| 摘要 |
4-18757/A N-Acyl-N-heterocyclylalkylamino acids, processes, compositions and use The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula (I), wherein R1 is C1-C7alkyl that is unsubstituted or substituted by halogen or by hydroxy, or is C2-C7-alkenyl, C3-C7cycloalkyl, C3-C7cycloalkoxy, C1-C7alkoxy or C3-C7cycloalkyl-C1-C7-alkoxy; R2 is 1H-tetrazol-5-yl, carboxy, C1-C7alkoxycarbonyl, SO3H, PO2H2, PO3H2 or halo-C1-C7alkanesulfonylamino; R3 is 1H-tetrazol-5-yl, hydroxymethyl, C1-C7alkoxymethyl, formyl, carboxy, C1-C7-alkoxycarbonyl, C1-C7alkoxy-C1-C7alkoxycarbonyl, phenyl-C1-C4alkoxycarbonyl or carbamoyl, the amino group of which is unsubstituted or mono-substituted by C1-C7alkyl, C3-C7alkenyl or by phenyl-C1-C7alkyl or di-substituted by C1-C7alkyl, C3-C7alkenyl or by phenyl-C1-C7alkyl independently of one another, or is di-substituted by C2-C7alkylene or by C2-C4alkyleneoxy-C2-C4alkylene; Alk is methylene, ethylene or ethylidene; Het is (i) wherein Y1 is O, S or N(R) and R is hydrogen or C1-C7alkyl; or (ii) wherein one of the variables Y2 and Y3 is C(R') and the other is N or each of the variables is C(R'); and R' is hydrogen, halogen, C1-C7alkyl, C1-C7alkoxy, C2-C7alkenyloxy, phenoxy, benzyloxy, trifluoromethyl or S(O)m-R, wherein m is 0, 1 or 2; and R ishydrogen or C1-C7alkyl; X1 is -CO- or -S(O)m- and the index m is 0, 1 or 2; one of the variables X2 and X4 is C1-C4alkylene and the other of the variables X2 and X4 is a bond; or each of the variables X2 and X4 is a bond; X3 is C3-C7cycloalkylidene or the structural element -C(Xa)(Xb)- and Xa is hydrogen or C1-C7alkyl and Xb is C1-C7alkyl; and the rings A, B, C and D, with the exception of the substiluents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C1-C7alkyl, C1-C7aLkoxy, C2-C7alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O)m-R, wherein m is 0, 1 or 2 and R is hydrogen or C1-C7alkyl; and their salts; preparation processes, pharmaceutical compositions comprising acompound of formula I or a pharmaceutically acceptable salt thereof, and use.
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