G.d. Searle & Company

Pharmacia Corporation

Biosynthema Inc.

Michelle A Schmidt

Ananthachari Srinivasan

John Jeffrey Talley

John Nicholas Freskos

Daniel L Flynn

Ish K Khanna

Daniel Paul Becker

Deborah A Mischke

Robert M Heintz

David Louis Brown

Joseph J McDonald

Yvette M Fobian

Thomas E Barta

Clara I Villamil

Lijuan Jane Wang

Margaret Lanahan Grapperhaus

Mark A Massa

Monica B Norton

William F Vernier

Joseph Gerace Rico

Susan Landis Hockerman

Alan Frank Gasiecki

Terri L Boehm

Louis J Bedell

Jeffery N Carroll

Brent V Mischke

Darren J Kassab

Nathan W Stehle

Stephen A Kolodziej

Larry P Feigen

Jeffery Alan Zablocki

Patrick B Mullins

Jack L Erion

Philip Needleman

Yiyuan Chen

Mark A Nagy

Thomas A Wynn

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

Peptide analogs of neurotensin are disclosed which are resistant to enzymatic degradation and which retain high binding affinity for neurotensin receptors. Pharmaceutical compositions of these compounds are useful for diagnostic and therapeutic purposes.

Labeled neurotensin derivatives

A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.

Radiopharmaceutical compositions capable of localizing at sites of

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Belleville, IL, United States of America

Michelle A Schmidt