Theravance, Inc.

Theravance Biopharma R&d Ip, LLC

Relypsa, Inc.

Nektar Therapeutics

Vifor (international) Ltd.

Advanced Medicine, Inc.

YongQi Mu

Mathai Mammen

Craig Husfeld

Li Li

Yuhua Ji

Yu-Hua Ji

Rick Andrew Lee

Eric L Stangeland

YuHua Ji

J Kevin Judice

Aaron Kushner

Trevor Mischki

Paul Ross Fatheree

Guang Yu Yang

Martin Sheringham Linsell

Michael Robert Leadbetter

Cameron Smith

Yan Zhu

Sean Gary Trapp

John L Pace

Bernice M T Lam

Michael W Conner

Adam D Hughes

Christopher W Lange

Johnny Uy

Sarah Dunham

Scott J Hecker

Paul Mansky

Eric F Connor

Neel Kumar Anand

Bo-Liang Deng

Michael James Cope

Kalpesh N Biyani

Jun Shao

David E Bergbreiter

Donogh John Roger O'Mahony

Natalia Aurrecoechea

Deidre Madsen

Faleh Salaymeh

Angela Lee

Elizabeth Goka

Jeng-Pyng Shaw

Inez Lees

Hongmin Zhang

Antoni Kozlowski

Jennifer A Riggs-Sauthier

Xiaoming Shen

Timothy A Riley

Zhongxu Ren

Pankaj Sharma

Xuyuan Gu

Yuan Song

Jordan Kopping

Grace Huynh

Xuejun Yuan

Aleksandrs Odinecs

Michael Lixin Shen

Jeng Pyng Shaw

Vijay Kumar Khatri

Leticia Maria Preza

Grace May

Xinnan Zhang

Erik Krogh-Jespersen

This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar, R, R, R, R, R, R, and Rare as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Biphenyl compounds useful as muscarinic receptor antagonists

The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine

The present invention generally relates to processes for converting acrylate esters or a derivative thereof to difluoropropionic acid or a derivative thereof. This process is generally performed using fluorine gas in a hydrofluorocarbon solvent.

Fluorination of acrylate esters and derivatives

The present invention relates to compounds and their use as ligands for mu opioid receptors. Also included are methods for preparing the compounds and pharmaceutical compositions containing the compounds. In one or more embodiments of the invention, a compound according to Formula I is provided: and pharmaceutically acceptable salts thereof, wherein R-Rare as described herein. 

Morphinan derivatives for the treatment of neuropathic pain

The present invention generally relates to processes for converting acrylate esters or a derivative thereof to difluoropropionic acid or a derivative thereof. This process is generally performed using fluorine gas in a hydrofluorocarbon solvent. In particular, a process for fluorinating a double bond is disclosed. This process comprises forming a reaction mixture comprising a hydrofluorocarbon solvent, fluorine gas, and a compound of formula 1 wherein Ris hydroxy, alkoxy, chloro, or &#x2014;OC(O)CH&#x2550;CHto form a compound of formula 2 in a yield of at least 50% wherein Ris hydroxy, alkoxy, chloro, &#x2014;OC(O)CHFCHF, wherein the hydrofluorocarbon solvent comprises 2H,3H-decafluoropentane and the reaction mixture further comprises a fluorination agent.

The present invention provides a crosslinked amine and amide polymers effective for binding and removing bile salts from the gastrointestinal tract. These bile acid binding polymers or pharmaceutical compositions thereof can be administered to subjects to treat various conditions, including hypercholesteremia, diabetes, pruritis, irritable bowel syndrome-diarrhea (IBS-D), bile acid malabsorption, and the like.

Crosslinked polyvinylamine, polyallylamine, and polyethyleneimine for use as bile acid sequestrants

The present disclosure generally relates to processes for converting acrylate esters or a derivative thereof to difluoropropionic acid or a derivative thereof. This process is generally performed using fluorine gas in a hydrofluorocarbon solvent. In particular, a continuous process for fluorinating a double bond is disclosed, the process comprising forming a reaction stream comprising a compound of formula 1 or formula 5 dissolved in a hydrofluorocarbon or fluorocarbon solvent, wherein Ris hydroxy, alkoxy, chloro, or &#x2014;OC(O)CH&#x2550;CHthe reaction stream flowing through a continuous fluorination reactor at a flow rate of from about 0.2 mL/minute to about 2 mL/minute and fluorine gas flows through the continuous fluorination reactor at a gas flow rate of from about 0.2 mmol/minute to about 2 mmol/minute; whereby reaction of the compound of formula 1 or formula 5 with the fluorine gas forms a compound of formula 2 or formula 6 wherein Ris hydroxy, alkoxy, chloro, or &#x2014;OC(O)CHFCHF.

The present invention provides crosslinked amine polymers effective for binding and removing bile salts from the gastrointestinal tract. These bile acid binding polymers or pharmaceutical compositions thereof can be administered to subjects to treat various conditions, including hypercholesteremia, diabetes, pruritus, irritable bowel syndrome-diarrhea (IBS-D), bile acid malabsorption, and the like.

Amine polymers for use as bile acid sequestrants

Growing community of inventors

Los Altos, CA, United States of America

YongQi Mu