Pharmacia Corporation

Monsanto Technology LLC

G.d. Searle & Company

Innov88 LLC

Warner-lambert Company

Jeffery N Carroll

Terri L Boehm

Deborah A Mischke

Joseph Gerace Rico

Gary A DeCrescenzo

Darren J Kassab

John Nicholas Freskos

Daniel Paul Becker

Joseph J McDonald

Thomas E Barta

Clara I Villamil

Susan Landis Hockerman

Shashidhar N Rao

Louis J Bedell

Yvette M Fobian

Nathan W Stehle

Daniel P Getman

William F Vernier

Daniel Patrick Walker

G Davis Harris, Jr

Justin Robert Struble

Matthew D McReynolds

Steve A Kolodziej

Mangesh Bore

John Jeffrey Talley

Michael B Tollefson

Lijuan Jane Wang

Monica B Norton

Joseph B Monahan

Anderson Gaweco

Stephen A Kolodziej

John Walker

Madeleine H Li

Patrick B Mullins

Carol Pearcy Howard

Jerry W Cubbage

Gunnar J Hanson

Ish K Khanna

Robert M Heintz

David Louis Brown

Margaret Lanahan Grapperhaus

Mark A Massa

Alan Frank Gasiecki

Brent V Mischke

Susan C Howard

Hui Li

Michelle A Schmidt

Theresa R Fletcher

Mark A Nagy

Thomas A Wynn

Gary A DeCrezcenzo

Yiyuan Chen

Matthew D Mcreynolds

Jr G Davis Harris

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

The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.

MIF inhibitors and their uses

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 sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Sulfamato hydroxamic acid metalloprotease inhibitor

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

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. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

This invention is directed to aromatic sulfone hydroxamates (also known as &ldquo;aromatic sulfone hydroxamic acids&rdquo;) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as &ldquo;matrix metalloprotease&rdquo; or &ldquo;MMP&rdquo;) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Aromatic sulfone hydroxamates and their use as protease inhibitors

This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

Aromatic sulfone hydroxamic acids and their use as protease inhibitors

A sulfamato hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease (mmp) activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Growing community of inventors

St. Louis, MO, United States of America

Jeffery N Carroll