Pfizer Corporation

Monsanto Technology LLC

Pharmacia & Upjohn Company

Daniel Patrick Walker

David W Piotrowski

Eric Jon Jacobsen

Vincent E Groppi, Jr

Brad A Acker

Donn G Wishka

Jason K Myers

Terri L Boehm

Jeffery N Carroll

G Davis Harris, Jr

Justin Robert Struble

Matthew D McReynolds

Mangesh Bore

Balekudru Devadas

Bruce Nelsen Rogers

Margaret Lanahan Grapperhaus

Eddine Saiah

Shaun Raj Selness

Susan Landis Hockerman

Mark E Schnute

William H Miller

Li Huang Xing

Robert Owen Hughes

Christoph Wolfgang Zapf

Zhao-Kui Wan

John Robert Springer

Seungil Han

Michelle Ann Schmidt

Steven Charles Reitz

Danny James Garland

David Andrew Griffith

Angel Guzman-Perez

Mary Theresa Didiuk

Jeffrey W Corbett

Kevin K Liu

Alice L Bodnar

Feng C Bi

Mark R Rauckhorst

Loretta J Walker

Mark Edward Schnute

Matthew D Mcreynolds

Jr G Davis Harris

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 disclosure relates, in general, to 5-halo-3,6-dichlorosalicylic acid compounds, 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 5-halo-3,6-dichlorosalicylic acid compounds, processes for preparing 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 3,6-dichlorosalicylic acid compounds, and processes that employ such compounds as intermediates in the preparation of the herbicide dicamba.

3,6-dichlorosalicylic acid compounds and related synthetic processes

Provided herein are processes for the preparation of heteroaryl carboxylic acids.

Processes for the preparation of heteroaryl carboxylic acids

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 diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 

Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole).

Processes for the preparation of 2-thiophenecarbonyl chloride

The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R, R, R, Rand Rare as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

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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.

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

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Kalamazoo, MI, United States of America

Daniel Patrick Walker