The Scripps Research Institute

Blackthorn Therapeutics, Inc.

Itherx Pharmaceuticals Inc.

Neumora Therapeutics, Inc.

Itherx Pharma, Inc.

Edward Roberts

Mariangela Urbano

Steven J Brown

Robert M Jones

Robert W Sullivan

Eric Douglas Turtle

Antonio Garrido Montalban

Justin T Ernst

Zhijun Wang

Hugh Rosen

Miguel A Guerrero

Ramulu Poddutoori

Xuemei Peng

Christopher Larson

Hiroshi Nakanishi

Russell Dahl

Jeffrey Dean Kahl

Erik Boman

Candace Mae Laxamana

Xianrui Zhao

Zhinjun Wang

Eddine Saiah

Nancy G J Delaet

Susana Conde Ceide

Stephen F Miller

Steven Brown

Stephen Miller

Robert Sullivan

Jeffrey D Kahl

Antonio G Montalban

Justin Ernst

Susana Conde-Ceide

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R, R, R, R, R, R, Rand Rare as defined herein.

Kappa opioid receptor antagonists and products and methods related thereto

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R, R, R, RR, R, Rand Rare as defined herein.

The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.

Sphinogosine-1 -phosphate receptor modulators for treatment of cardiopulmonary disorders

Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

Modulators of sphingosine phosphate receptors

Sphinogosine-1-phosphate receptor modulators for treatment of cardiopulmonary disorders

The invention provides novel ligands of Kappa (&#x3ba;) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress/anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.

Kappa opioid ligands

Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphingosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.

The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.

Cytokine inhibitors

Growing community of inventors

Fallbrook, CA, United States of America

Edward Roberts