G.d. Searle & Company

Pharmacia Corporation

Loyola University of Chicago

Microdose Therapeutx, Inc.

University of Texas System

G.d. Searle LLC

Other

Monsanto Company

Marquette University

Daniel Paul Becker

Clara I Villamil

Daniel L Flynn

Joseph J McDonald

Thomas E Barta

Roger A Nosal

Gary A DeCrescenzo

John Nicholas Freskos

Alan E Moormann

Daniel P Getman

Louis J Bedell

Terri L Boehm

Susan Landis Hockerman

Brent V Mischke

Deborah A Mischke

Joseph Gerace Rico

Hui Li

Yvette M Fobian

Jeffery N Carroll

Nathan W Stehle

Steve A Kolodziej

Robert M Heintz

William F Vernier

Shashidhar N Rao

Henri M Akouka

Darren J Kassab

Alan E Moorman

Madeleine H Li

John Jeffrey Talley

Michael B Tollefson

Lijuan Jane Wang

Monica B Norton

Norman A Abood

Lori A Schretzman

Marlon Ray Lutz, Jr

Patrick B Mullins

Tahirah K Heath

Brian M Bax

Cory Reidl

Dale P Spangler

Robert L Shone

Michael S Dappen

Susan C Howard

Stephen A Kolodziej

Daniel L Zabrowski

Carol Pearcy Howard

Walter Fast

Jeffrey N Carroll

Gunnar J Hanson

Paul Waddell Collins

Ish K Khanna

David Louis Brown

Julie M Miyashiro

Margaret Lanahan Grapperhaus

James W Malecha

Mark A Massa

Alan Frank Gasiecki

Joe T Collins

Michelle A Schmidt

Jennifer Ann Van Camp

Gary A De Crescenzo

Theresa R Fletcher

Craig Oakum

Andria M Panagopoulos

Yiyuan Chen

Maxwell Moore

Mark A Nagy

Thomas A Wynn

Rao N Shashidhar

Richard C Holz

Anna Starus

Gary A DeCrezcenzo

Renee Hyer

Elizabeth C Arner

Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase (“MMP”) inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: Formula (I) wherein the substituents are as described.

Carborane hydroxamic acid matrix metalloproteinase inhibitors and agents for boron neutron capture therapy

Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase ('MMP') inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: Formula (I) wherein the substituents are as described. 

Indoline sulfonamide compounds that can inhibit DapE and/or bacterial metallo-&#x3b2;-lactamases (MBLs), such as NDM-1, are disclosed. Also disclosed are methods of treating an individual suffering from a bacterial infection using the indoline sulfonamide compounds disclosed herein.

Indoline sulfonamide inhibitors of DapE and NDM-1 and use of the same

Indoline and tetrahydroquinoline sulfonyl compounds that can inhibit DapE and/or bacterial metallo-&#x3b2;-lactamases ('MBLs'), such as NDM-1 are disclosed. Also disclosed are methods of treating an individual suffering from a bacterial infection using the compounds disclosed herein.

Indoline and tetrahydroquinoline sulfonyl inhibitors of dimetalloenzymes and use of the same

The present disclosure provides a method and device for delivering a pharmaceutical to the airway of a human or animal patient. In one aspect, the device includes a dose drum formed into a cylinder and including a plurality of dose compartments for containing individual doses. In another aspect, the device may include a reservoir containing a pharmaceutical material in bulk form and a metering recess for metering the pharmaceutical material to form a pharmaceutical dose. Another aspect provides an inhaler with a combined reservoir and dosing chamber configured to contain multiple doses of a pharmaceutical material.

Inhalation device and method

A medicament delivery device comprises a dosing chamber configured to contain dry powder medicament, a transducer and a controller electrically coupled to the transducer. The medicament delivery device is capable of delivering a therapeutically effective dose of dry powder medicament in response to between 2-20 tidal inhalations, the dose preferably having a mass median aerodynamic diameter (MMAD) of about 6 microns or less and a fine particle fraction of at least 30%.

Inhaler and methods of use thereof

A method and device for delivering a pharmaceutical to the airway of a human or animal patient, in one aspect, includes a dose drum formed into a cylinder and including a plurality of dose compartments for containing individual doses. In another aspect, the device may include a reservoir containing a pharmaceutical material in bulk form and a metering recess for metering the pharmaceutical material to form a pharmaceutical dose. Another aspect provides an inhaler with a combined reservoir and dosing chamber configured to contain multiple doses of a pharmaceutical material.

Tribenzo-1,4,7-triazacyclononane and derivatives thereof having a formula (I) are disclosed. Methods of making tribenzo-1,4,7-triazacyclononane and related compounds also are disclosed. 

Supramolecular scaffolds and methods of making the same

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 sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula  wherein W and the R groups are defined elsewhere.

Sulfonyl aryl or heteroaryl hydroxamic acid compounds

A class of compounds which are (H/K)ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula III:

Method of using (H+/K+) ATPase inhibitors as antiviral agents

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

Growing community of inventors

Glenview, IL, United States of America

Daniel Paul Becker