New quinoxaline-di:one derivs.

摘要

Quinoxalinedione derivs. of formula (I) and their isomers and salts, are new. R<1> = (CH2)nCR<2>H(CH2)m-Z; R<5>-R<8> = H, T, CF3, NO2, halo, NR<9>R<10>, CN, SOPR<11>, SO2NR<12>R<13>, SO3H, SO3T or OR<14>; T = 1-6C alkyl; R<2> = H or (CH2)qR<3>; R<3> = H, OH, OT or NR<15>R<16>; r,m,q = 0, 1, 2 or 3; Z = POXY, OPOXY, OR<17>, NR<18>R<19>, NHCOR<20>, NHSO2R<21>, SO2R<22>, CO2R<23>, halo, CN or tetrazolyl; R<11> = H, T or phenyl; p = 0, 1 or 2; R<12>, R<13>, R<17>, R<23> = H or Q; Q = 1-4C alkyl; R<14> = H, or Q; Q = 1-4C alkyl; R<14> = H, or Q (opt. substd. by 1-3 halo); R<20>, R<21> = T, phenyl (opt. substd. by halo), or heteroaryl; R<22> = HO, TO or NR<24>R<25>; X,Y = OH, TO, Q or NR<18>R<19>; R<9>,R<10> = H, COT, phenyl, or T (opt. substd. by QO, NH2, NHQ or N(Q)2); or NR<9>R<10> = 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.); R<15>, R<16>,R<18>,R<19> = H, Q or phenyl; or NR<15>R<16> and/or NR<18>R<19> = a gp. as NR<9>R<10>; R<24>, R<25> = H or Q; or NR<24>R<25> = a satd. 5-7 membered heterocycle (which contains one other S, O or N atom and which is opt. substd.). Provided that (a) when R<2> is H and Z is CO2R<23> or POXY, then R<5>-R<8> are not H; (b) when R<2> is H, Z is POXY or CO2R<23> and R<5>, R<6>, R<7> or R<8> is CF3, NO2, NH2, halo or Me, the cpds. (I) are disubstituted.; (c) when R<1> is methanephosphonic acid and R<6> is CN or substd. imidazolyl, then R<5>, R<7> and R<8> cannot all be H; (d) when R<1> is methanephosphonic acid, R<6> is CF3 or NO2 and R<7> is imidazolyl, then R<5> and R<8> cannot both be H; and (e) when R<1> is CH2COOH and R<5> and R<8> are H, then R<6> and R<7> cannot both be halo or Me.