Amgen Inc.

Gilead Sciences, Inc.

Oric Pharmaceuticals, Inc.

Genentech, Inc.

Tularik Limited

The Dupont Merck Pharmaceutical Company

Other

Japan Tobacco Inc.

Epiodyne, Inc.

Lawrence R McGee

Julio Cesar Medina

Jonathan B Houze

Xiaohui Du

Xiaodong Wang

Richard V Connors

Xiaoqi Chen

Jeffrey Thomas Mihalic

Jeffrey Deignan

John Eksterowicz

Zhihua Ma

David John Kopecky

Zice Fu

Steven H Olson

Julie Anne Heath

Steven Marc Rubenstein

Jason A Duquette

Choung U Kim

Ning Chen

Nobuko Nishimura

Kevin Chao Yang

Daqing Sun

Matthew R Kaller

Xuelei Yan

Paul John Dransfield

Yosup Rew

Vatee Pattaropong

Ernest J Prisbe

Daniel B Horne

Mikkel V Debenedetto

Su-Jen Lai

Simon J Hedley

Frank Kayser

Ted Charles Judd

Zhihong Li

Liusheng Zhu

Timothy David Cushing

Felix Gonzalez Lopez De Turiso

Alan C Cheng

Norbert W Bischofberger

Brian Stuart Lucas

Robert S McDowell

Matthew A Williams

Thomas Gadek

John C Rohloff

Lijun Zhang

Kenneth M Kent

Valeria R Fantin

Gayathri Swaminath

Brent K Blackburn

Yi Heng Chen

Robert Michael Rzasa

Dustin L McMinn

Dawei Zhang

Xiaolin Hao

Brian M Fox

Youngsook Shin

Xiao He

Wen-Chen Yeh

Kirk D Robarge

Sarah Lively

Andreas Reichelt

Todd C Somers

Yinhong Chen

Aarif Yusuf Khakoo

Pingchen Fan

Kuei-Ying Lin

Rajiv Sharma

Robert J Jones

Hisashi Shinkai

Kexue Li

Murty N Arimilli

John A Flygare

Juan Carlos Jaen

William A Lee

Wenjin Yang

Ming Yu

Michael G Johnson

Jonathan Dante Low

Prabhakar Kondaji Jadhav

Jiwen Liu

Xianghong Wang

Michael D Bartberger

Hilary Plake Beck

Jin-Long Chen

Christopher Neil Farthing

Ana Zurisadai Gonzalez Buenrostro

Darin J Gustin

Yingcai Wang

Stephen Clinton Young

John Walter Liebeschuetz

Bing Yang

Stuart Donald Jones

Brian Gregory Lucas

Joel McIntosh

Sebastien Caille

Patrick C Kearney

Jian Zhang

Pingyu Ding

Thomas T Nguyen

Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R, R, R, R, R, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.

Opioid receptor modulators and products and methods related thereto

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

Inhibitors of glucocorticoid receptor

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Triazole agonists of the APJ receptor

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110&#x3b4; activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Heterocyclic compounds and their uses

Compounds of Formula VII, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula VII have the following structure: where the definitions of the variables are provided herein.

Intermediates for preparing triazole agonists of the APJ receptor

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Processes of making and crystalline forms of a MDM2 inhibitor

Methods of preparing compounds of Formula VI, salts thereof, tautomers thereof, or salts of the tautomers include cyclizing compounds of Formula V, salts thereof, tautomers thereof, or salts of the tautomers. Compounds of Formula VI and Formula V have the following structures: where the definitions of the variables are provided herein.

Methods for preparing triazole agonists of the APJ receptor

Compounds of Formula V, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula V have the following structure: where the definitions of the variables are provided herein.

Growing community of inventors

Pacifica, CA, United States of America

Lawrence R McGee