Pfizer Corporation

Pharmacia & Upjohn Company

Brad A Acker

Eric Jon Jacobsen

David W Piotrowski

Daniel Patrick Walker

Vincent E Groppi, Jr

Kristine E Frank

Michael D Ennis

Donn G Wishka

Bruce Nelsen Rogers

Jian-Min Fu

Donald J Rogier

William W McWhorter, Jr

Jed F Fisher

Jeanette Kay Morris

Jason K Myers

Jackson B Hester, Jr

Steven Charles Reitz

Susan L Vander Velde

Michele A Promo

Horng-Chih Huang

Susan J Hartmann

Jeffrey W Corbett

Alice L Bodnar

Sergey Gregory Wolfson

Jin Xie

Mark R Rauckhorst

Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation. 

Pyrrolo[2,3-D]pyrimidine compounds

The invention provides compounds of Formula I: wherein Azabicyclo is where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which &#x3b1;7 is known to be involved.

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The invention provides compounds of Formula I:wherein Azabicyclo isW is a six-membered heterocyclic ring system having 1&#x2013;2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1&#x2013;2 substitutents independently selected from R. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which &#x3b1;7 is known to be involved.

Azabicyclic compounds for the treatment of disease

The invention provides compounds of Formula I:wherein Azabicyclo is any of:These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &#x3b1;7 is known to be involved.

Azabicyclic-phenyl-fused-heterocyclic compounds for treatment of disease

The invention provides compounds of Formula I:Azabicyclo-N(R)&#x2014;C(&#x2550;X)&#x2014;W&#x2003;&#x2003;Formula IThese compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &#x3b1;7 is known to be involved.

Azabicyclic-substituted-heteroaryl compounds for the treatment of disease

The invention provides compounds of Formula I:wherein Azabicyclo isThese compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &#x3b1;7 is known to be involved.

Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease

Disclosed are compounds of Formula (I):wherein R-R, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.

Substituted azepino[4,5b]indole derivatives

The invention provides compounds of Formula I:wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which &#x3b1;7 is known to be involved.

The present invention provides compounds of formula I:wherein R, R, X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I).

Tetracyclic azepinoindole compounds

The invention provides compounds of Formula I:These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which &#x3b1;7 is known to be involved.

Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease

The invention provides compounds of Formula I:These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which &#x3b1;7 is known to be involved.

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Kalamazoo, MI, United States of America

Brad A Acker