Abbott Laboratories Corporation

Cumbre Pharmaceuticals Inc.

Global Alliance for Tb Drug Development

Other

Janssen Pharmaceutica Nv

Cumbre IP Ventures, L.p.

Tennor Therapeutics Limited

Zhenkun Ma

Yat Sun Or

Daniel T Chu

Richard F Clark

Jacob J Plattner

Charles Z Ding

Jing Li

Curt S Cooper

George W Griesgraber

Keith D Combrink

In Ho Kim

Hong Yong

Susan Harran

Yafei Jin

Stevan Wakefield Djuric

Ly Tam Phan

Anthony K Fung

Brian Desmond Palmer

Keith P Minor

Jamie C Longgood

William Alexander Denny

Christopher Blair Cooper

Andrew Mark Thompson

Yu-Gui Gu

Adrian Blaser

Suoming Zhang

Rolf Wagner

Koenraad Jozef Lodewijk Marcel Andries

Genliang Lu

Michael D Tufano

Christopher E Motter

Qun Li

Douglas M Kalvin

Cheuk M Lee

David D Anderson

Moshe Weitzberg

Mira Hinman

William Sanders

Wei-Bo Wang

Teresa A Rosenberg

Bruce A Beutel

Linda M Lynch

Jiancheng Wang

Hamish Scott Sutherland

Yong He

Iveta Kmentova

Anna Marie Upton

Walter Marcel Mathilde Van Den Broeck

Peter Dandliker

Caroline David

Andrew M Thompson

Yang Liu

Hao Zhang

Kai Liu

Yan Chen

Todd M Hansen

Gang Zhang

Alan S Florjancic

Chun Li

Dongfeng Zhang

Robert F Keyes

Ly Th Phan

Haihong Huang

Leping Li

Huan Wang

Daniel P Larson

Todd D Bosse

Tianyuan Zhang

Yu Liu

Ying Yuan

Dali Yin

Jingbin Wang

Fabio Palazzo

A Simon Lynch

Dianjun D Chen

Jun Ding

Minsoo Song

Daniel Denton

Shijie He

Timothy W Morris

Peter Nemoto

Dawei Wan

Sanyi Wang

Michael John Rupp

Qian Zhang

Zhijun Zhuang

Binna Liu

Huibing Ai

Tamara Rehm

Jerome Emile Guillemont

Koenraad Jozef Andries

Jamie Carol Longgood

Keith Combrink

Zhang Suoming

Souming Zhang

Novel iron chelating group conjugated penam derivatives described herein show antibacterial activity, and could be used as antibacterial agents or beta-lactamase inhibitors (BLIs) which are of value for application in combination with other antibacterial agents. 

Penam derivatives for treating bacterial infections

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis. 

Antibacterial compounds and uses thereof

The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treatingand other microbial infections, either alone or in combination with other anti-infective treatments.

Nitroimidazooxazines and their uses in anti-tubercular therapy

The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treatingand other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below. 

Riminophenazines with 2-(heteroaryl)amino substituents and their anti-microbial activity

The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for, for use as anti-tubercular drugs, for use as anti-protozoal agents with unexpectedly high potency againstor, and for the treatment of other microbial infections.

Nitroimidazooxazine and nitroimidazooxazole analogues and their uses

Antibacterials having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods of prophylaxis and treatment of bacterial infections using the compounds are disclosed.

Antibacterial compounds

Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.

Nitroheteroaryl-containing rifamycin derivatives

The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as

Bicyclic nitroimidazole-substituted phenyl oxazolidinones

The current invention relates to a series of rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the 3,4-cyclo-rifamycin derivatives having an oxime group at the C-11 position.

Rifamycin C-11 oxime cyclo derivatives effective against drug-resistant microbes

The invention relates to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the rifamycin derivatives having an oxime group at the C-11 position.

Rifamycin C-11 oxime derivatives effective against drug-resistant microbes

Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to C-25 carbamate derivatives of rifamycin having another functional group or pharmacophore covalently attached to this position through a carbamate linkage. The resulting compounds exert their antimicrobial activity through a dual-function mechanism and therefore exhibit reduced frequency of resistance.

C-25 carbamate rifamycin derivatives with activity against drug-resistant microbes

Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.

Rifamycin derivatives effective against drug-resistant microbes

The present invention relates to rifamycin 3-iminomethylenyl (&#x2014;CH&#x2550;N&#x2014;) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (&#x2014;CH&#x2550;N&#x2014;) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.

Rifamycin imino derivatives effective against drug-resistant microbes

Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C-C) forms): or their salts, hydrates or prodrugs thereof,wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG., provided L is not wherein Ris H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.

Rifamycin derivatives

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Dallas, TX, United States of America

Zhenkun Ma