公开(公告)号：WO2009156966A1

公开(公告)日：2009-12-30

申请号：PCT/IB2009/052753

申请日：2009-06-25

Applicant: RANBAXY LABORATORIES LIMITED ,  SATTIGERI, Jitendra, A. ,  KUMAR, Naresh ,  YADAV, Ajay ,  SHARMA, Lalima ,  CLIFFE, Ian, A. ,  VARUGHESE, Shibu, B. ,  SHABBIR, Shaikh, Rizwan ,  RAJ, V., Samuel ,  UPADHYAY, Dilip, J. ,  BHATNAGAR, Pradip, K.

Inventor： SATTIGERI, Jitendra, A. ,  KUMAR, Naresh ,  YADAV, Ajay ,  SHARMA, Lalima ,  CLIFFE, Ian, A. ,  VARUGHESE, Shibu, B. ,  SHABBIR, Shaikh, Rizwan ,  RAJ, V., Samuel ,  UPADHYAY, Dilip, J. ,  BHATNAGAR, Pradip, K.

IPC: C07D417/04 ,  C07D417/14 ,  C07D493/04 ,  A61K31/428 ,  A61P31/04

CPC classification number: C07D417/14 ,  C07D417/04 ,  C07D493/04

Abstract: The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Coryne bacterium, Bacillus spp., Enterobactericeae,' (E.coli, Klebsiella spp., Proteus spp.,etc. ) or any combination thereof Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections. (Formula)

Abstract translation: 本发明提供可用作抗菌剂的促旋酶B和/或拓扑异构酶IV对E抑制剂。 本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性和厌氧细菌引起的或由其贡献的病症，更具体地针对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，假单胞菌属，醋酸杆菌属，莫氏假单胞菌 ，衣原体属，支原体属，军团菌属，棒状杆菌属，幽门螺杆菌属，梭菌属，拟杆菌属，棒状杆菌属，芽孢杆菌属，肠杆菌属（E.coli，Klebsiella spp。，Proteus spp。 等）或其任何组合。还提供了制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗细菌感染的方法。 （式）

公开(公告)号：WO2006117762A8

公开(公告)日：2009-03-05

申请号：PCT/IB2006051397

申请日：2006-05-03

Applicant: RANBAXY LAB LTD ,  DAS BISWAJIT ,  ARORA JASBIR SINGH ,  AHMED SHAHADAT ,  BANDYOPADHYAY ANISH ,  KATOCH RITA ,  KURHADE SANTOSH HARIBHAU ,  RATHY SUJATA ,  GHOSH SOMA ,  KHOJE ABHIJIT DATTA ,  GUJRATI ARTI ,  UPADHYAY DILIP J

Inventor： DAS BISWAJIT ,  ARORA JASBIR SINGH ,  AHMED SHAHADAT ,  BANDYOPADHYAY ANISH ,  KATOCH RITA ,  KURHADE SANTOSH HARIBHAU ,  RATHY SUJATA ,  GHOSH SOMA ,  KHOJE ABHIJIT DATTA ,  GUJRATI ARTI ,  UPADHYAY DILIP J

IPC: C07D333/34 ,  A61K31/381

CPC classification number: C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D231/20 ,  C07D239/42 ,  C07D249/12 ,  C07D277/36 ,  C07D295/096 ,  C07D307/68 ,  C07D333/34 ,  C07D333/38 ,  C07D333/62 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D513/04

Abstract: Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia,Rickettsiae, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes,Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.

