University of Kansas

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

The Scripps Research Institute

Northwestern University

The University of North Carolina at Chapel Hill

California Institute of Technology

Uwm Research Foundation, Inc.

Cleave Biosciences, Inc.

Kevin Frankowski

Frank John Schoenen

Jeffrey Aube

Noel Terrence Southall

Juan Jose Marugan

Marc Ferrer

Thomas Edward Prisinzano

Laura Bohn

Wei Ping Zheng

Xin Hu

Samarjit Patnaik

Sui Huang

Kelin Li

Warren S Weiner

Chen Wang

David Robert Sibley

John Thomas Norton

Steven Titus

Joseph Perry Steiner

R Benjamin Free

Jeffrey Aubé

Amy Elizabeth Moritz

Han-Jie Zhou

Samuel Gerritz

Raymond J Deshaies

Bryan Leo Roth

Jingbo Xiao

Prashi Jain

Tsui-Fen Chou

Tsanyang Liang

Altea Rocchi

Zongyi Hu

Shanshan He

Yuchi Chen

Brian Scott Jonathan Blagg

Congcong He

David Norman Frick

Partha Ghosh

Jennie L Conroy

Kathryn D Luderman

Wei Zheng

Jeffrey AubÉ

The disclosure of a compound of Formula I or a pharmaceutically acceptable salt thereof

Selective D3 dopamine receptor agonists and methods of their use

The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R, R, R, and Rare defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

Selective Ddopamine receptor agonists and methods of their use

The invention provides a compound of formula (I): wherein R, R, R, and Rare as defined herein, ginsenoside Rg2 of structure (II): or a combination thereof, for use in treating or preventing a condition responsive to the induction of autophagy in a brain of a mammal in need thereof. 

Autophagy inducers for treatment of CNS conditions

The present technology is directed to compounds, compositions, and methods related to non-morphinan-like kappa opioid receptor (KOR) antagonists. The technology is suited to treat addiction, diuresis, depression, post traumatic stress disorder, an eating disorder, panic disorder, social anxiety disorder, general anxiety disorder, obsessive compulsive disorders, excessive or unreasonable specific phobias, and/or other conditions related to anxiety or aversion-reward responses.

Antagonists of the kappa opioid receptor

The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R, R, R, and Rare as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal. 

Compounds and methods for the prevention and treatment of tumor metastasis and tumorigenesis

Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers. 

Heterocyclic compounds and methods of use thereof

The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

Kappa opioid receptor effectors and uses thereof

The present invention discloses thioflavine S and primuline derivatives which inhibit hepatitis C virus helicase and protease activity. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are useful as antiviral agents. The present invention further relates to pharmaceutical compositions containing the aforementioned compounds and methods of treating an HCV infection.

HCV helicase inhibitors and methods of use thereof

Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.

Methods and compositions for inhibition of the transitional endoplasmic reticulum ATPase

A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.

Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods

Growing community of inventors

Lawrence, KS, United States of America

Kevin Frankowski