Patent ID: 6812256
Filing Date: 2004-11-02
Classification: A61K,A61P

Abstract:
A compound of the formula I, in whichR1, R2, R3, R4 independently of one another are H, F, Cl, Br, I, CN, N3, NO2, OH, O(C1-C8)-alkyl, O(C3-C8)-cycloalkyl, Oâ€”CH2-phenyl, O-phenyl, Oâ€”COâ€”(C1-C8)-alkyl, Oâ€”COâ€”(C3-C8)-cycloalkyl, where in the alkyl radicals up to seven hydrogen atoms may be replaced by fluorine; S(O)0-2(C1-C8)-alkyl, S(O)0-2(C3-C8)-cycloalkyl, wherein in the alkyl radicals up to seven hydrogen atoms may be replaced by fluorine; NH2, NHâ€”(C1-C8)-alkyl, NHâ€”(C3-C8)-cycloalkyl, N[(C1-C8)-alkyl]2, N[(C3-C8)-cycloalkyl]2, NHâ€”COâ€”(C1-C8)-alkyl, or NHâ€”COâ€”(C3-C8)-cycloalkyl; SO3H; SO2â€”N2, SO2â€”NHâ€”(C1-C8)-alkyl, SO2â€”NHâ€”(C3-C8)-cycloalkyl; SO2â€”(C1-C6)-alkyl NHâ€”SO2â€”NH2; NHâ€”SO2â€”(C1-C8)-alkyl, NHâ€”SO2â€”(C3-C8)-cycloalkyl; Oâ€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O(C1-C8)-alkyl, COOH, COO(C1-C8)-alkyl, COâ€”Oâ€”(C3-C8)-cycloalkyl, COâ€”NH2, COâ€”NH(C1-C8)-alkyl, COâ€”N[(C1-C8)-alkyl]2; (C1-C8)-alkyl, (C3-C8)cycloalkyl, (C2-C8)-alkenyl, or (C2-C8)-alkynyl, wherein in the alkyl, alkenyl and alkynyl groups one to seven hydrogen atoms may be replaced by fluorine; or one hydrogen may be replaced by OH, OC(O)CH3, Oâ€”CH2â€”Ph, NH2, NHâ€”COâ€”CH3 or N(COOCH2Ph)2; phenyl, 1- or 2-naphthyl, where the aryl radical may be substituted up to two times by F, Cl, Br, CN, OH, (C1-C4)-alkyl, CF3, Oâ€”(C1-C4)-alkyl, S(O)0-2(C1-C6)-alkyl, NH2, NHâ€”SO2â€”(C1-C4)-alkyl, COOH, COâ€”Oâ€”(C1-C4)-alkyl, COâ€”NH2 and wherein in the alkyl groups one to seven hydrogen atoms may be replaced by fluorine; X is SO; Y is (CH2)p, where in p may be 0, 1, 2 or 3; R5 is (C1-C18)-alkyl, or (C3-C8)-cycloalkyl, wherein in the alkyl groups up to seven hydrogen atoms may be replaced by fluorine; (CH2)1-6â€”COOH, (CH2)1-6â€”COOâ€”(C1-C6)-alkyl, (CH2)1-6â€”CONH2; CH2â€”CH(NHR10)-COR11, where R10 may be H or C(O)â€”(C1-C6)-alkyl and R11 may be OH, Oâ€”(C1-C6)-alkyl or NH2; phenyl, 1- or 2-naphthyl, or biphenyl, where the rings or ring systems are in each case substituted up to three times by