C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 295/26 (2006.01) A61K 31/18 (2006.01) A61K 31/535 (2006.01) A61K 31/66 (2006.01) C07C 307/06 (2006.01) C07F 9/40 (2006.01)
Patent
CA 2114623
2114623 9324475 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 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino (-NH2), substituted amino, carboxyl (-CO2H) or esterified carboxyl 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 of -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 a group -NR10R11 where R10 is a hydrogen atom or an optionally substituted alkyl, alkanoyl, aryl, aroyl, aralkyl or aralkanoyl group, and R11 is a straight or branched alkylaminosulphonylamino group wherein the alkyl portion is optionally interrupted by one or more -O- or -S- atoms or N(R7)- or aminocarbonyloxy groups; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective inhibitory action against gelatinase and may be of use in the treatment of cancer to control the development of tumour metastases.
Beeley Nigel Robert Arnold
Millican Thomas Andrew
Morphy John Richard
Porter John Robert
Celltech Therapeutics Limited
Kirby Eades Gale Baker
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