The Scripps Research Institute

Blackthorn Therapeutics, Inc.

California Institute of Technology

Kyorin Pharmaceutical Co., Ltd.

Neumora Therapeutics, Inc.

Hugh Rosen

Edward Roberts

Miguel A Guerrero

Steven J Brown

Mariangela Urbano

Xuemei Peng

Ramulu Poddutoori

Robert M Jones

Eric Douglas Turtle

Candace Mae Laxamana

Xianrui Zhao

Brian M Stoltz

Raymond J Deshaies

Masahiro Ueno

Tsui-Fen Chou

Steven Brown

Shyama Herath

Eun-Kyong Kim

Qiang Li

Julia Ayers

Kaikoo Nakamura

Xiuwen Zhu

Jonathan S Rosenblum

Amanda C Jones

Yongsheng Liu

Melissa C Zhang

Chixu Chen

A compound having one of formula (1), formula (2), formula (3) and formula (4) or a pharmacologically acceptable salt thereof.

15-PGDH inhibitors

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.

One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.

Inhibitors of p97

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.

Growing community of inventors

La Jolla, CA, United States of America

Hugh Rosen