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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)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
273
Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/-C07D271/183
02
having two nitrogen atoms and only one oxygen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
521
Heterocyclic compounds containing unspecified hetero rings
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES OR MICRO-ORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1
Measuring or testing processes involving enzymes or micro-organisms; Compositions therefor; Processes of preparing such compositions
34
involving hydrolase
37
involving peptidase or proteinase
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:
08/856,22314.05.1997US
Title (EN) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
(FR) NOUVEAUX COMPOSES MACROCYCLIQUES COMME INHIBITEURS DE METALLOPROTEASE
Abstract:
(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)
Also published as:
EP0981521JP2001524949 CA2287923AU1998073853