Amgen Inc.

Epiodyne, Inc.

Biomea Fusion, Inc.

Xiaodong Wang

Richard V Connors

Julio Cesar Medina

Xiaoqi Chen

Jeffrey Thomas Mihalic

Zhihua Ma

David John Kopecky

Julie Anne Heath

Zice Fu

Jeffrey Deignan

Steven H Olson

Lawrence R McGee

Jonathan B Houze

Paul John Dransfield

Vatee Pattaropong

Su-Jen Lai

Ning Chen

Nobuko Nishimura

Frank Kayser

Xiaohui Du

Matthew R Kaller

Daniel B Horne

Alan C Cheng

Mikkel V Debenedetto

Kevin Chao Yang

Ted Charles Judd

Gayathri Swaminath

Simon J Hedley

Wen-Chen Yeh

Yinhong Chen

Aarif Yusuf Khakoo

Robert P Farrell

John Eksterowicz

Jason A Duquette

Zhihong Li

Jiasheng Fu

Yihong Li

Benjamin Fisher

Dustin L McMinn

James S Harvey

Pingchen Fan

Pingyu Ding

Thomas T Nguyen

Daqing Sun

Xuelei Yan

Rajiv Sharma

Michael G Johnson

Yosup Rew

Felix Gonzalez Lopez De Turiso

Brian M Fox

Michael D Bartberger

Hilary Plake Beck

Ana Zurisadai Gonzalez Buenrostro

Darin J Gustin

Kexue Li

Joel McIntosh

Zhi-Liang Wei

Ulhas Bhatt

Philip M Roveto

Alok Nerurkar

Malgorzata Wanska

Frederick Seidl

Ming Yu

Jonathan Dante Low

Jiwen Liu

Brian Stuart Lucas

Yingcai Wang

Lars V Heumann

XianYun Jiao

Tien Widjaja

Michael W Gribble, Jr

Xin Huang

Kang Dai

SuJen Lai

Jiang Zhu

Martin Holan

John Lee

Heng Cheng

Corinne Sadlowski

Matthew Irvine Brown

Thorsten A Kirschberg

Nan-Horng Lin

Thomas Butler

Thu Phan

Michael J Schmitt

Ravindra B Upasani

Yongli Su

James T Palmer

David Sperandio

Christine Weathers

Dai Kang

Solomon B Ungashe

Amna Trinity-Turjuman Adam

Neil Howard Squires

Richard Victor Connors

Brian Matthew Fox

Philip Marley Roveto

Dustin Mcminn

Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.

Opioid receptor modulators

Disclosed herein are heterocyclic compounds, for example, according to the following formula and analogs thereof: that inhibit the activity of FLT3. Also described are specific covalent inhibitors of FLT3. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the FLT3 inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of proliferative diseases or conditions, including hematological malignancies and other diseases or conditions dependent on FLT3 activity.

Pyrazine compounds as inhibitors of FLT3

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

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 may 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.

Heteroaryl-substituted triazoles as APJ receptor agonists

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: (I); (II). Intermediates (V) are also claimed. 

Triazole furan compounds as agonists of the APJ receptor

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

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

Compounds for use in preparing heterocyclic triazole agonists of the APJ receptor

Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.

Methods of treating heart failure

Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may 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.

Heterocyclic triazole compounds as agonists of the APJ receptor

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

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.

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Johns Creek, GA, United States of America

Xiaodong Wang