The University of Texas System

Cytometix, Inc.

Other

University of Vermont

The Medical College of Wisconsin, Inc.

Mcw Research Foundation, Inc.

New York Medical College

Max-Delbrueck-Centrum Fuer Molekulare Medizin

Medical College of Georgia

Alcon, Inc.

William Marsh Rice University

Oregon State University

Alcon Universal Ltd.

Max-Delbruck-Centrum Fur Molekulare Medizin

Omeicos Therapeutics Gmbh

John Russell Falck

Martin M Bednar

Cordell E Gross

Robert Fischer

John David Imig

Michael Balazy

Gerd Wallukat

Wolf-Hagen Schunck

Lane Brostrom

Dominik N Mueller

Richard J Roman

David R Harder

Cosima Arnold

Narender Puli

Magdalena Alonso-Galicia

Elizabeth R Jacobs

Mark R Hellberg

Peter G Klimko

Raymond E Conrow

Anne Konkel

Vanessa Sperandio

William B Campbell

William H Gerwick

Daniel Halsell Ess

Michal L Schwartzman

Donald R Stewart

Tim Wesser

Abdul Hye Khan

Adeniyi Adebesin

Philipp Westphal

Wolf-Hagen Schunk

Christina Westphal

Mahesh P Paudyal

László Kürti

Henry Bordas-Murphy

Jawahar Lal Jat

Laszlo Kurti

Derun Li

Deb K Barma

Abhijit Kundu

Yingming Zhao

Victor Garcia

Brian L Marquez

Lumin Sun

Systems, compositions, and methods are disclosed for developing and delivering therapeutically effective 14,15-epoxyeicosatrienoic acid (14,15-EET) analogs, for example for pain management or treatment. Of particular interest are intermediate salts.

Methods of manufacturing 14,15-epoxyeicosatrienoic acid analogs and improved therapeutic delivery of same

The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents.

20-HETE receptor (GPR75) antagonists and methods of use

The present invention provides compounds (n-3 PUFA derivatives) of formula (I): that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.

Eicosanoid derivatives

Described here are EET analogs conjugated to folate receptor ligands such as folic acid or folic acid analogs recognized by and selectively bound by folate receptors and other folate binding proteins and the use of such conjugated EET analogs for targeted delivery of therapeutic agents to folate-receptor bearing cell populations. More particularly, provided herein are EET analogs conjugated to folate receptor ligands and uses of such conjugated EET analogs as kidney targeted therapeutics.

Substituted epoxyeicosatrienoic acid (EET) analogs for treatment of kidney disease

The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias.

CYP-eicosanoid derivatives

The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of cardiovascular diseases.

Metabolically robust analogs of CYP-eicosanoids for the treatment of cardiac disease

In some aspects, the present disclosure provides methods of aminating an aromatic compound comprising reacting an aminating agent with an aromatic compound in the presence of a rhodium catalyst. In some embodiments, the methods may comprise aminating an aromatic compound which contains multiple different functional groups. The methods described herein may also be used to create bicyclic system comprising reacting an intramolecular aminating agent with an aromatic ring to obtain a second ring containing a nitrogen atom. In another aspect, the methods described herein may also be used to create a cyclic aliphatic cyclic/poly cyclic amine system comprising a reacting an intramolecular aminating agent by insertion into a C(sp3)-H bond.

Direct C&#x2014;H amination and aza-annulation

The present invention provides a system enabling the oral delivery of therapeutics derived from polyunsaturated fatty acids (PUFAs), their metabolites and derivatives, including, eicosanoids, prostaglandins, prostacyclins, leukotrienes, resolvins, endocannabinoids, thromboxanes, epoxyeicosa-trienoic acids (EETs), hydroxyeicostetraenoic acids (HETEs), and CMX-020. The delivery system includes a vehicle comprising a purified docosahexaenoic acid (DHA) in triglyceride or ester form; a purified eicosapentaenoic acid (EPA) in triglyceride or ester form; a combination of DHA, EPA in either triglyceride or ester forms; or a modified DHA, EPA, or omega-3 fatty acid analog; and optionally, an antioxidant, a surfactant, a solubilizer, a stabilizer, a lubricant, or a pH/tonicity adjustment agent.

Compositions and methods for delivery of polyunsaturated fatty acid derivatives and analogs

A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N&#x2014;H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature.

Direct stereospecific synthesis of unprotected aziridines from olefins

The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.

Methods for modulating bacterial virulence and related compounds

Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.

Epoxyeicosatrienoic acid analogs and methods of making and using the same

The present invention provides compounds (n-3 PUFA derivatives) of formula (I) that modulate conditions associated with cardiac damage, especially cardiac arrhythmias. 

The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.

Arachidonic acid analogs and methods for analgesic treatment using same

Growing community of inventors

Dallas, TX, United States of America

John Russell Falck