Abstract translation: 本文提供的是取代的芳族化合物，其是tRNA合成酶抑制剂，因此可以用作抗微生物剂。 本文所述的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性，厌氧菌或真菌生物引起或促成的病症，特别是针对细菌，例如葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫萨拉， 大肠杆菌，衣原体，立克次氏体，支原体，军团菌，分枝杆菌，幽门螺杆菌，梭菌属，拟杆菌属，棒状杆菌属，芽孢杆菌属或肠杆菌属，以及真菌生物体，例如曲霉属，布氏酵母属，假丝酵母​​属，椰子球菌属，隐球菌属，表皮癣菌，亨氏球菌，组织胞浆菌， ，副球菌属，肺孢子虫属，毛癣菌属或Trichosporium。 还提供了制备这些化合物的方法，其药物组合物和治疗微生物感染的方法。

公开(公告)号：WO2012014109A1

公开(公告)日：2012-02-02

申请号：PCT/IB2011/053090

申请日：2011-07-11

Applicant: RANBAXY LABORATORIES LIMITED ,  DAS, Biswajit ,  UPADHYAY, Dilip, J. ,  PURNAPATRE, Kedar ,  GHOSH, Soma ,  KATOCH, Rita

Inventor： DAS, Biswajit ,  UPADHYAY, Dilip, J. ,  PURNAPATRE, Kedar ,  GHOSH, Soma ,  KATOCH, Rita

IPC: C07D239/88 ,  C07D239/96 ,  A61K31/517 ,  A61P31/04

CPC classification number: C07D239/88

Abstract: The present invention provides aromatic sulphonamides as tRNA synthetase inhibitors and process for their synthesis, pharmaceutical composition and method for treatment. Compounds disclosed can be used as antibacterial agents for the treatment or prevention of conditions caused by or contributed by aerobic and anaerobic Gram-positive pathogens, more particularly against bacterium, for example Staphylococcus, Enterococci and Streptococci . Compounds disclosed are used in particular for the treatment of skin and soft tissue infection, Formula (I).

Abstract translation: 本发明提供芳族磺酰胺作为tRNA合成酶抑制剂及其合成方法，药物组合物和治疗方法。 所公开的化合物可以用作抗菌剂，用于治疗或预防由需氧和厌氧革兰氏阳性病原体引起的或由其贡献的病症，特别是针对细菌，例如葡萄球菌，肠球菌和链球菌。 所公开的化合物特别用于治疗皮肤和软组织感染，式（I）。

公开(公告)号：WO2007029076A1

公开(公告)日：2007-03-15

申请号：PCT/IB2006/002368

申请日：2006-08-30

Applicant: RANBAXY LABORATORIES LIMITED ,  AHMED, Shahadat ,  DAS, Biswajit ,  UPADHYAY, Dilip, J.

Inventor： AHMED, Shahadat ,  DAS, Biswajit ,  UPADHYAY, Dilip, J.

IPC: C07D209/46 ,  C07D209/48 ,  C07D403/12 ,  C07D401/12 ,  C07D417/12 ,  A61K31/4035 ,  A61K31/4192 ,  A61K31/4427 ,  A61K31/433 ,  A61P31/00

CPC classification number: C07D209/46 ,  C07D209/44 ,  C07D209/48 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12

Abstract: Provided herein are substituted aromatic compound of Formula (I), which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds disclosed herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Rickettsiae, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and method of treating microbial infections are also provided.

Abstract translation: 本文提供了取代的式（I）芳族化合物，其为tRNA合成酶抑制剂，因此可用作抗微生物剂。 本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性，厌氧细菌或真菌生物引起的或由其贡献的病症，特别是针对细菌，例如葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫萨拉， 大肠杆菌，衣原体，立克次氏体，支原体，军团菌，分枝杆菌，幽门螺杆菌，梭菌属，拟杆菌属，棒状杆菌属，芽孢杆菌属或肠杆菌属，以及真菌生物体，例如曲霉属，布氏酵母属，假丝酵母​​属，椰子球菌属，隐球菌属，表皮癣菌，亨氏球菌，组织胞浆菌， ，副球孢子虫，肺孢子虫，发癣菌或三孢子虫。还提供了用于制备这些化合物的方法，其药物组合物和治疗微生物感染的方法。

