CO5011108A1 - DERIVATIVES OF N- (4-CARBAMIMIDOFENIL) PHENYL-GLYCINAMIDE - Google Patents

Abstract

N- (carbamidofe-nyl) glycinamide derivatives of the formula wherein E is hydrogen or OH, Q is hydrogen or alkyl, R is aryl, cycloalkyl or alkyl which is substituted by R1, R2 and R3, R1 is hydrogen, COOH, COO-alkyl or aryl, R2 is hydrogen, aryl or cycloalkyl or heteroaryl, R3 is hydrogen, aryl or (in a different position from the alpha position relative to the nitrogen atom to which the R alkyl group is attached OH, alkoxy or amino optionally protected, N (Q, R) is pyrrolidino COOH- or COO-alkyl-substituted, piperidino or 1,2,3,4-tetrahydroisoquinolin-3-yl, three of the radicals X1 to X4 independently of each other are a group C (Ra), C (Rb) or C (Rc) and the fourth radical is a group C (Rd) or N, Ra a Rd independently of each other are H, OH, NO2, dialkylamino, halogen, alkyl, alkoxy, aryloxy, aralkyloxy, heteroarylalkyloxy, heterocycloalkyloxy, COOH, COO-alkyl, NH-SO2-alkyl, NHSO2 -aryl, NHCO-alkyl, NHCO-aryl, NHCOO-alkyl, NHCO- alkyl-NH2, NHCO-alkyl-NH-G, 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 adjacent Ra Rd groups together are alkylenedioxy, where no more than three of the radicals Ra to Rd must have the same meaning and X1 must not be CCOOH or CCOO-alkyl, G is an amine protecting group and one of the radicals G1 and G2 is hydrogen and the other radical is hydrogen, alkyl, OH, alkoxy, aroyl, alkanoyl- -OCH2, aroyl-OCH2 or a group COO-Rg or OCO-Rg, Rg is optionally halogen alkyl- , OH-, alkoxy-, COOH- or COO-alkyl-substituted, and hydrates or solvates and their physiologically acceptable salts.