Pfizer Corporation

Stephen Wayne Wright

Joseph Walter Strohbach

David Hepworth

Frank Eldridge Lovering

Christoph Martin Dehnhardt

Eddine Saiah

Christoph Wolfgang Zapf

Nikolaos Papaioannou

Arthur Lee

Katherine Lin Lee

John David Trzupek

Seungil Han

Lori Krim Gavrin

John Paul Mathias

Dafydd Rhys Owen

Akshay Patny

Kevin Joseph Curran

Xiaolun Wang

Joel A Goldberg

Michael Dennis Lowe

Richard Vargas

Matthew Frank Brown

David R Anderson

Mark Edward Bunnage

Horng-Chih Huang

Matthew Merrill Hayward

Li Huang Xing

Brian Stephen Gerstenberger

Andrew Fensome

Betsy Susan Pierce

Xiaojing Yang

Alpay Dermenci

Robert L Dow

Christophe Philippe Allais

Keith Michael DeVries

Agustin Casimiro-Garcia

Felix Vajdos

Chulho Choi

Joel Adam Goldberg

David Randolph Anderson

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

Bicyclic-fused heteroaryl or aryl compounds

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

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

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

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

Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme

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.

Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators

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

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

This invention relates to processes for preparing compounds of the formula (I)

Process for substituted pyridines

Growing community of inventors

Old Lyme, CT, United States of America

Stephen Wayne Wright