Pfizer Corporation

Advanced Optical Technologies, Inc.

Other

Abl IP Holding LLC

Pfizer Products Inc.

Matthew Frank Brown

Mark Edward Flanagan

Justin Ian Montgomery

Ye Che

Matthew Merrill Hayward

Usa Reilly

Jack C Rains, Jr

Adam Matthew Gilbert

Rayomand Jal Unwalla

Michael Joseph Melnick

Anthony Marfat

Timothy Allan Johnson

Li Huang Xing

Todd A Blumenkopf

Dafydd Rhys Owen

Stephen Wayne Wright

Brian Stephen Gerstenberger

Andrew Fensome

Christopher Stanley Poss

Atli Thorarensen

John Isidro Trujillo

Xiaojing Yang

Agustin Casimiro-Garcia

Jean-Baptiste Telliez

Paul S Changelian

Alpay Dermenci

Michael Aaron Brodney

Lei Zhang

Joseph Walter Strohbach

Christopher Ryan Butler

Jotham Wadsworth Coe

Ruth Elizabeth TenBrink

Erik Alphie LaChapelle

Neelu Kaila

John David Trzupek

Laura Ann McAllister

Andrea Joy Gonzales

Michael L Vazquez

Mark J Mitton-Fry

Michael Joesph Melnick

Jonathan David Langille

Mihir D Parikh

Christopher Bates

Loren Michael Price

Mark Stephen Plummer

Ashley Edward Fenwick

David P Ramer

Laura Cook Blumberg

Clarke Bentley Taylor

Edmund Lee Ellsworth

Elizabeth Mary Beck

Joseph Scott Warmus

Sean Timothy Murphy

Denton Wade Hoyer

Jinshan Michael Chen

Manjinder Singh Lall

Debra Ann Sherry

Daniel Paul Uccello

Charles Francis Donovan

John I Trujillo

John Charles Kath

Richard Andrew Ewin

Tamim F Braish

Chris Limberakis

Ronald P Gladue

Sidney Xi Liang

Seungil Han

Felix Vajdos

Andrei Shavnya

Timothy Allen Johnson

Andre Shavnya

Joseph Alan Abramite

Hud Lawrence Risley

Ruth E Tenbrink

Veerabahu Shanmugasundaram

Chris Lim-Berakis

Molly A McGlynn

Gregory D Lundquist

Joseph A Abramite

Gregory Dean Lundquist

Jeremy T Starr

Andrea Gonzales

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

The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description.

Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides

The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III wherein Q is selected from the group consisting of —P(O)(OH), —P(O)(OH)(OM), —P(O)(OM)and —P(O)(O)M; Mat each occurrence is a pharmaceutically acceptable monovalent cation; and Mis a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

Fluoro-pyridinone phosphates and boronates useful as antibacterial agents

The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R, R, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

5,7-dihydro-pyrrolo-pyridine 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

The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R)a, (R)b, (R)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder. 

Dihydro-pyrrolo-pyridine derivatives

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

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.

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof

A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein A, A' and A&#x2033; are independently O, C&#x2550;O, etc.; 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, etc.; R, Rand Rare each independently H, C-Calkyl, C-Calkoxy(C-Calkyl), etc.; 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

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Pyrrolo[2,3-D]pyrimidine derivatives

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Stonington, CT, United States of America

Matthew Frank Brown