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1. (WO1998051665) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS

Pub. No.:    WO/1998/051665    International Application No.:    PCT/US1998/009789
Publication Date: Fri Nov 20 00:59:59 CET 1998 International Filing Date: Fri May 15 01:59:59 CEST 1998
IPC: C07D 273/02
C07D 413/12
C07D 413/14
C07D 417/12
C07D 521/00
C12Q 1/37
Applicants: DUPONT PHARMACEUTICALS COMPANY
Inventors: XUE, Chu-Bio
DECICCO, Carl, P.
CHERNEY, Robert, J.
ARNER, Elizabeth
DEGRADO, William, F.
DUAN, Jingwu
HE, Xiaohua
JACOBSON, Irina, Cipora
MAGOLDA, Ronald, L.
NELSON, David
Title: NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
Abstract:
This invention relates to macrocyclic molecules of formula (I) which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases. A novel enzymatic assay was developed to detect potential inhibitors of aggrecanase. The assay uses active aggrecanase accumulated in media from stimulated bovine nasal cartilage (BNC) or related cartilage sources and purified cartilage aggrecan monomer or a fragment thereof as a substrate.