Pfizer Corporation

Schering Corporation

Merck Sharp + Dohme Corp.

Schering-plough Corporation

Xiaojing Yang

Anantha R Sudhakar

Dafydd Rhys Owen

Daw-long Albert Kwok

Matthew Frank Brown

Matthew Merrill Hayward

Tiruvettipuram K Thiruvengadam

George G Wu

Li Huang Xing

Frank Xing Chen

Marc Poirier

Stephen Wayne Wright

Brian Stephen Gerstenberger

Tao Wang

Andrew Fensome

Jing Liao

Hoa N Nguyen

Ji Xie

Mingsheng Huang

Ngiap Kie Lim

Jian Cui

Alpay Dermenci

Vijay Sabesan

Minzhang Chen

Ilia A Zavialov

Jeonghan Park

Eugene John Vater

Juergen Weber

Weidong Tong

Ramani R Raghavan

Ingyu Jeon

Maria M Tamarez

Patrick Robert Verhoest

Jamison Bryce Tuttle

Martin Youngjin Pettersson

George S K Wong

Matthew Forrest Sammons

Matthew Richard Reese

Qingyi Yang

Liuqing Wei

George S Wong

Daw-Iong Albert Kwok

Vijay Sabesen

Daw-Jong Kwok

Amanda Patrice Surajhie Samuel

Illia Zavialov

Daw-Long Kwok

Ilia Zavialov

The present invention discloses a novel crystalline form of ((S)-2,2-difluorocyclopropyl)-((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)-pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone free base, pharmaceutical composition containing the same, preparations thereof and uses thereof.

Crystalline pyrimidinyl-3,8-diazabicyclo[3.2.1]octanylmethanone compound and use 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 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 invention relates to compounds of Formula I&#x2033; wherein R, R, R, R, p, q and q' are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

Nitrile-containing antiviral compounds

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 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.

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 application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: 

Exo- and diastereo-selective synthesis of himbacine analogs

Exo- and diastereo- selective synthesis of himbacine analogs

Exo- and diastereo-selective syntheses of himbacine analogs

In one embodiment, the present application relates to a process of making a compound of formula I. and to certain intermediate compounds that are made within the process of making the compound of formula I.

[object Object]

Exo- and diastereo- selective syntheses of himbacine analogs

Process and intermediates for the preparation of (1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates for salts thereof

Process and intermediates for the preparation of (1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates or salts thereof

Growing community of inventors

Waterford, CT, United States of America

Xiaojing Yang