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1. (WO1992009563) IMPROVED MATRIX METALLOPROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/009563 International Application No.: PCT/US1991/008722
Publication Date: 11.06.1992 International Filing Date: 21.11.1991
Chapter 2 Demand Filed: 04.06.1992
IPC:
A61K 31/165 (2006.01) ,A61K 31/405 (2006.01) ,A61K 31/454 (2006.01) ,A61K 38/00 (2006.01) ,C07C 259/06 (2006.01) ,C07D 209/20 (2006.01) ,C07K 5/078 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
165
having aromatic rings, e.g. colchicine, atenolol, progabide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
404
Indoles, e.g. pindolol
405
Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
259
Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04
without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06
having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20
substituted additionally by nitrogen atoms, e.g. tryptophane
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:
GLYCOMED, INC. [US/US]; 860 Atlantic Avenue Alameda, CA 94501, US
GALARDY, Richard, E. [US/US]; US
GROBELNY, Damian [AU/AU]; AU
Inventors:
GALARDY, Richard, E.; US
GROBELNY, Damian; AU
MUSSER, John, H.; AU
Agent:
MURASHIGE, Kate, H. ; Morrison & Foerster 545 Middlefield Road Suite 200 Menlo Park, CA 94025, US
Priority Data:
615,79821.11.1990US
747,75120.08.1991US
Title (EN) IMPROVED MATRIX METALLOPROTEASE INHIBITORS
(FR) INHIBITEURS AMELIORES DE METALLOPROTEASE MATRICIELLE
Abstract:
(EN) Compounds of formulas (1) or (2), wherein each R1 is independently H or alkyl (1-8C) and R2 is alkyl (1-8C) or wherein the proximal R1 and R2 taken together are -(CH2)p- wherein p = 3-5; R3 is H or alkyl (1-4C); R4 is fused or conjugated unsubstituted or substituted bicycloaryl methylene; n is 0, 1 or 2; m is 0 or 1; and X is OR5 or NHR5, wherein R5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); or X is an amino acid residue or amide thereof; or X is the residue of a cyclic amine or heterocyclic amine; Y is selected from the group consisting of R7ONR6CONR6-, R62NCONOR7-, and R6CONOR7-, wherein each R6 is independently H or lower alkyl (1-4C); R7 is lower alkyl (1-4C) or an acyl group; and wherein -CONR3- is optionally in modified isosteric form are inhibitors of matrix metalloproteases.
(FR) Composés définis par les formules (1) ou (2) constituant des inhibiteurs de métalloprotéases matricielles. Dans les formules, chaque R1 représente indépendamment H ou alkyle (C1-8) et R2 représente alkyle (C1-8), ou R1 et R2 pris ensemble représentent -(CH2)p, où p est compris entre 3 et 5; R3 représente H ou alkyle (C1-4); R4 représente du méthylène de bicycloaryle fusionné ou conjugué, substitué ou non substitué; n vaut 0, 1 ou 2; m vaut 0 ou 1; X représente OR5 ou NHR5, où R5 représente H ou alkyle (C1-12) substitué ou non substitué, aryle (C6-12), arylalkyle (C6-16); ou X est un reste d'acide aminé ou un amide de ce dernier; ou bien X est le reste d'une amine cyclique ou d'une amine hétérocyclique; Y est sélectionné dans le groupe composé de R7ONR6CONR6-, R62NCONOR7-, et R6CONOR7-, où chaque R6 représente indépendamment H ou alkyle inférieur (C1-4); R7 représente alkyle inférieur (C1-4) ou un groupe acyle; -CONR3- se présente éventuellement sous une forme isostérique modifiée.
Designated States: AT, AU, BB, BG, BR, CA, CH, CS, DE, DK, ES, FI, GB, HU, JP, KP, KR, LK, LU, MC, MG, MN, MW, NL, NO, PL, RO, SD, SE, SU
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
NO19931844EP0558635JPH06511468CA2096225AU1991090897