Pfizer Corporation

Acurx Pharmaceuticals, LLC

Pharmacia Corporation

Other

Ensemble Therapeutics Corporation

Li Huang Xing

Liying Zhang

Brian Stephen Gerstenberger

Andrew Fensome

Mark E Schnute

Eddine Saiah

Zhao-Kui Wan

Andrew Christopher Flick

Matthew Frank Brown

Peter M Jones

Ariamala Gopalsamy

Matthew Merrill Hayward

Scot Richard Mente

Neelu Kaila

Dafydd Rhys Owen

Stephen Wayne Wright

John David Trzupek

Michael L Vazquez

Edouard Zamaratski

Balekudru Devadas

Shaun Raj Selness

Rayomand Jal Unwalla

Ivan Viktorovich Efremov

John Isidro Trujillo

Xiaojing Yang

Betsy Susan Pierce

Jean-Baptiste Telliez

Alpay Dermenci

Goran Mattias Wennerstal

Casey Cameron McComas

Xiang Y Yu

Minghua Wang

Richard Soll

Michael Silverman

Shuang Liu

Richard C Durley

Margaret Lanahan Grapperhaus

Brian S Hickory

Ian L Scott

Michele A Promo

Susan Landis Hockerman

Rajesh Devraj

Terri L Boehm

Robert Owen Hughes

Christoph Wolfgang Zapf

Daniel Patrick Walker

Paul Vincent Rucker

John Robert Springer

Seungil Han

Thomas Dale Owen

Kevin D Jerome

Win Naing

John Walker

Aruna Sambandam

Edgardo Alvira

Huey S Shieh

Michelle Ann Schmidt

Heather M Madsen

Radhika M Blevis-Bal

Laura D Marruto

Danny James Garland

Jeff Hitchcock

Kevin F McGee

John Jeffrey Talley

David Louis Brown

E Ann Hallinan

Lijuan Jane Wang

Joseph Walter Strohbach

Francis J Koszyk

John Paul Mathias

Bruce C Hamper

Atli Thorarensen

Cindy L Ludwig

Xiaolun Wang

James Robert Blinn

Steven W Kramer

Yi Yu

Stephen Paul Hale

Agustin Casimiro-Garcia

Karl W Aston

Jason Shaoyun Xiang

Marvin Jay Meyers

Kelley C Shortsleeves

Renee Huff

Felix Vajdos

Ravi G Kurumbail

Benjamin A Seigal

Timothy F Briggs

Frank G Favaloro, Jr

Steven J Kirincich

Nicholas K Terrett

William H Connors

Cheri Snedeker

Tyler J Cipriani

Dingxue Yan

Sethu L Alexander

Jeffry Carter

John Springer

Subo Laio

Angela Deprow

A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A' and A″ are independently O, C═O, C—R′ or N—R″, where R′ and R″ may independently be H, amino, —NRCOR, COR, —CONRR, C-Calkyl, or hydroxy(C-Calkyl), and R″ may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A′ and A″ is O or C═O; Rand R are independently H, Br, Cl, F, or C-Calkyl; Ris H, C-Calkyl, or hydroxy(C-Calkyl); Ris selected from the group consisting of H, C-Calkyl, C-Calkoxy, hydroxy(C-Calkyl), phenyl(C-Calkyl), formyl, heteroaryl, heterocyclic, —COR, —OCOR, —COOR, —NRCOR, —CONRR, and —(CH)—W, where W is cyano, hydroxy, C-Ccycloalkyl, —SONRR, and —SO—R, where Ris C-Calkyl, C-Ccycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C-Calkyl; X is C—Ror N, where Rmay be H or C-Calkyl; Rand Rare independently H, amino, C-Calkyl, or hydroxy(C-Calkyl); R, Rand Rare each independently H, C-Calkyl, C-Calkoxy(C-Calkyl), or C-Ccycloalkyl, said C-Calkyl is optionally substituted by halo, CN or hydroxy; or, Rand Rtogether with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C-Calkyl; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.

Pyrazolo[1,5-a]pyrazin-4-yl derivatives

There is a method for treating a psoriasis. A compound is administered in a therapeutically effective amount to a subject suffering therefrom. The compound has the structure or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.

A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.

Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives

A compound compound having the structure: or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C-Calkyl, C-Calkoxy, C-Ccycloalkyl, aryl, heteroaryl, aryl(C-Calkyl), CN, amino, alkylamino, dialkylamino, CF, or hydroxyl; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, &#x2014;(C&#x2550;O)NR&#x2014;, and &#x2014;(CRR)&#x2014;, where Ris H or C-Calkyl, and Rand Rare independently hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, aryl(C-Calkyl), heteroaryl, (C-Calkyl)heteroaryl, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, &#x2014;(C&#x2550;O)NR&#x2032;, &#x2014;NR&#x2032;(C&#x2550;O)&#x2014;, and &#x2014;(CR&#x2032;R&#x2032;)&#x2014;, where R&#x2032; is H or C-Calkyl, and R&#x2032; and R&#x2032; are independently hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, aryl(C-Calkyl), heteroaryl, (C-Calkyl)heteroaryl, heteroaryl(C-Calkyl), and heterocyclic(C-Calkyl); Z is &#x2014;(CH)&#x2014; or a bond, where one or more methylene units are optionally substituted by one or more C-Calkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; Rand R&#x2032; are independently selected from the group consisting of hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, heteroaryl, aryl(C-Calkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C-Calkyl, halo, CN, C-Calkylamino, C-Ccycloalkyl, etc.; Ris selected from the group consisting of hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; Ris selected from the group consisting of hydrogen, deuterium, and amino; Ris monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C-Calkyl, heterocycloalkyl, halo, C-Ccycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C-Calkyl, halo, CN, OH, alkoxy, amino, &#x2014;COH, &#x2014;(CO)NH, &#x2014;(CO)NH(C-Calkyl), or &#x2014;(CO)N(C-Calkyl), and where said alkyl may be further substituted by one or more fluorine atoms; Ris independently selected from the group consisting of hydrogen, C-Calkyl, C-Calkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

Aminopyrimidinyl compounds

The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections. 

DNA polymerase IIIC inhibitors and use thereof

A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, etc.; Z is &#x2014;(CH)&#x2014; or a bond, etc.; Rand Rare independently selected from the group consisting of hydrogen, alkyl, etc.; Ris selected from hydrogen, alkyl, etc.; Ris selected from the group consisting of hydrogen, and amino; Ris monocyclic or bicyclic, etc.; Ris independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

A compound compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A' and A&#x2033; are independently O, C&#x2550;O, C&#x2014;R&#x2032; or N&#x2014;R&#x2033;, where R&#x2032; and R&#x2033; may independently be H, amino, &#x2014;NRCOR, COR, &#x2014;CONRR, C-Calkyl, or hydroxy(C-Calkyl), and R&#x2033; may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A&#x2032; and A&#x2033; is O or C&#x2550;O; Rand R are independently H, Br, Cl, F, or C-Calkyl; Ris H, C-Calkyl, or hydroxy(C-Calkyl); Ris selected from the group consisting of H, C-Calkyl, C-Calkoxy, hydroxy(C-Calkyl), phenyl(C-Calkyl), formyl, heteroaryl, heterocyclic, &#x2014;COR, &#x2014;OCOR, &#x2014;COOR, &#x2014;NRCOR, &#x2014;CONRR, and &#x2014;(CH)&#x2014;W, where W is cyano, hydroxy, C-Ccycloalkyl, &#x2014;SONRR, and &#x2014;SO&#x2014;R, where Ris C-Calkyl, C-Ccycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C-Calkyl; X is C&#x2014;Ror N, where Rmay be H or C-Calkyl; Rand Rare independently H, amino, C-Calkyl, or hydroxy(C-Calkyl); R, Rand Rare each independently H, C-Calkyl, C-Calkoxy(C-Calkyl), or C-Ccycloalkyl, said C-Calkyl is optionally substituted by halo, CN or hydroxy; or, Rand Rtogether with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C-Calkyl; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I) 

Bruton's tyrosine kinase inhibitors

The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacteria infections. 

A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, etc.; Z is &#x2014;(CH)&#x2014; or a bond, etc.; Rand R&#x2032; are independently selected from the group consisting of hydrogen, alkyl, etc.; Ris selected from hydrogen, alkyl, etc.; Ris selected from the group consisting of hydrogen, and amino; Ris monocyclic or bicyclic, etc.; Ris independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR&#x3b3; activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

Methyl- and trifluromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof

The present invention provides sulfonamide-substituted indoles and Methods of Use Thereof-substituted pyrrolopyridines, pharmaceutical compositions thereof methods of modulating RORy activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such indoles and pharmaceutical compositions thereof.

Sulfonamide-substituted indole modulators of RORC2 and methods of use thereof

The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR&#x3b3; activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

Methyoxy-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof

Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Heterocyclic compounds as inhibitors of Vanin-1 enzyme

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Lexington, MA, United States of America

Li Huang Xing