| 摘要 |
<p>N-(carbamimidophenyl)glycinamide derivatives (I) are new. N-(carbamimidophenyl)glycinamide derivatives of formula (I) and their hydrates, solvates and salts are new. E = H or OH; Q = H or alkyl; R = aryl, cycloalkyl or alkyl (substituted by R<1>, R<2> and R<3>); R<1> = H, COOH, COO-alkyl or aryl; R<2> = H, aryl, cycloalkyl or heteroaryl; R<3> = H, aryl, or OH, alkoxy or optionally protected NH2, provided these are not bound to R via the position which is alpha - to the N-atom; Or Q and R together form pyrrolidino, piperidino or 1,2,3,4-tetrahydroisoquinolin-3-yl which are substituted by COOH or COO-alkyl; Three of X<1>-X<4> = independently C(Ra), C(Rb) or C(Rc) and the fourth is C(Rd) or N; Ra-Rd = independently H, OH, NO2, dialkylamino, halo, alkyl, alkoxy, aryloxy, aralkyloxy, heteroaryl-alkoxy, heterocyclyl-alkoxy, COOH, COO-alkyl, NH-SO2-alkyl, NH-SO2-aryl, NHCO-alkyl, NHCO-aryl, NHCOO-alkyl, NHCO-alkyl-NH2, NHCO-alkyl-NHG, aralkyl-CONH, alkyl-O-alkyl-CONH, aryl-O-alkyl-CONH, alkyl-COOH, alkyl-COO-alkyl, O-alkyl-COOH or O-alkyl-COO-alkyl, or two neighbouring Ra-Rd groups together form alkylenedioxy, provided that not more than three Ra-Rd groups have the same meaning and that X1 is not CCOOH or CCOO-alkyl; G = a protecting group; One of G1 and G2 is H and the other is H, alkyl, OH, alkoxy, aroyl, alkanoyl-OCH2, aroyl-OCH2 or COO-Rg or OCO-Rg; Rg = alkyl optionally substituted by halo, OH, alkoxy, COOH or COO-alkyl. An Independent claim is also included for new intermediates of formula (IV) - (VI). ((V) and (VI) are intermediates for (IV)).</p> |
