Biogen Ma Inc.

Abbott Laboratories Corporation

Mcgill University

Millennium Pharmaceuticals Limited

Sunesis Pharmaceuticals, Inc.

Abbvie Inc.

Isis Pharmaceuticals, Inc.

Zhili Xin

Gnanasambandam Kumaravel

Kevin Guckian

Lei Zhang

Hairuo Peng

Gang Liu

Jeffrey Vessels

Bin Ma

John Howard Jones

Lihong Sun

Arthur G Taveras

Zhonghua Pei

Eric Marsault

Yi Jin

George Just

Philip R Kym

Sha Mi

Zhaohui Shao

Edward Yin Shiang Lin

Nathan Genung

Ryan Gianatassio

Andrew J Souers

Alexey Alexandrovich Lugovskoy

Hiroko Tanaka

Bo Liu

Bing Guan

Noel Aaron Powell

Brian Raimundo

Jennifer Cossrow

Thomas Wynn

Hongyu Zhao

Hing L Sham

Martin Winn

Deping Wang

Todd M Hansen

Rajesh R Iyengar

Felix Gonzalez Lopez De Turiso

James T Link

Bruce G Szczepankiewicz

Gang Zhao

Jianchao Wang

Martin Himmelbauer

Vince S Yeh

Edward Yin-Shiang Lin

Timothy Raymond Chan

Michael A Dechantsreiter

Weirong Chen

Ju Gao

Tom W Von Geldern

Benjamin Lane

Lloyd Franklin

Adam Littke

Michael D Serby

Mei Liu

Muthiah Manoharan

Steven Armen Boyd

Richard F Clark

Jyoti R Patel

Gui-Dong Zhu

Andrew S Judd

Jianhua Chao

Hwan-soo Jae

Brian Stuart Lucas

Alexey V Ishchenko

Istvan J Enyedy

Robert F Keyes

Indrani W Gunawardana

Sheldon Wang

David A Janowick

John K Lynch

Michael A Staeger

Lissa T J Nelson

Jennifer C Freeman

Tom Von Geldern

TeYu Chen

Tianyuan Zhang

Kurt D Van Vloten

Andrew George Capacci

Barbara L Cool

Yugui Gu

Ernst U Frevert

Kevin M Guckian

Lioyd Franklin

Bo X Liu

Todd Matthew Hansen

Described herein are compounds represented by formula (I) (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R, R, R, Y, Y, and Z are as defined herein.

Azetidinyl O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitors

Provided are compounds of Formula (I): including compounds of Formulas (II), (III) and (IV), wherein X, R, R, Rand n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

ASK1 inhibiting agents

Described herein are compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R, R, R, Y, Y, m, n, and p are as defined herein.

Morpholinyl, piperazinyl, oxazepanyl and diazepanyl O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

Described herein are compounds represented by formulas (IA) or (IB) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables R, R, R, Y, Y, Ar, Z and n are as defined herein.

O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitors

O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors

Provided are compounds of Formula (I): Formula (I), including compounds of Formulas (II), (III), (IV), (V) and (VI), wherein X, R, R, R, Rand n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Described herein are compounds represented by formula (I&#x2033;) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, R, R, m, n, Y, Y, Rand Rare defined herein.

O-glycoprotein-2-acetamido-2-deoxy-3-D-glycopyranosidase inhibitors

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.

NRF2 activator

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

Compounds that are S1P modulating agents and/or ATX modulating agents

Compounds of formula (I) can modulate the activity of autotaxin (ATX). 

ATX modulating agents

Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 

The present invention provides methods of inhibiting Raf kinase activity in a patient, the method comprising administering to the patient a compound having formula I: or a pharmaceutically acceptable salt thereof, wherein R, R, R, L, L, Cy, and Cyare as defined as set forth in the specification.

Substituted pyrimidines for inhibiting Raf kinase activity

Compounds of formula (I) wherein: X is &#x2014;O&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;CH&#x2014;, or &#x2014;NR&#x2014;, wherein r is 0, 1, or 2; X, X, and Xare each independently CRor N; one of Xor Xis C and is attached by a single bond to -L-, and the other is CRor N, provided that no more than three of X, X, X, X or Xare N; Ring A is monocyclic Cscycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or O; wherein Ring A is further optionally substituted with from 1 to 3 R; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, &#x2014;O&#x2014;, &#x2014;NR&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;CH&#x2014;, or &#x2014;C(O)&#x2014;, wherein n is 0, 1, or 2; 1 2 Lis an Calkylene, Ccycloalkylene, &#x2014;CH-L-, or a 3- to 8-membered heterocyclylene comprising 1 to 5; Ris Calkyl or a monocyclic Ccycloalkyl; wherein said Ccycloalkyl is substituted with at least one Rand may be optionally substituted with from 1 to 5 additional Rsubstituents, wherein Rfor each occurrence is independently selected; and Ris &#x2014;C(O)OR, &#x2014;C(O)N(R)&#x2014;S(O)R, &#x2014;S(O)OR, &#x2014;C(O)NHC(O)R, &#x2014;Si(O)OH, &#x2014;B(OH), &#x2014;N(R)S(O)R, &#x2014;S(O)N(R), &#x2014;O&#x2014;P(O)(OR), or &#x2014;P(O)(OR), &#x2014;CN, &#x2014;S(O)NHC(O)R, &#x2014;C(O)NHS(O)R3, &#x2014;C(O)NHOH, &#x2014;C(O)NHCN, &#x2014;CH(CF)OH, &#x2014;C(CF)OH, or a selected heteroaryl or heterocyclyl; and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 

S1P and/or ATX modulating agents

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Lexington, MA, United States of America

Zhili Xin