| 摘要 |
In the present invention there are disclosed peptide derivatives of the general formula I, in which Re1 represents alkyl containing 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, aryl, alkylaryl containing 1 to 6 carbon atoms in the alkyl moiety or alkyl-Are9 with 1 to 6 carbon atoms in the alkyl moiety and where A represents oxygen, NRe9 or S(O)im, wherein m = 0 to 2 and/or each Re9 represents hydrogen, alkyl containing 1 to 4 carbon atoms, aryl or alkylaryl containing 1 to 4 carbon atoms in the alkyl moiety, Re2 represents hydrogen or alkyl containing 1 to 6 carbon atoms, Re4 represents hydrogen or alkyl containing 1 to 6 carbon atoms being optionally substituted with amine (NHi2), arylamine, a protected amine, aryl, dialkylamine containing 1 to 6 carbon atoms in the alkyl moiety, monoalkylamine containing 1 to 6 carbon atoms in the alkyl moiety, COOH, a protected carboxyl, carbamoyl, monoalkylcarbamoyl containing 1 to 6 carbon atoms in the alkyl moiety or dialkylcarbamoyl containing 1 to 6 carbon atoms in the alkyl moiety, and Re5 represents hydrogen or alkyl containing 1 to 6 carbon atoms, or NRe4Re5 represents pyrrolidine, piperidine or morpholine, Re6 represents an optionally substituted cycloalkyl containing 3 to 6 carbon atoms, cycloalkenyl having 3 to 6 carbon atoms, alkyl containing 1 to 6 carbon atoms, benzyl, alkoxybenzyl containing 1 to 6 carbon atoms in the alkoxy moiety, benzyloxybenzyl or 3-indolylmethyl, Alk represents alkyl containing 1 to 6 carbon atoms, or alkenyl containing 2 to 6 carbon atoms and n = 0 or 1, Re7 represents hydrogen H or Re10CO, wherein Re10 represents alkyl containing 1 to 4 carbon atoms, alkylaryl containing 1 to 4 carbon atoms in the alkyl moiety, cycloalkyl containing 3 to 6 carbon atoms, cycloalkylalkyl containing 3 to 6 carbon atoms in the cyclo alkyl moiety and 1 to 4 carbon atoms in the alkyl moiety, alkenyl having 2 to 6 carbon atoms, alkenylaryl having 2 to 6 carbon atoms in the alkenyl moiety, and Re8 represents hydrogen, alkyl containing 1 to 4 carbon atoms, alkylaryl containing 1 to 4 carbon atoms in the alkyl moiety or aryl or salt, solvates or hydrates thereof as well as pharmaceutical preparation in which they are comprised. Those compounds can be used for treating states connected with metalloproteinases, TNF and/or another activity.
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