Lehigh University

Rutgers, the State University of New Jersey

University of Medicine and Dentistry of New Jersey

Other

Azevan Pharmaceuticals, Inc.

Buckman Laboratories International, Inc.

Elder Pharmaceuticals Ltd.

Ned D Heindel

Jeffrey D Laskin

Diane E Heck

Carl Jeffrey Lacey

Christophe Guillon

Sherri C Young

Marilyn S Whittemore

Anna Marie Vetrano

Robert D Rapp

Gary A Koppel

Marvin J Miller

Thomas E McNeel

Robert F Bruns, Jr

Mou-Tuan Huang

Peter DeMatteo

Christophe D G Guillon

Marion K Gordon

Angela Hunter

Michele C Jetter Nee Siller

Michael A Gallo

Miguel Turizo

Hugh D Burns

Venkataraman Balasubramanian

Mridula D Choudhuri

Ivan Jabin

Karine Fabio

Pramod Mohanta

Christine Martey

Abhilash N Pillai

Geraldine Guillon

Thomas Finetti

Erik Aponte

Christophe D Guillon

Robert F Bruns

Shifang Lu

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.

Augmenting moieties for anti-inflammatory compounds

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X=C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed. 

Unique dual-action therapeutics

Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.

Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.

Vanilloid fatty hydroxamates as therapeutic anti-inflammatory pharmaceuticals

Nitric oxide biosynthesis-inhibiting anti-inflammatory and anti-microbial compounds of Formula (3) and Formula (4) wherein R1 and R2 are independently selected from optionally substituted thienyl, optionally substituted furyl, optionally substituted &#x2014;CH&#x2550;CH-thienyl and optionally substituted &#x2014;CH&#x2550;CH-furyl, provided that R2 is substituted with as nitro group Treatment methods utilizing the compounds, and methods of synthesis of the compounds are also disclosed.

Furyl and thienyl triazole derivatives and therapeutic uses thereof

This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.

Pharmacologically-active vanilloid carbamates

Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.

Dimethyl amino ethyl ether psoralens and methods for their production and use

Fused-ring triazole compounds which inhibit proliferation of cells and exhibit a unique and intense fluorescence are provided. Also provided are methods for synthesizing these compounds and methods for using these compounds to inhibit cell proliferation and infection and to label and fluorescently detect selected molecules.

Fluorescent fused-ring traizoles that inhibit cell proliferation and uses thereof

Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin Vreceptor 

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Methods and kits for labeling and detecting thiol containing species and nucleic acids using mercurimethyl-dihydropsoralen compounds and derivatives thereof which intercalate nucleic acids and are highly reactive with thiol containing species are provided. Fluorescent reactions products of the mercurimethyl-dihydropsoralen compounds or derivatives thereof attached to a thiol containing species and nucleic acids fluorescently labeled with these reaction products are also provided.

Fluorescent tags for amino acid and nucleic acid analysis

Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin Vreceptor.

Fluorescent fused-ring triazoles that inhibit cell proliferation and uses thereof

5&prime;-substituted, 4&prime;,5&prime;-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described.

Amino-and mercurio-substituted 4&prime;,5'-dihydropsoralens and therapeutical uses thereof

The invention relates to 4&prime;-substituted-4&prime;,5&prime;-dihydropsoralen compounds of formula(V):

Growing community of inventors

Easton, PA, United States of America

Ned D Heindel