Heterocyclic and benzene derivatives of lipoic acid, are nitrogen monoxide synthase inhibitors and anti-oxidant regeneration agents, useful for treating cardiovascular, cerebrovascular, nervous system, disorders and the like

摘要

Lipoic acid heterocyclic and benzene derivatives (Ia) and (Ib) are new. Lipoic acid heterocyclic and benzene derivatives of formula (Ia) and (Ib), and their salts are new. n = 0-6; R1, R2 = H or 1-6C alkyl; X-Y = -O-(CH2)r-, -N(R3)-(CH2)r-, -CO-(CH2)r-, -CO-N(R3) -(CH2)r-, -N(R4)-CO-(CH2)r-, or -N(R3)-CO-N(R4) -(CH2)r-; X', Y' = -(CH2)r-, -(CH2)r-O-(CH2)r-, -(CH2)r-N(R3) -(CH2)r-, -(CH2)r-CO-(CH2)r-, -(CH2)r-CO-N(R3)(CH2)r-, -(CH2)r-N(R4)-CO-(CH2)r-, or -(CH2)r-N(R3)-CO-N(R4)-(CH2)r-; R3, R4 = H, alkyl, alkoxycarbonyl, or aralkoxy carbonyl; r = 0-6; OMICRON = 5-6 membered aromatic heterocycle, 4-7 membered non-aromatic heterocycle, or phenylene substituted by R5; R5 = H, 1-6C alkyl, or -(CH2)m-Q; Q = halogen, OH, CN, NH2, alkoxy, alkylamino, or dialkylamino; m = 0-6; P = -(CH2)g- or -C6H3(R6)-; g = 0-6; R6 = H, 1-6C alkyl, -(CH2)n-Q', or 5-6 membered aromatic or non-aromatic heterocycle in which the heteroatoms are O, N(R7), or S; Q' = halogen, CF3, OH, NH2, CN, alkoxycarbonylamino, aralkoxycarbonylamino, alkoxy, alkylthio, alkylamino, or dialkylamino; n = 0-6; R7 = H, or 1-6C alkyl; A = -N=C(B)-NH2; B = 1-6C alkyl, carbocyclic aryl optionally substituted by alkyl, alkenyl or alkoxy, or heterocyclic aryl of 5 or 6 members with 1-4 heteroatoms (O, N, S); B = NR8R9 or SR10; R8, R9 = H, 1-6C alkyl, or one of them is NO2 and the other is H or 1-6C alkyl; or NR8R9 = 5-6 membered heterocycle; and R10 = H or 1-6C alkyl. Independent claims are also included for intermediates of formula (II), (III), and (IV).