摘要 |
<p>The invention provides hydroxamic acid derivatives of general formula (I) wherein R<1> represents 1-7C alkyl; R<2> represents a saturated 5-, 6- or 7-membered monocyclic or bridged N-heterocyclic ring which is attached via the N atom and which, when it is monocyclic, optionally contains -NR<4>-, -O-, -S-, -SO- or -SO2- as a ring member and/or is optionally benz-fused or optionally substituted on one or more C atoms by hydroxy, 1-6C alkyl, 1-6C alkoxy, oxo, ketalized oxo, amino, protected amino, mono(1-6C alkyl)amino, di(1-6C alkyl)amino, (1-6C alkoxy)carbonyl, hydroxymethyl, (1-6C alkoxy-methyl, hydroxyimino, carbamoyl, mono(1-6C alkyl)carbamoyl, di(1-6C alkyl)carbamoyl, N-(1-6C alkyl)-N-(1-6C alkoxy)carbamoyl, aryl-(1-6C alkyl-carbamoyl, 3-6C cycloalkylcarbamoyl, 2,2,6,6-tetra(1-6C alkyl)-4-piperidinyl-carbonyl or 1,2,2,6,6-penta(1-6C alkyl)-4-piperidinylcarbonyl; R<3> represents 1-6C alkyl or a group of the formula -(CH2)m-aryl or -(CH2)m-Het in which m stands for 1-4 and Het represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the nitrogen atom, (b) optionally contains N, O and/or S as additional hetero atom(s), (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 carbon atoms by 1-6C alkyl or oxo and/or on any additional N atom(s) by 1-6C alkyl or aryl; R<4> represents hydrogen, 1-6C-alkyl, aryl or a protecting group; and pharmaceutically acceptable salts thereof, which are matrix metalloproteinase inhibitors useful in the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis or in the treatment of invasive tumours, atherosclerosis or multiple sclerosis.</p> |
申请人 |
F.HOFFMANN-LA ROCHE AG;BROADHURST, MICHAEL, JOHN;BROWN, PAUL, ANTHONY;JOHNSON, WILLIAM, HENRY |
发明人 |
BROADHURST, MICHAEL, JOHN;BROWN, PAUL, ANTHONY;JOHNSON, WILLIAM, HENRY |