Peptidyl derivatives and their use as metalloproteinases...

Details Peptidyl derivatives and their use as metalloproteinases... Peptidyl derivatives and their use as metalloproteinases...

C - Chemistry, Metallurgy

07

C

C07C 237/22 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/44 (2006.01) A61K 31/675 (2006.01) C07C 235/74 (2006.01) C07C 259/06 (2006.01) C07C 323/62 (2006.01) C07D 213/56 (2006.01) C07F 9/40 (2006.01)

Patent

CA 2114622

2114622 9324449 PCTABS00028 Compounds of formula (1) are described wherein R represents a -CONHOH, carboxyl (-CO2H), esterified carboxyl or -P(O)(X1R8)X2R9 group, where X1 and X2, which may be the same or different is each an oxygen or a sulphur atom, and R8 and R9, which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl or aralkyl group; R1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R2 represents an optionally substituted aryloxy, arylthio, aryloxyalkyl, arylthioalkyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl or heteroarylthioalkyl group; R3 represents a hydrogen atom or an alkyl group; R4 represents a hydrogen atom or an alkyl group; R5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7) groups, [where R7 is a hydrogen atom or a C1-6 alkyl group] or a group -[Alk]nR6 where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7) groups, n is zero or an integer 1 and R6 is an optionally substituted cycloalkyl or cycloalkenyl group; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular are selective inhibitors of the action of gelatinase, and may be of use in the treatment of cancer to control the development of tumour metastases.

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