公开(公告)号：WO02085886A3

公开(公告)日：2003-05-22

申请号：PCT/IN0200111

申请日：2002-04-24

Applicant: DE SOUZA NOEL J ,  PATEL MAHESH V ,  DESHPANDE PRASAD K ,  AGARWAL SHIV KUMAR ,  GUPTE SHRIKANT V ,  UPADHYAY DILIP J ,  BHAWSAR SATISH B ,  BERI RUPINDER K ,  SREENIVAS KANDEPU ,  NAIR SHEELA C ,  SHUKLA MILIND C ,  CHUGH Y ,  SHETTY NITIN ,  YEOLE RAVINDRA D ,  REDDY MADHAV M

Inventor： DE SOUZA NOEL J ,  PATEL MAHESH V ,  DESHPANDE PRASAD K ,  AGARWAL SHIV KUMAR ,  GUPTE SHRIKANT V ,  UPADHYAY DILIP J ,  BHAWSAR SATISH B ,  BERI RUPINDER K ,  SREENIVAS KANDEPU ,  NAIR SHEELA C ,  SHUKLA MILIND C ,  CHUGH Y ,  SHETTY NITIN ,  YEOLE RAVINDRA D ,  REDDY MADHAV M

IPC: A61K31/095 ,  A61K31/191 ,  A61K31/47 ,  A61K31/4709 ,  A61K45/06 ,  A61P3/04 ,  A61P11/00 ,  A61P13/10 ,  A61P13/12 ,  A61P19/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  C07D215/22 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00 ,  C07D413/04

CPC classification number: C07D215/233 ,  A61K31/47 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08

Abstract: 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.

Abstract translation: 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：WO0209758A3

公开(公告)日：2002-12-27

申请号：PCT/IN0100139

申请日：2001-07-31

Applicant: DE SOUZA NOEL J ,  PATEL MAHESH V ,  GUPTE SHRIKANT V ,  UPADHYAY DILIP J ,  SHUKLA MILIND C ,  CHATURVEDI NISHITH C ,  BHAWSAR SATISH B ,  NAIR SHEELA C ,  JAFRI MOHAMMED A ,  KHORAKIWALA HABIL F ,  WOCKHARDT LTD

Inventor： DE SOUZA NOEL J ,  PATEL MAHESH V ,  GUPTE SHRIKANT V ,  UPADHYAY DILIP J ,  SHUKLA MILIND C ,  CHATURVEDI NISHITH C ,  BHAWSAR SATISH B ,  NAIR SHEELA C ,  JAFRI MOHAMMED A ,  KHORAKIWALA HABIL F

IPC: A61K45/06 ,  A61P31/00 ,  C07D215/22 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00

CPC classification number: A61K31/546 ,  A61K31/65 ,  A61K31/7048 ,  A61K45/06 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  A61K2300/00

Abstract: Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.

Abstract translation: 描述了作为微生物细胞外排泵的外排泵抑制剂的化合物。 还描述了制备这些化合物的方法，使用这种外排泵抑制剂化合物的方法和包含这些化合物的药物组合物。

公开(公告)号：WO2002085886A2

公开(公告)日：2002-10-31

申请号：PCT/IN2002/000111

申请日：2002-04-24

Applicant: DE SOUZA, Noel J ,  PATEL, Mahesh V ,  DESHPANDE, Prasad K ,  AGARWAL, Shiv Kumar ,  GUPTE, Shrikant V ,  UPADHYAY, Dilip J ,  BHAWSAR, Satish B ,  BERI, Rupinder K ,  SREENIVAS, Kandepu ,  NAIR, Sheela C ,  SHUKLA, Milind C ,  CHUGH, Y ,  SHETTY, Nitin ,  YEOLE, Ravindra D ,  REDDY, Madhav M

Inventor： DE SOUZA, Noel J ,  PATEL, Mahesh V ,  DESHPANDE, Prasad K ,  AGARWAL, Shiv Kumar ,  GUPTE, Shrikant V ,  UPADHYAY, Dilip J ,  BHAWSAR, Satish B ,  BERI, Rupinder K ,  SREENIVAS, Kandepu ,  NAIR, Sheela C ,  SHUKLA, Milind C ,  CHUGH, Y ,  SHETTY, Nitin ,  YEOLE, Ravindra D ,  REDDY, Madhav M

IPC: C07D401/04

CPC classification number: C07D215/233 ,  A61K31/47 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08

Abstract: 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.

