Biogen Ma Inc.

Biogen Idec Ma Inc.

Sunesis Pharmaceuticals, Inc.

Millennium Pharmaceuticals Limited

Millenium Pharmaceuticals, Inc.

Boigen Ma Inc.

Edward Yin-Shiang Lin

Kevin Guckian

Gnanasambandam Kumaravel

Jermaine Thomas

Bin Ma

Guo Zhu Zheng

Richard Dana Caldwell

Arthur G Taveras

Xiaogao Liu

Wen-Cherng Lee

Daniel M Scott

Zhan Shi

Sha Mi

Lei Zhang

Lihong Sun

Daniel A Erlanson

Timothy Raymond Chan

Kurt D Van Vloten

Zhili Xin

Deping Wang

Robert Lowell Simmons

Stig Hansen

Kathy Jingyuan Cao

Joseph Arndt

Nuzhat Pathan

Bradley T Tangonan

Kenneth Egnard Lind

Jianhua Chao

John Howard Jones

Brian Stuart Lucas

Hairuo Peng

Istvan J Enyedy

TeYu Chen

Andrew George Capacci

Ma Bin

Daniel Erlanson

Kurt Van Vloten

Kevin M Guckian

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

NRF2 activator

The present invention provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and their use in modulating the activity of S1P) receptors. Also provided is a pharmaceutical composition comprising the compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient or carrier.

S1P modulating agents

Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

SIP modulating agents

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Bicyclic aryl sphingosine 1-phosphate analogs

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Heterobicyclic sphingosine 1-phosphate analogs

The present invention provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and their use in modulating the activity of S1P receptors. Also provided is a pharmaceutical composition comprising the compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient or carrier.

The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

Heterocyclic compounds useful as PDK1 inhibitors

The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.

Methods of treatment using pyridinonyl PDK1 inhibitors

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

Compounds of formula (I) or (II) can modulate the activity of SIP receptors.

Growing community of inventors

Ashland, MA, United States of America

Edward Yin-Shiang Lin