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Machine translation
1. (WO1998051665) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1998/051665    International Application No.:    PCT/US1998/009789
Publication Date: 19.11.1998 International Filing Date: 14.05.1998
Chapter 2 Demand Filed:    27.11.1998    
IPC:
C07D 273/02 (2006.01), C07D 413/12 (2006.01), C07D 413/14 (2006.01), C07D 417/12 (2006.01), C07D 521/00 (2006.01), C12Q 1/37 (2006.01)
Applicants: DUPONT PHARMACEUTICALS COMPANY [US/US]; 1007 Market Street, Wilmington, DE 19807 (US)
Inventors: XUE, Chu-Bio; (US).
DECICCO, Carl, P.; (US).
CHERNEY, Robert, J.; (US).
ARNER, Elizabeth; (US).
DEGRADO, William, F.; (US).
DUAN, Jingwu; (US).
HE, Xiaohua; (US).
JACOBSON, Irina, Cipora; (US).
MAGOLDA, Ronald, L.; (US).
NELSON, David; (US)
Agent: KONRAD, Karen, K.; DuPont Pharmaceuticals Company, Legal Patent Records Center, 1007 Market Street, Wilmington, DE 19898 (US)
Priority Data:
08/856,223 14.05.1997 US
Title (EN) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
(FR) NOUVEAUX COMPOSES MACROCYCLIQUES COMME INHIBITEURS DE METALLOPROTEASE
Abstract: front page image
(EN)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.
(FR)La présente invention concerne des molécules macrocycliques inhibant des métalloprotéases, y compris une aggrécanase, et la production d'un facteur de nécrose des tumeurs (TNF). En particulier, les composés sont des inhibiteurs de métalloprotéases intervenant dans la dégradation de tissus et des inhibiteurs de libération de facteur de nécrose des tumeurs. La présente invention concerne également des compositions pharmaceutiques comprenant de tels composés, ainsi que des méthodes d'utilisation de ces composés dans le traitement d'affections inflammatoires.
Designated States: AU, BR, CA, CN, CZ, EE, HU, IL, JP, KR, LT, LV, MX, NO, NZ, PL, RO, SG, SI, SK, UA, VN.
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE).
Publication Language: English (EN)
Filing Language: English (EN)