Abstract translation: 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：WO2008111020A2

公开(公告)日：2008-09-18

申请号：PCT/IB2008/050979

申请日：2008-03-14

Applicant: RANBAXY LABORATORIES LIMITED ,  CHAKRABARTI, Anjan ,  SURASE, Yogesh, Baban ,  JADHAV, Jitendra, Sambhaji ,  DAS, Biswajit ,  UPADHYAY, Dilip

Inventor： CHAKRABARTI, Anjan ,  SURASE, Yogesh, Baban ,  JADHAV, Jitendra, Sambhaji ,  DAS, Biswajit ,  UPADHYAY, Dilip

CPC classification number: C07H17/00 ,  C07H17/08

Abstract: The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided, are the processes for preparing the compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.

Abstract translation: 本发明提供了可用作抗菌剂的大环内酯衍生物。 本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性或厌氧菌引起的疾病或更有针对性地对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，莫拉沙拉菌，衣原体属，支原体 军团菌属，分枝杆菌属，螺杆菌属，梭菌属，拟杆菌属，棒状杆菌属，芽孢杆菌属，肠杆菌属或其任何组合。 还提供了用于制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗细菌感染的方法。

公开(公告)号：WO2007060627A3

公开(公告)日：2007-05-31

申请号：PCT/IB2006/054391

申请日：2006-11-22

Applicant: RANBAXY LABORATORIES LIMITED ,  UPADHYAY, Dilip, J. ,  CHAKRABARTI, Anjan ,  DAS, Biswajit ,  GOWRISHANKAR, Radhakrishnan

Inventor： UPADHYAY, Dilip, J. ,  CHAKRABARTI, Anjan ,  DAS, Biswajit ,  GOWRISHANKAR, Radhakrishnan

IPC: A61K31/7056 ,  A61P17/10

Abstract: This invention relates to 14-membered macrolides derivatives for treating or preventing acne vulgaris and inflammatory conditions thereof. Also provided herein are pharmaceutical compositions comprising one or more 14-membered macrolides derivatives together with one or more pharmaceutically acceptable carriers, excipients, diluents or mixture thereof, and methods for treating or preventing acne vulgaris and inflammatory condition thereof.

公开(公告)号：WO2007060627A2

公开(公告)日：2007-05-31

申请号：PCT/IB2006054391

申请日：2006-11-22

Applicant: RANBAXY LAB LTD ,  UPADHYAY DILIP J ,  CHAKRABARTI ANJAN ,  DAS BISWAJIT ,  GOWRISHANKAR RADHAKRISHNAN

Inventor： UPADHYAY DILIP J ,  CHAKRABARTI ANJAN ,  DAS BISWAJIT ,  GOWRISHANKAR RADHAKRISHNAN

CPC classification number: A61K31/7056

Abstract: This invention relates to 14-membered macrolides derivatives for treating or preventing acne vulgaris and inflammatory conditions thereof. Also provided herein are pharmaceutical compositions comprising one or more 14-membered macrolides derivatives together with one or more pharmaceutically acceptable carriers, excipients, diluents or mixture thereof, and methods for treating or preventing acne vulgaris and inflammatory condition thereof.

Abstract translation: 本发明涉及用于治疗或预防寻常痤疮及其炎性症状的14-元大环内酯衍生物。 本文还提供了包含一种或多种14-元大环内酯衍生物以及一种或多种药学上可接受的载体，赋形剂，稀释剂或其混合物的药物组合物，以及用于治疗或预防寻常痤疮及其炎性病症的方法。