New imino- or pyridyl-substituted lipoic acid derivatives, as nitrogen monoxide synthase inhibitors and antioxidant regenerating agents, useful e.g. for treating nervous system or cerebrovascular disorders or cancer

摘要

Imino- or pyridyl-substituted lipoic acid derivatives (Ia) or (Ib) are new. Imino- or pyridyl-substituted lipoic acid derivatives of formulae (Ia) or (Ib) and their salts are new. R1, R2 = H or D'; or R1+ R2 = direct bond; D' = 1-6C alkyl; A = (CH2)mN(R3)CO(CH2)n, (CH2)mCON(R3)(CH2)n, (CH2)mN(R3)(CH2)n, (CH2)mCON(R3)(CH2)p-N(R4)(CH2)n, (CH2)mN(R3)CON(R4)(CH2)n or (CH2)m; m, n = 0-6; p = 2-6; R3, R4 = H or D'; X = phenylene or phenylene-alkylene group of formula -C6H3(R5)-T-; or (CH2)q; T = (CH2)i, T being attached to Y'; R5 = H, D', -(CH2)mQ or 5- or 6-membered heterocycle (containing O, N(R6) or S); i, q = 0-6; Q = halo, OH, CN, NH2, alkoxy, alkylthio, alkylamino or dialkylamino; R6 = H, D' or the bond to the phenyl ring; Y' = -N=C(B)-NH2 or R7-substituted 2-aminopyridinyl; B' = D', NR8R9, SR10 or 5- or 6-membered aryl or 5-or 6-membered heteroaryl (containing 1-4 O, S and N, especially thiophene, furan, pyrrole or thiazole), both optionally substituted by D', 2-6C alkenyl or OD'; R8R9 = H or D'; or NR8R9 = 5- or 6-membered non-aromatic heterocycle in which the ring members are CH2, NH, O or S; R7, R10 = H or D'. Independent claims are included for the preparation of (Ia) or (Ib).