C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07F 9/40 (2006.01) C07F 9/547 (2006.01) C07F 9/6533 (2006.01)
Patent
CA 2105309
2105309 9314096 PCTABS00024 Compounds of formula (I) are described wherein R represents a -P(O)(X1R6)X2R7 group, where X1 and X2, which may be the same of different, is each an oxygen or a sulphur atom, and R6 and R7, 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 a group -[Alk]nR8 where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R9)- groups [where R9 is a hydrogen atom or a C1-6alkyl group], n is zero or an integer 1, and R8 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 have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastasises.
Beeley Nigel Robert Arnold
Millican Thomas Andrew
Morphy John Richard
Celltech Therapeutics Limited
Kirby Eades Gale Baker
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