NEW CHINOXALINDION DERIVATIVES, THEIR PRODUCTION AND USE IN MEDICINAL PRODUCTS

摘要

Quinoxalinedione derivs. of formula (I) and their isomers and salts, are new. R1 = (CH2)nCR2H(CH2)m-Z; R5-R8 = H, T, CF3, NO2, halo, NR9R10, CN, SOPR11, SO2NR12R13, SO3H, SO3T or OR14; T = 1-6C alkyl; R2 = H or (CH2)qR3; R3 = H, OH, OT or NR15R16; r,m,q = 0, 1, 2 or 3; Z = POXY, OPOXY, OR17, NR18R19, NHCOR20, NHSO2R21, SO2R22, CO2R23, halo, CN or tetrazolyl; R11 = H, T or phenyl; p = 0, 1 or 2; R12, R13, R17, R23 = H or Q; Q = 1-4C alkyl; R14 = H, or Q; Q = 1-4C alkyl; R14 = H, or Q (opt. substd. by 1-3 halo); R20, R21 = T, phenyl (opt. substd. by halo), or heteroaryl; R22 = HO, TO or NR24R25; X,Y = OH, TO, Q or NR18R19; R9,R10 = H, COT, phenyl, or T (opt. substd. by QO, NH2, NHQ or N(Q)2); or NR9R10 = a 5-7 membered satd. heterocycle (which contains one other N, O or S atom and which is opt. substd.), or an unsatd. 5-membered heterocycle (which contains 1-3N atoms and which is opt. substd.); R15, R16,R18,R19 = H, Q or phenyl; or NR15R16 and/or NR18R19 = a gp. as NR9R10; R24, R25 = H or Q; or NR24R25 = a satd. 5-7 membered heterocycle (which contains one other S, O or N atom and which is opt. substd.). Provided that (a) when R2 is H and Z is CO2R23 or POXY, then R5-R8 are not H; (b) when R2 is H, Z is POXY or CO2R23 and R5, R6, R7 or R8 is CF3, NO2, NH2, halo or Me, the cpds. (I) are disubstituted.; (c) when R1 is methanephosphonic acid and R6 is CN or substd. imidazolyl, then R5, R7 and R8 cannot all be H; (d) when R1 is methanephosphonic acid, R6 is CF3 or NO2 and R7 is imidazolyl, then R5 and R8 cannot both be H; and (e) when R1 is CH2COOH and R5 and R8 are H, then R6 and R7 cannot both be halo or Me.