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1. (WO1997018207) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018207 International Application No.: PCT/US1996/018382
Publication Date: 22.05.1997 International Filing Date: 13.11.1996
Chapter 2 Demand Filed: 20.05.1997
IPC:
A61K 38/00 (2006.01) ,C07D 245/02 (2006.01) ,C07D 255/02 (2006.01) ,C07D 267/00 (2006.01) ,C07D 273/02 (2006.01) ,C07D 291/02 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/12 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01) ,C07D 419/12 (2006.01) ,C07D 498/08 (2006.01) ,C07D 521/00 (2006.01) ,C07K 5/06 (2006.01) ,C07K 5/065 (2006.01) ,C07K 5/078 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
245
Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
255
Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/-C07D253/178
02
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
267
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
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
291
Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
02
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
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
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
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
419
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur 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
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
08
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
521
Heterocyclic compounds containing unspecified hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
065
the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
078
the first amino acid being heterocyclic, e.g. Pro, His, Trp
Applicants:
THE DU PONT MERCK PHARMACEUTICAL COMPANY [US/US]; 1007 Market Street Wilmington, DE 19898, US
Inventors:
XUE, Chu-Biao; US
CHERNEY, Robert, Joseph; US
DeCICCO, Carl, Peter; US
DeGRADO, William, Frank; US
HE, Xiaohua; US
HODGE, Carl, Nicolas; US
JACOBSON, Irina, Cipora; US
MAGOLDA, Ronald, Louis; US
ARNER, Elizabeth, Catherine; US
DUAN, Jingwu; US
NELSON, David, J.; US
Agent:
KONDRAD, Karen, H.; The du Pont Merck Pharmaceutical Company Legal/Patent Records Center 1007 Market Street Wilmington, DE 19898, US
Priority Data:
08/743,43901.11.1996US
60/006,68414.11.1995US
60/646,90208.05.1996US
Title (EN) NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS
(FR) NOUVEAUX COMPOSES MACROCYCLIQUES TENANT LIEU D'INHIBITEURS DE LA METALLOPROTEASE
Abstract:
(EN) This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.
(FR) L'invention concerne des molécules macrocycliques qui inhibent les métalloprotéinases, y compris l'agrécanase, et la production du facteur de nécrose tumorale (TNF). En particulier, les composés en question inhibent les métalloprotéinases intervenant dans la dégradation des tissus, d'une part, et la libération du TNF, d'autre part. On décrit par ailleurs des compositions pharmaceutiques renfermant ces composés et un certain nombre de procédés relatifs à l'utilisation de ces composés pour le traitement des maladies inflammatoires.
Designated States: AM, AU, AZ, BR, BY, CA, CN, CZ, EE, HU, IL, JP, KG, KR, KZ, LT, LV, MD, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, UA, VN
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, 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:
CZPV1998-1447NO19982185NZ324933SK63498MXPA/a/1998/003851VN2320
EP0863885JP2000502050 CN1202161CA2237524EA199800372KR1019990067592
AU1997012726