Chugai Seiyaku Kabushiki Kaisha

Neurocrine Biosciences, Inc.

Dart Neuroscience, (cayman) Ltd.

Crinetics Pharmaceuticals, Inc.

Dart Neuroscience, LLC

Mi Chen

Jie Fei Cheng

Thomas Arrhenius

Martin W Rowbottom

Warren Stanfield Wade

Timothy Richard Coon

Neil Ashweek

Todd Ewing

Yun-Fei Zhu

Graham Beaton

Wanlong Jiang

Willy Moree

Liren Zhao

David Mark Wallace

Richard B Lowe

Nicole Smith

Gary David Lopaschuk

Jason Roland Dyck

Sovouthy Tith

Yoshiaki Watanabe

Mark E Wilson

Yoshiyuki Ono

Hirotaka Kashiwagi

Vincent Santora

Yujin Huang

Alex Michael Nadzan

Alan P Kaplan

Lin Zhang

DeMichael Chung

Richard Penuliar

Jian Zhao

William Charles Ripka

Terence P Keenan

Yunfei Zhu

Brett C Bookser

Andrew Richard Hudson

Michael I Weinhouse

Joel Renick

Jillian Basinger

Rossy Serafimov

Andrew Lindstrom

Jinghua Yu

Richard Julius Penuliar

Bin Liu

Masahiro Nishimoto

Joseph Pontillo

Shimiao Wang

Nicole Harriott

James Na

Gary D Lopaschuk

Jason R Dyck

Varsha Gupta

Masayuki Haramura

Steve Joel Brown

Charles Stanford Harmon

Jie Fei Chang

Demichael Chung

Substituted benzoxazole and benzofuran chemical entities of Formula (I): wherein, V, W, X, Y, Z, and m have any of the values described herein and compositions comprising such chemical entities; processes for making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; and the treatment of one or more disorders, including neurological, cognitive, immunological, and inflammatory disorders, as well as other conditions and diseases involving PDE7 or cyclic nucleotide signaling.

Substituted benzoxazole and benzofuran compounds as PDE7 inhibitors

Described herein are somatostatin subtype-2 receptor (SST2R) targeted therapeutics that target tumor cells expressing SST2R and their use in the treatment of cancer.

Somatostatin subtype-2 receptor (SST2R) targeted therapeutics and uses thereof

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R, R, R, R, R, R, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

Nonpeptide somatostatin type 5 receptor agonists and uses thereof

The invention provides a chemical entity of Formula (I) wherein R, R, R, R, X, and Y have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence. 

Substituted azetidinyl compounds as GlyT1 inhibitors

The invention provides a chemical entity of Formula (I), wherein R, R, R, R, Rand X have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence. 

Substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors

The invention includes a compound of formula I: wherein R, Y, A, n, Rand Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.

Therapeutic piperazines

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R, R, R, R, R, R, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

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San Diego, CA, United States of America

Mi Chen