The United States of America As Represented by the Department of Health

The United States of America, As Represented by the Secretary, Department of Health and Human Services

US Government As Represented by the Secretary of the Army

G.d. Searle & Company

The United States of America As Represented by the Secretary of

Brown University

Other

Neurogen Corporation

G.d. Searle LLC

Kenner C Rice

Brian R De Costa

Wayne D Bowen

Arthur E Jacobson

Xiao-Shu He

Celia Dominguez

Malliga R Iyer

George Kunos

Patricia C Contreras

Resat Cinar

Andrew Y Thurkauf

Mariena V Mattson

Nancy M Gray

Thomas L O'Donohue

Richard B Rothman

Lilian A Radesca

Ulrich Weiss

Michael Francis Rafferty

Frank Casper Tortella

Michael J Iadarola

Andrew Coop

Fuying Li

Ralph A Lessor

James A Monn

Karen F Berman

Sylvia N Calderon

Mark A DeCoster

Carl R Alving

Terrence R Burke, Jr

Amy Hauck Newman

Anita H Lewin

Michael A Rogawski

Gary R Matyas

Phil Skolnick

Candace B Pert

Tappey H Jones

William C Eckelman

Alexander V Mayorov

Juan-Carlos Marvizon

David Lewis

Dorota Matecka

John R Glowa

Neile A Grayson

Shunichi Yamaguchi

Kejun Cheng

J Michael Walker

Eric W Bow

Eugene S Gutman

Steven M Larson

Michael A Channing

John M Farah

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CBreceptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

Cannabinoid receptor mediating compounds

The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain. 

Biased potent opioid-like agonists as improved medications to treat chronic and acute pain and methods of using the same

Cannabinoid receptor mediating iminopyrazole compounds

A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X and Y are each independently selected from optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted cycloalkyl, optionally-substituted heterocycloalkyl, or optionally-substituted alkyl;

Pyrazole derivatives and their use as cannabinoid receptor mediators

In this application is described a composition and method for inducing in a subject anti-hapten antibodies without inducing antibodies to the carrier protein. Kits for designing and making compositions with desired haptens are also described.

Induction of highly specific antibodies to a hapten but not to a carrier peptide by immunization

Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:

Aralkyl diazabicycloalkane derivatives for CNS disorders

Compositions having neuroprotective and analgesic activity

The present invention provides a method for N-deprotecting an opioid compound, a method for N-deprotecting and O-demethylating an opioid compound, a method for O-demethylating an opioid compound, and a method for O-demethylating a nonpeptidic delta agonist compound or an opioid compound having a tertiary amide with no significant reaction at amide groups.

Methods of O-demethylation and N-deprotection

The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-&lsqb;2&lsqb;bis(aryl)methoxy&rsqb;ethyl&rsqb;-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.

Sustained-release derivatives of hydroxylated analogs of substituted 1-&lsqb;2&lsqb;bis(aryl)methoxy&rsqb;ethyl&rsqb;-piperazines and -homopiperazines and their use

Methods of o-demethylation and n-deprotection

Compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are alkyl of 1-8 carbons have been shown to have both neuroprotective and analgesic activities. The compounds of the invention may be used in treatment of conditions that would normally result in neuronal damage, including those arising on account of cerebral ischemia/hypoxia or increase in intracranial pressure such as neoplasms, stroke, meningitis or trauma. Compositions of the invention can also be useful for treatment of toxin-related damage such as drug over-dose or exposure to toxins in the environment.

Growing community of inventors

Bethesda, MD, United States of America

Kenner C Rice