EP 0648206 A1 19950419 - PEPTIDYL DERIVATIVES AND THEIR USE AS METALLOPROTEINASE INHIBITORS.
Title (en)
PEPTIDYL DERIVATIVES AND THEIR USE AS METALLOPROTEINASE INHIBITORS.
Title (de)
PEPTIDYLDERIVATE ALS INHIBITOREN VON METALLPROTEINASE.
Title (fr)
DERIVES PEPTIDIQUES ET LEUR UTILISATION COMME INHIBITEURS DE METALLOPROTEASES.
Publication
Application
Priority
- GB 9400896 W 19940427
- GB 9308695 A 19930427
Abstract (en)
[origin: WO9425435A1] Compounds of formula (1), wherein R represents a -CONHOR<6> [where R<6> is a hydrogen atom or an acyl group], carboxyl (-CO2H), esterified carboxyl, -SR<6> or -P(O)(X<1>R<7>)-X<2>R<8> group, where X<1> and X<2>, which may be the same or different, is each an oxygen or sulphur atom and R<7> and R<8>, which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl, or aralkyl group; R<1> represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R<2> represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, amino (-NH2), substituted amino, carboxyl (-CO2H), or esterified carboxyl group; R<3> represents a hydrogen atom or an alkyl group; R<4> represents a hydrogen atom or an alkyl group; R<5> represents a group -C(R<9>)(R<10>)Het-R<11>, wherein R<9> and R<10> which may be the same or different is each an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R<12>)- groups (where R<12> is a hydrogen atom or an optionally substituted alkyl group), or an optionally substituted cycloalkyl, cycloalkenyl, aryl or heteroaryl group, or R<9> and R<10> together with the carbon atom to which they are attached are linked together to form an optionally substituted cycloalkyl or cycloalkenyl group, Het is -O-, -S(O)p- [where p is zero, or an integer 1 or 2] or -N(R<12>)-, and R<11> is a hydrogen atom or an aliphatic, cycloaliphatic, heterocycloaliphatic, aromatic, or heteroaromatic group; X is an amino (-NH2), substituted amino, hydroxyl or substituted hydroxyl group, or is linked to the atom or group Het in R<5> to form a chain -X-Alk-R<5>- where X is -N(R<12>)-, Alk is an optionally substituted alkylene chain and R<5> is -Het-C(R<9>)(R<10>)-; and the salts, solvates, hydrates and prodrugs thereof. The compounds are orally active metalloproteinase inhibitors, with a good duration of action and may be of use in the prophylaxis or treatment of diseases or disorders in which stromelysin, collagenase and gelatinase have a role, for example in the treatment of cancer to control the development of tumor metastases.
IPC 1-7
IPC 8 full level
C07D 233/61 (2006.01); A61K 31/16 (2006.01); A61K 31/165 (2006.01); A61K 31/19 (2006.01); A61K 31/215 (2006.01); A61K 31/22 (2006.01); A61K 31/33 (2006.01); A61K 31/40 (2006.01); A61K 31/415 (2006.01); A61K 31/505 (2006.01); A61K 31/66 (2006.01); A61K 38/00 (2006.01); A61P 1/02 (2006.01); A61P 1/04 (2006.01); A61P 3/00 (2006.01); A61P 27/02 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C07C 237/22 (2006.01); C07C 259/06 (2006.01); C07C 315/04 (2006.01); C07C 317/48 (2006.01); C07C 319/20 (2006.01); C07C 323/57 (2006.01); C07C 323/60 (2006.01); C07D 207/325 (2006.01); C07D 231/12 (2006.01); C07D 239/28 (2006.01); C07F 9/38 (2006.01); C07F 9/40 (2006.01)
CPC (source: EP)
A61P 1/02 (2017.12); A61P 1/04 (2017.12); A61P 3/00 (2017.12); A61P 27/02 (2017.12); A61P 29/00 (2017.12); A61P 35/00 (2017.12); A61P 43/00 (2017.12); C07C 323/60 (2013.01)
Citation (search report)
See references of WO 9425435A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9425435 A1 19941110; AU 6575494 A 19941121; CA 2139129 A1 19941110; EP 0648206 A1 19950419; GB 9308695 D0 19930609; JP H08500610 A 19960123
DOCDB simple family (application)
GB 9400896 W 19940427; AU 6575494 A 19940427; CA 2139129 A 19940427; EP 94913710 A 19940427; GB 9308695 A 19930427; JP 52402794 A 19940427