Pharmacia Corporation

Pfizer Corporation

Sugen Incorporated

Stephen A Kolodziej

John Nicholas Freskos

Daniel Paul Becker

Deborah A Mischke

Joseph J McDonald

Jennifer R Zhang

Thomas E Barta

Clara I Villamil

Jingrong Jean Cui

William F Vernier

Joseph Gerace Rico

Susan Landis Hockerman

Terri L Boehm

Louis J Bedell

Cathleen Elizabeth Hanau

Jeffery N Carroll

Lei Jia

Pei-Pei Kung

G Davis Harris, Jr

Dilip Ramakant Bhumralkar

Mitchell David Nambu

Mason Alan Pairish

Hong Shen

Iriny Botrous

Michelle Bich Tran-Dube

Fang-Jie Zhang

Nathan W Stehle

Jerry Jialun Meng

Lee Andrew Funk

Ji Yu Chu

Christopher G Nelson

Xiaoyuan (Sharon) Li

John Jeffrey Talley

Gunnar J Hanson

Daniel P Getman

Ish K Khanna

Robert M Heintz

David Louis Brown

Yvette M Fobian

Lijuan Jane Wang

Margaret Lanahan Grapperhaus

Mark A Massa

Monica B Norton

Emily J Reinhard

Alan Frank Gasiecki

Brent V Mischke

Darren J Kassab

Shridhar G Hegde

G Davis Harris

Patrick B Mullins

Allison Walter

Jason (Qishen) Lin

Joanne Johnson

Madeleine H Li

Michelle A Schmidt

Carol Pearcy Howard

Theresa R Fletcher

Mark A Nagy

Gary A DeCrezcenzo

David R Anderson

Thomas A Wynn

Yiyuan Chen

Dilip Bhumralkar

Jason(qishen) Lin

Xiaoyuan(sharon) Li

Jingjong Jean Cui

Jason Lin

G Davis Harris Jr

Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET. 

Aminoheteroaryl compounds as protein kinase inhibitors

Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET 

This invention is directed generally to proteinase (also known as 'protease') inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as 'matrix metalloprotease' or &#x201c;MMP&#x201d;) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A, A, Y, E, E, E, and Rare as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.

Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors

A method of making aminocyanopyridine compounds which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2 is described.

Method of making tricyclic aminocyanopyridine compounds

A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein Rand Rare both hydrido or Rand Rtogether with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. Rin formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Aromatic sulfone hydroxamic acid metalloprotease inhibitor

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Ballwin, MO, United States of America

Stephen A Kolodziej