Hydroxylamine derivatives

Details Hydroxylamine derivatives Hydroxylamine derivatives

C - Chemistry, Metallurgy

07

D

167/209, 167/269

C07D 225/02 (2006.01) C07K 5/04 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/068 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1314655

Abstract Compounds of the formula Image , wherein A represents a group of the formula HN(OH)-CO- or HCO-N(OH)-: R1 represents a C2-C5-alkyl group; R represents the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R2 does not represent a hydrogen atom or a methyl group; R3 represents a hydrogen atom, an amino, hydroxy, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylamino, C1-C6-alkylthio or aryl-(C1- -C6-alkyl) group or an amino-(C1-C6-alkyl), hydroxy- -(C1-C6-alkyl), mereapto-(Cl-C6-alkyl) or carboxy- -(C1-C6-alkyl) group in which the amino, hydroxy, mercapto or carboxyl group may be proteeted, the amino group may be acylated or ths carboxyl group may be amidated, R4 represents a hydrogen atom or a methyl group; R5 represents a hydrogen atom or a C1-C6- -alkyl, C1-C6-alkoxy-C1-C6-alkyl, di(C1-C6- -alkoxy)-methylene, carboxyl, (C1-C6-alkyl)-carbonyl, (C1-C6-alkoxy)carbonyl, arylmethoxycarbonyl, (C1-C6-alkyl)aminocarbonyl or arylaminocarbonyl group: and R4 represants a hydrogen atom or a methyl group: or R4 and R6 together represent a group of the formula -(CH2)n- in which n stands for a number of 4 to 11; or R4 and R6 together represent a trimethylene group: and pharmaceutically acceptable salts of those compounds which are acidic or basic possess collagenase inhibitory activity and can be used in the control or prevention of degenerative joint diseases.

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