Cumbre Pharmaceuticals Inc.

University of Texas System

Cumbre IP Ventures, L.p.

Jing Li

Zhenkun Ma

Charles Z Ding

In Ho Kim

Susan Harran

Yafei Jin

Keith P Minor

Jamie C Longgood

Patrick G Harran

Susan L Mooberry

April L Risinger

Jiangnan Peng

Susan Jeong

Yong He

Timothy W Morris

The invention provides epoxytaccalonolide microtubule stabilizers and their use as anti-proliferative microtubule stabilizing agents.

Taccalonolide microtubule stabilizers

The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrateuseful in the treatment abnormal cell mitosis. The application also discloses novel methods for synthesis of these compounds and methods of using these compounds.

Synthetic diazonamides

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

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

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

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 a series of novel spiro rifamycin derivatives which have demonstrated potent antimicrobial activity.

Growing community of inventors

Dallas, TX, United States of America

Jing Li