C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 259/06 (2006.01) A61K 31/165 (2006.01) A61K 31/33 (2006.01) C07C 237/22 (2006.01) C07C 323/47 (2006.01) C07C 323/60 (2006.01) C07D 207/36 (2006.01) C07D 213/70 (2006.01) C07D 237/18 (2006.01) C07D 239/38 (2006.01) C07D 307/64 (2006.01) C07D 333/24 (2006.01) C07D 333/34 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2100661
2100661 9213831 PCTABS00014 Compounds of general formula (I): wherein R1 is hydrogen, C1-C6 alkyl, phenyl, substituted phenyl, phenyl(C1-C6 alkyl), or heterocyclyl; or R1 is ASOnR7 wherein A represents a C1-C6 hydrocarbon chain, optionally substituted with one or more C1-C6 alkyl, phenyl or substituted phenyl groups n = 0, 1, 2; R7 is C1-C6 alkyl, phenyl, substituted phenyl, phenyl(C1-C6 alkyl), heterocyclyl, (C1-C6 alkyl)acyl thienyl or phenacyl; R2 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, phenyl (C1-C6 alkyl) or cycloalkyl(C1-C6 alkyl); R3 and R4 are selected from hydrogen, halogen, cyano amino, amino(C1-C6)alkyl, amino di (C1-C6)alkyl, amino(C1-C6)alkylacyl, aminophenacyl, amino (substituted phenacyl, amino acid or derivative thereof, hydroxy, oxy(C1-C6)alkyl, oxyacyl, formyl, carboxylic acid, carboxamide, carboxy (C1-C6) alkylamide, carboxyphenylamide, carboxy(C1-C6) alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkyloxy(C1-C6) alkyl or acyloxy(C1-C6)alkyl, (C1-C6)alkylcarboxylic acid, (C1-C6) alkylcarboxy (C1-C6) alkyl, amino (C1-6)alkylacyl carboxylic acid or amino (C1-6)alkylacyl (C1-6) alkylcarboxylate; or R3 is OCH2COR8 R4 is hydrogen; wherein R8 is hydroxyl, C1-C6 oxyalkyl, C1-C6 oxyalkylphenyl, amino, C1-C6 aminoalkyl, C1-C6 aminodialkyl, C1-C6 aminoalkylphenyl, an amino acid or derivative thereof; or R3 is OCH2CH2OR9 and R4 is hydrogen; wherein R6 is C1-C6 alkyl, C1-C6 alkylphenyl, phenyl, substituted phenyl, (C1-C6 alkyl)acyl, or phenacyl; or R3 is OCH2CN and R4 is hydrogen; R5 is hydrogen or C1-C6 alkyl, or (C1-C6) alkylphenyl; R6 is hydrogen or methyl; or a salt thereof; specifically excluded are compounds wherein: R3 = R4 = hydrogen or R3 = R4 = hydroxy or R3 = hydrogen and R4 = oxybenzyl or R3 = hydrogen and R4 = oxy(C1-C6 alkyl); or a salt thereof; have collagenase inhibition activity and are useful in the management of disease involving collagen degradation. Its uses include rheumatoid arthritis, corneal ulceration, osteoporosis, periodontitis, gingivitis and tumour invasion.
Beckett Raymond Paul
Crimmin Michael John
Davidson Alan Hornsby
British Bio-Technology Limited
Gowling Lafleur Henderson Llp
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