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1. AU1995025722 - Succinyl hydroxamic acid, n-formyl-n-hydroxy amino carboxylic acid and succinic acid amide derivatives as metalloprotease inhibitors

Office Australia
Application Number 25722/95
Application Date 26.05.1995
Publication Number 1995025722
Publication Date 01.02.1996
Publication Kind A
IPC
C07D 521/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
521Heterocyclic compounds containing unspecified hetero rings
A61K 31/195
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
20having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61P 1/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
C07C 237/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
CPC
A61P 1/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 237/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 259/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds 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
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
Applicants British Biotech Pharmaceuticals Limited
Inventors Beckett, Paul Raymond
Martin, Fionna Mitchell
Miller, Andrew
Whittaker, Mark
Priority Data 9410802 28.05.1994 GB
9503754 24.02.1995 GB
Title
(EN) Succinyl hydroxamic acid, n-formyl-n-hydroxy amino carboxylic acid and succinic acid amide derivatives as metalloprotease inhibitors
Abstract
(EN)
Compounds of general formula (I) wherein X is a -CO2H, -N(OH)CHO or -CONHOH group; R1 is hydrogen; (C1-C6)alkyl; (C2-C6)alkenyl; phenyl; substituted phenyl; phenyl(C1-C6)alkyl; substituted phenyl(C1-C6)alkyl; heterocyclyl; substituted heterocyclyl; heterocyclyl(C1-C6)alkyl; substituted heterocyclyl(C1-C6)alkyl; a group BSOnA- wherein n is 0, 1 or 2 and B is hydrogen or a (C1-C6)alkyl, phenyl, substituted phenyl, heterocyclyl, (C1-C6)acyl, phenacyl or substituted phenacyl group, and A represents (C1-C6)alkyl; amino; protected amino; acylamino; OH; SH; (C1-C6)alkoxy; (C1-C6)alkylamino; di-(C1-C6)alkylamino; (C1-C6)alkylthio; aryl (C1-C6)alkyl; amino(C1-C6)alkyl; hydroxy(C1-C6)alkyl, mercapto(C1-C6)alkyl or carboxy(C1-C6)alkyl wherein the amino-, hydroxy-, mercapto- or carboxyl-groups are optionally protected or the carboxyl-group amidated; lower alkyl substituted by carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, or carboxy-lower alkanoylamino; R2 represents a linear saturated or unsaturated C13-C24 hydrocarbon chain, which chain (i) may be interrupted by one or more non-adjacent -O- or -S- atoms or -C(=O)-, -S($m(7)O)-, -S(=O)2- or -N(Rx)- groups wherein Rx is hydrogen, methyl or ethyl, provided that the maximum length of the chain is no more than 28 C, O, S and N atoms, and/or (ii) may be substituted with one ore more groups selected from C1-C6 alkyl, OH, OMe, halogen, NH2, NHCH3, N(CH3)2, CO2H, CO2CH3, COCH3, CHO, CONH2, CONHCH3, CON(CH3)2, CH2OH, NHCOCH3, provided that the maximum length of the chain is no more than 28 C, O, S and N atoms; R3 is the characterising side chain of a natural or non-natural $g(a) amino acid in which any functional groups may be protected, with the proviso that R3 does not represent hydrogen; R4 is hydrogen, C1-C6 alkyl, (C1-C4)perfluoroalkyl or a group D-(C1-C6 alkyl) wherein D represents hydroxy, (C1-C6)alkoxy, (C1-C6)alkylthio, acylamino, optionally substituted phenyl or heteroaryl, NH2, or mono- or di-(C1-C6 alkyl)amino; R5 is hydrogen or a (C1-C6)alkyl group; or a salt, hydrate or solvate thereof. The compounds are inhibitors of matrix metalloproteinases, especially gelatinases.