Pharmacia Corporation

G.d. Searle & Company

Monsanto Technology LLC

Warner-lambert Company

Euclises Pharmaceuticals, Inc.

Pfizer Corporation

Terri L Boehm

Gary A DeCrescenzo

Jeffery N Carroll

Deborah A Mischke

Joseph J McDonald

Joseph Gerace Rico

John Nicholas Freskos

Daniel Paul Becker

Thomas E Barta

Clara I Villamil

Darren J Kassab

Susan Landis Hockerman

Louis J Bedell

Daniel P Getman

Yvette M Fobian

John Jeffrey Talley

Shashidhar N Rao

Nathan W Stehle

Steve A Kolodziej

William F Vernier

Susan C Howard

Robert M Heintz

Michael B Tollefson

Lijuan Jane Wang

Monica B Norton

Daniel Patrick Walker

Brent V Mischke

G Davis Harris, Jr

Justin Robert Struble

Kevin D Jerome

Matthew D McReynolds

Madeleine H Li

Mangesh Bore

Balekudru Devadas

Shuang Liu

Richard C Durley

Brian S Hickory

Ian L Scott

Michele A Promo

Shaun Raj Selness

Rajesh Devraj

Li Huang Xing

Eduardo J Martinez

Paul Vincent Rucker

Thomas Dale Owen

Hui Li

Win Naing

John Walker

Aruna Sambandam

Stephen A Kolodziej

Edgardo Alvira

Huey S Shieh

Patrick B Mullins

Carol Pearcy Howard

Heather M Madsen

Radhika M Blevis-Bal

Laura D Marruto

Jeff Hitchcock

Kevin F McGee

Jeffrey N Carroll

Gunnar J Hanson

Ish K Khanna

David Louis Brown

Margaret Lanahan Grapperhaus

Mark A Massa

John C Hodges

Alan Frank Gasiecki

Gary A De Crescenzo

Theresa R Fletcher

Michelle A Schmidt

Elizabeth C Arner

Howard D H Showalter

Yiyuan Chen

Mark A Nagy

Thomas A Wynn

Gary A DeCrezcenzo

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 present disclosure provides NO-releasing guanidine-coxib anti-cancer agents, having the structure of Formula (I): wherein R, R, Z and L are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, acne, or a disease mediated by arginine deficiency using a compound of Formula (I).

No-releasing guanidine-coxib anti-cancer agents

The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide-linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R, X, L, R, R, R, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).

No-releasing nonoate(nitrogen-bound)sulfonamide-linked-coxib anti-cancer agents

Diaryl substituted pyridinones

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

Disclosed are compounds Formula Iand pharmaceutically acceptable salts thereof, wherein R, R, R, R, and Rare defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

Substituted pyridinones

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

This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as 'matrix metalloprotease' or 'MMP') 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 hydroxamic acids and their use as protease inhibitors

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. A contemplated compound corresponds in structure to formula B, below,

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.

An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Aromatic sulfonyl alpha-hydroxy hydroxamic acid compounds

Growing community of inventors

Ballwin, MO, United States of America

Terri L Boehm