Hydroxamic acid derivatives

Details Hydroxamic acid derivatives Hydroxamic acid derivatives

C - Chemistry, Metallurgy

07

D

C07D 417/06 (2006.01) A61K 31/445 (2006.01) A61K 31/50 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 207/27 (2006.01) C07D 207/404 (2006.01) C07D 209/48 (2006.01) C07D 211/88 (2006.01) C07D 233/74 (2006.01) C07D 249/12 (2006.01) C07D 271/07 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 413/06 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2098168

RAN 4070/084 Abstract The invention provides hydroxamic acid derivatives of the formula Image (I) wherein R1 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 optionally substituted on one or more other C atoms by lower alkyl or oxo and/or on any additional N atom(s) by lower alkyl or aryl; R2 represents lower alkyl and R3 represents lower alkyl or aryl, or NR2R3 represents a saturated 5-, 6- or 7-membered hsterocyclia ring which optionally contains -NRa, -O-,-S-, -SO- or -SO2- as a ring member and/or which is optionally substituted by hydroxy, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; Ra represents hydrogen, lower alkyl, lower alkanoyl, aryl-lower alkanoyl, lower alkoxycarbonyl, aryl-lower alkoxycarbonyl or mono(lower alkyl)carbamoyl; R4, R5, R6 and R7 each represent hydrogen or methyl, provided that at least two of these symbols represent hydrogen; and n stands for 1-4; and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured either by hydroxamidating a corresponding novel carboxylic acid or deprotecting a corresponding novel benzyloxycarbamoyl compound.

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