F, Cl, Br, I, CN, OH, O(C1-C8)-alkyl, O(C3-C8)-cycloalkyl, Oâ€”COâ€”(C1-C8)-alkyl, Oâ€”COâ€”(C3-C8)-cycloalkyl, S(O)0-2(C1-C8)-alkyl, S(O)0-2(C3-C8)-cycloalkyl, NH2, NHâ€”(C1-C8)-alkyl, NHâ€”(C3-C8)-cycloalkyl, N[(C1-C8)-alkyl]2, N[(C3-C8)-cycloalkyl]2, NHâ€”COâ€”(C1-C8)-alkyl, NHâ€”COâ€”(C3-C8)-cycloalkyl, SO3H; SO2â€”NH2, SO2â€”NHâ€”(C1-C8)-alkyl, SO2â€”NHâ€”(C3-C8)-cycloalkyl, NHâ€”SO2â€”NH2; NHâ€”SO2â€”(C1-C8)-alkyl, NHâ€”SO2â€”(C3-C8)-cycloalkyl, Oâ€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O(C1-C8)-alkyl, COOH, COâ€”O(C1-C8)-alkyl, COâ€”Oâ€”(C3-C8)-cycloalkyl, COâ€”NH2, COâ€”NH(C1-C8)-alkyl, COâ€”N[(C1-C8)-alkyl]2; (C1-C8)-alkyl, or (C3-C8)-cycloalkyl, wherein in the alkyl groups in each case one to seven hydrogen atoms may be replaced by fluorine; R6 is (CH2)0-6-R9, (CH2)0-6â€”COOH, (CH2)0-6â€”COOâ€”(C1-C6)-alkyl, (CH2)0-6â€”CONH2, (CH2)0-6â€”CH(NHR15)â€”COR16, F, Cl, Br, CN, (C1-C18)-alkyl, (C3-C4)-cycloalkyl, or (C6-C8)-cycloalkyl, where in the alkyl radicals or cycloalkyl radicals up to seven hydrogen atoms may be replaced by fluorine; R15 is H or C(O)â€”(C1-C6)-alkyl; R16 is OH, Oâ€”(C1-C6)-alkyl, or NH2, R7 is (CH2)0-4â€”R12, H, (C1-C12)-alkyl, (C3-C4)-cycloalkyl, (C6-C8)-cycloalkyl, COO(C1-C6)-alkyl, or COO(C3-C8)-cycloalkyl, wherein in the alkyl radicals or cycloalkyl radicals up to seven hydrogen atoms may be replaced by fluorine; R8 is (CH2)0-4â€”R14, (C1-C12)-alkyl, (C3-C4)-cycloalkyl, or (C6-C8)-cycloalkyl, wherein in the alkyl or cycloalkyl radicals up to seven hydrogen atoms may be replaced by fluorine atoms; R9, R12, R14 independently of one another are phenyl, 1- or 2-naphthyl, or biphenyl, where the rings or ring systems are in each case substituted up to three times by F, CI, Br, I, CN, OH, O(C1-C8)-alkyl, O(C3-C8)-cycloalkyl, Oâ€”COâ€”(C1-C8)-alkyl, Oâ€”COâ€”(C3-C8)-cycloalkyl, S(O)0-2(C1-C8)-alkyl, S(O)0-2(C3-C8)-cycloalkyl, NH2, NHâ€”(C1-C8)-alkyl, NHâ€”(C3-C8)-cycloalkyl, N[(C1-C8)-alkyl]2, N[(C3-C8)-cycloalkyl]2, NHâ€”COâ€”(C1-C8)-alkyl, NHâ€”COâ€”(C3-C8)-cycloalkyl, SO3H; SO2â€”NH2, SO2â€”NHâ€”(C1-C8)-alkyl, SO2â€”NHâ€”(C3-C8)-cycloalkyl, NHâ€”SO2â€”NH2; NHâ€”SO2â€”(C1-C8)-alkyl, NHâ€”SO2â€”(C3-C8)-cycloalkyl; Oâ€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O(C1-C8)-alkyl, COOH, COâ€”O(C1-C8)-alkyl, COâ€”Oâ€”(C3-C8)-cycloalkyl, COâ€”NH2, COâ€”NH(C1-C8)-alkyl, COâ€”N[(C1-C8)-alkyl]2; (C1-C8) alkyl, or (C3-C8)-cycloalkyl, wherein in the alkyl groups, in each case one to seven hydrogen atoms may be replaced by fluorine; and their physiologically acceptable salts.