Uwm Research Foundation, Inc.

Columbia University

Women & Infants Hospital of Rhode Island

Alexander E Arnold

James M Cook

Douglas C Stafford

Charles W Emala

Michael Rajesh Stephen

Rakesh Kumar Singh

Guanguan Li

Premchendar Nandhikonda

Gloria Forkuo

Rajwana Jahan

Revathi Kodali

Preetpal Singh Sidhu

George Gallos

The present invention describes substituted benzo[f]imidazo[1,5-a][1,4]diazepines of the formula (I): wherein R, R, R, R, and X are as disclosed herein. These compounds target alpha-4 and alpha-5 GABAa receptors and are useful for the treatment of airway hyperresponsiveness and inflammation in asthma.

Substituted benzo[f]imidazo[1,5-a][1,4]diazepines as GABA(a) receptor modulators

Substituted benzo[f]imidazo[1,5-&#x3b1;][1,4]diazepines of formula (I') target alpha-4 and alpha-5 GABAreceptors for use in the treatment of airway hyperresponsiveness and inflammation in asthma. Compounds selectively partition to the peripheral compartment and have reduced CNS effects. 

Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

Vitamin D receptor-coregulator inhibitors

Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzo-diazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAreceptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.

GABAA agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma

Growing community of inventors

Milwaukee, WI, United States of America

Alexander E Arnold