Hydroxamic acid derivatives

Details Hydroxamic acid derivatives Hydroxamic acid derivatives

C - Chemistry, Metallurgy

07

C

C07C 239/08 (2006.01) A61K 31/16 (2006.01) A61K 31/40 (2006.01) A61K 31/505 (2006.01) A61K 38/05 (2006.01) C07C 237/22 (2006.01) C07C 259/06 (2006.01) C07D 207/408 (2006.01) C07D 209/48 (2006.01) C07D 211/88 (2006.01) C07D 233/72 (2006.01) C07D 233/74 (2006.01) C07D 239/54 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) C07K 5/065 (2006.01) C07K 5/068 (2006.01)

Patent

CA 2098166

RAN 4070/086 Abstract The invention provides hydroxamic acid derivatives of the formula Image (I) wherein R1 represents 1-7C alkyl; R2 represents hydrogen, 1-6C alkyl or a group of the formula -(CH2)n-aryl or -(CH2)n-Het in which n stands for 1-4 and Het represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S as additional hetero atom(s) in a position or positions other than adjacent to the linking N atom, (c) is substituted by oxo on one or both C atoms adjacent to the linking N atom and (d) is optionally benz-fused or option- ally substituted on one or more other carbon atoms by 1-6C alkyl or oxo and/or on any additional N atom(s) by 1-6C alkyl; R3 represents the characterizing group of a natural or non-natural .alpha.-amino acid in which any functional group present may be protected, with the proviso that R3 does not represent hydrogen; R4 represents carboxyl, (1-6C alkoxy)- carbonyl, carbamoyl or (1-6C alkyl)carbamoyl; R5 represents the characterizing group of a naturally occurring .alpha.-amino acid in which any functional group present may be protected; and R6 represents hydrogen; or R4, R5 and R6 each individually represent hydrogen or 1-6C alkyl, and their pharmaceutically acceptable salts, which are matrix metalloproteinase inhibitors useful for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteo- arthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods by deprotecting a corresponding novel benzyloxyamino compound or hydroxamidating a corresponding novel amino acid or activated derivative thereof.

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