Lehigh University

Rutgers, the State University of New Jersey

University of Medicine and Dentistry of New Jersey

Other

Buckman Laboratories International, Inc.

Jeffrey D Laskin

Ned D Heindel

Diane E Heck

Carl Jeffrey Lacey

Christophe Guillon

Anna Marie Vetrano

Sherri C Young

Marilyn S Whittemore

Ron Udasin

Robert D Rapp

Lauren Aleksunes

Thomas E McNeel

Mou-Tuan Huang

Peter DeMatteo

Debra L Laskin

Andrew J Gow

Marion K Gordon

David T Denhardt

Karma C Fussell

Jaclynn A Meshanni

Erik Aponte

Christine Martey

Abhilash N Pillai

Ivan Jabin

Geraldine Guillon

Michael A Gallo

Michele C Jetter Nee Siller

Grace L Guo

Pramod Mohanta

Thomas Finetti

Shiaw-Min Hwang

Karine Fabio

Angela Hunter

Cecilia Ang Lopez

A method of treating reduced pulmonary function by administering an effective dose of a Farnesoid X Receptor (FXR) agonist, particularly obeticholic acid, is disclosed. Also disclosed is an in vivo animal model of lung injury and altered functioning, useful for identifying compounds active in restoring pulmonary function.

Pulmonary function treatment

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

Methods and pharmaceutical compositions for inhibiting or decreasing transport of a drug by a transporter of multidrug resistance-associated protein comprising a compound of Formula (V): wherein Rand Rare small peptides or modified peptides, are provided. The methods and compositions are useful in enhancing efficacy of drugs such as anti-inflammatory agents, neurological agents, thyroid agents, ocular agents, cancer chemotherapeutics, antibiotics, antimicrobials, antivirals and protease inhibitors to treat human immunodeficiency virus.

Methods and compositions for modulating transport of a drug

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

Methods and pharmaceutical compositions for inhibiting or decreasing transport of a drug by a transporter of multidrug resistance-associated protein comprising a compound of Formula (IV) wherein Rand Rare small peptides or modified peptides, are provided. The methods and compositions are useful in enhancing efficacy of drugs such as anti-inflammatory agents, neurological agents, thyroid agents, ocular agents, cancer chemotherapeutics, antibiotics, antimicrobials, antivirals and protease inhibitors to treat human immunodeficiency virus.

Methods and pharmaceutical compositions for inhibiting or decreasing transport of a drug by a transporter of multidrug resistance-associated protein comprising a compound of Formula (VI) wherein Rand Rare small peptides or modified peptides, are provided. The methods and compositions are useful in enhancing efficacy of drugs such as anti-inflammatory agents, neurological agents, thyroid agents, ocular agents, cancer chemotherapeutics, antibiotics, antimicrobials, antivirals and protease inhibitors to treat human immunodeficiency virus.

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

A high throughput method and apparatus for rapidly screening a plurality of genotoxicants to determine the degree and type of genotoxicity are provided.

Sensitive high throughput method for DNA damage and repair

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

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.

Growing community of inventors

Piscataway, NJ, United States of America

Jeffrey D Laskin