Concert Pharmaceuticals, Inc.

Vertex Pharmaceuticals, Inc.

Merrell Pharmaceuticals, Inc.

Other

Merrell Dow Pharmaceuticals

Sun Pharmaceutical Industries Limited

Scott L Harbeson

Roger D Tung

Julie Fields Liu

Craig E Masse

Luc J Farmer

Mark Andrew Murcko

David D Deininger

Govinda Rao Bhisetti

Rose A Persichetti

Stephen H Buck

James R McCarthy

Jeremy Green

Bhaumik Pandya

Xuejun Tang

Guy W Bemis

Mark Willem Ledeboer

Alan J Bitonti

John E Cochran

Jon H Come

Julie A Straub

Michael J Arnost

John L Krstenansky

Elizabeth M Kudlacz

I Robert Silverman

Adam J Morgan

Craig Marhefka

Thomas J Owen

Ly Pham

Chester F Hassman, Iii

Julie F Liu

Vladimir Savic

James R Mccarthy

Chester F Hassman

This invention relates to novel thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of binding between an acetylated histone and a bromodomain-containing protein.

Deuterated OTX-015

This invention relates to novel inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase.

Inhibitors of the enzyme UDP-glucose: N-acyl-sphingosine glucosyltransferase

This invention relates to novel substituted triazolobenzodiazepines of the Formula I: wherein each of the variables are defined herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering I-BET762.

Substituted triazolobenzodiazepines

This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Substituted xanthine derivatives

This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Zis hydrogen or fluorine; Zis hydrogen, deuterium, or fluorine; Zis deuterium; Zis fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Zand Zare hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.

Deuterated pyrazino[2,1-a]isoquinoline compounds and methods of treatment using the same

This invention relates to novel substituted triazolobenzodiazepines of the Formula (I), wherein each of the variables are defined herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering I-BET762. 

The present invention in one embodiment provides a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, wherein Y, Yand Yare each independently selected from hydrogen and deuterium; R, R, and Rare each methyl and are independently substituted with 0 to 3 deuterium; and Ris t-butyl and is substituted with 0 to 9 deuterium; provided that if R, Rand Rare each &#x2014;CH, and Ris &#x2014;C(CH), then at least one of Yand Yis deuterium. 

Substituted thienotriazolodiazapines

The present invention is directed to a process for preparing a 2,26,6-d-morpholine derivative represented by Structural Formula (I): or a salt thereof.

Synthesis of deuterated morpholine derivatives

This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentifylline and related compounds are beneficial.

The present invention in one embodiment provides a compound of Formula A: or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising the compound; and methods of treating the indications disclosed herein.

Deuterated derivatives of ruxolitinib

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Cambridge, MA, United States of America

Scott L Harbeson