Cumbre Pharmaceuticals Inc.

Cumbre IP Ventures, L.p.

Astellas Pharma Gmbh

Alcon Research, Ltd.

Global Alliance for Tb Drug Development

Keith D Combrink

Zhenkun Ma

Charles Z Ding

Yafei Jin

In Ho Kim

Susan Harran

Jing Li

Keith P Minor

Jamie C Longgood

Genliang Lu

Jiancheng Wang

Yong He

Mark R Hellberg

William Alexander Denny

Hwang-Hsing Chen

Najam A Sharif

Iok-Hou Pang

Brian Desmond Palmer

Andrew Mark Thompson

Abdelmoula Namil

Bryon Severns

Adrian Blaser

Hamish Scott Sutherland

Iveta Kmentova

Ganesh Prasanna

A Simon Lynch

Dianjun D Chen

Minsoo Song

Daniel Denton

Timothy W Morris

Suchismita Mohapatra

Jamie Carol Longgood

Andrew M Thompson

Diajun D Chen

The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Bradykinin receptor agonists and uses thereof to treat ocular hypertension and glaucoma

The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.

Quinolone carboxylic acid-substituted rifamycin derivatives

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

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

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

Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C-C) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred Rcomprises hydrogen or acetyl and a prefered Rcomprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.

(R/S) rifamycin derivatives, their preparations and pharmaceutical compositions

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Arlington, TX, United States of America

Keith D Combrink