物作为活性成分的药物组合物以及用该化合物治疗微生物感染的方法。

公开(公告)号：US20090247478A1

公开(公告)日：2009-10-01

申请号：US12379539

申请日：2009-02-24

申请人： Milind Dattatraya Sindkhedkar ,  Vijaya Narayan Desai ,  Rajesh Maganlal Loriya ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Rajesh Onkardas Bora ,  Santosh Devidas Diwakar ,  Ganesh Rajaram Jadhav ,  Shivaji Sampatrao Pawar

发明人： Milind Dattatraya Sindkhedkar ,  Vijaya Narayan Desai ,  Rajesh Maganlal Loriya ,  Mahesh Vithalbhai Patel ,  Bharat Kalidas Trivedi ,  Rajesh Onkardas Bora ,  Santosh Devidas Diwakar ,  Ganesh Rajaram Jadhav ,  Shivaji Sampatrao Pawar

IPC分类号： A61K31/7048 ,  C07H17/08

CPC分类号： C07D493/04

摘要： The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-γ lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.

摘要翻译： 本发明提供具有抗微生物活性的化合物，其用于预防和治疗由微生物感染引起的疾病。 因此，本发明涉及具有抗微生物活性的新型半合成的11,12-γ-内酯大环内酯和酮内酯，以及制备化合物的方法以及含有所述化合物作为活性成分的药物组合物以及用该化合物治疗微生物感染的方法。

公开(公告)号：US07868173B2

公开(公告)日：2011-01-11

申请号：US11715921

申请日：2007-03-09

申请人： Mahesh Vithalbhai Patel ,  Vijaya Narayan Desai ,  Prasad Keshav Deshpande ,  Ravindra Dattatraya Yeole ,  Rajesh Prabhakar Kale

发明人： Mahesh Vithalbhai Patel ,  Vijaya Narayan Desai ,  Prasad Keshav Deshpande ,  Ravindra Dattatraya Yeole ,  Rajesh Prabhakar Kale

IPC分类号： C07D221/06 ,  A61K31/473

CPC分类号： C07D455/04

摘要： The instant invention relates to novel prodrugs of optically pure benzoquinolizine-2-carboxylic acid and pharmaceutical compositions that include the prodrugs. In particular, the present invention relates to the sulfonic acid salts of L-alanine and L-valine prodrugs of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid. The compounds and compositions of the invention can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections, especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.

摘要翻译： 本发明涉及光学纯苯醌喹唑啉-2-羧酸的新型前体药物和包含前药的药物组合物。 特别地，本发明涉及L-丙氨酸的磺酸盐和S - （ - ） - 9-氟-6,7-二氢-8-（4-羟基哌啶-1-基） - 5-甲基-1-氧代-1H，5H-苯并[i，j]喹嗪-2羧酸。 本发明的化合物和组合物可用于治疗细菌革兰氏阳性，革兰氏阴性和厌氧感染，特别是由抗性革兰氏阳性生物和革兰氏阴性生物，分枝杆菌感染和新出现的医院病原体感染引起的感染。