| 摘要 |
Hydroximic acids can be used to treat autoimmune diseases, especially insulin dependent diabetes, as they are inhibitors of poly(adenosine diphosphate ribose)polymerase. The use of hydroximic acids of formula (I) and their salts to treat autoimmune disease is new. R1 = H or 1-5C alkyl; R2 = H, 1-5C alkyl, 3-8C cycloalkyl or phenyl optionally substituted by OH or phenyl; or R1 + R2 together with the N atom to which they are attached = 5- to 8-membered ring optionally substituted by one or more further N, O or S atom(s), and the ring can be condensed with another alicyclic or heterocyclic ring, preferably a benzene, naphthalene, quinoline, isoquinoline, pyridine or pyrazoline ring, and furthermore, if desired and chemically possible, the N and/or S heteroatom(s) are in the form of an oxide or dioxide; R3 = H, phenyl, naphthyl or pyridyl, all optionally substituted by one or more halogen or 1-4C alkoxy; Y = H, OH, 1-24C alkoxy optionally substituted by amino, 2-24C polyalkenyloxy containing 1-6 double bonds, 1-25C alkanoyl, 3-9C alkenoyl or R7-COO-; R7 = 2-30C polyalkenyl containing 1-6 double bonds; X = halo, amino, 1-4C alkoxy; or X + B' = O ;or X + Y together with the C atoms to which they are attached and the -NROCH2- group being between the C atoms = a ring of formula (a); Z' = O or N; R = H or forms with B' a chemical bond; A = 1-4C alkylene , chemical bond or -(CHR4)m(CHR5)n-; R4 = H, 1-5C alkyl, 3-8C cycloalkyl or phenyl optionally substituted by halo, 1-4C alkoxy or 1-5C alkyl; R5 = H, 1-4C alkyl or phenyl; and m, n = 0-2. Compounds (I) are described in e.g. HU177578 and US4308399. |
