Patent ID: 6667345
Filing Date: 2003-12-23
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, 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, 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, (C3-C8)cycloalkyl, (C2â€”C8)-alkenyl, or (C2â€”C8)-alkynyl, where in the alkyl, alkenyl and alkynyl groups in each case 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 or heterocycle 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€”SO2-(C1-C4)-alkyl, COOH, COâ€”Oâ€”(C1-4)-alkyl, or COâ€”NH2 and where in the alkyl groups one to seven hydrogen atoms may be replaced by fluorine; X is SO2; Y is (CH2)p, where p may be 0, 1, 2 or 3; R5 is CF3, (C1-C18)-alkyl, or (C3-C8)-cycloalkyl, where in the alkyl groups one to seven hydrogen atoms may be replaced by fluorine; (CH2)rCOR6, where r=1-6 and R6 may be OH, Oâ€”(C1-C6)-alkyl or NH2; CH2â€”CH(NHR7)-COR8, where R7 may be H or C(O)â€”(C1-C4)-alkyl and R8 may be OH, Oâ€”(C1-C6)-alkyl or NH2; or phenyl, 1- or 2-naphthyl, or biphenyl, where the rings or ring systems may be substituted up to two 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€”(C2-C8)-alkyl, NHâ€”COâ€”(C3-C8)-cycloalkyl; SO3H, SO2â€”NH2, SO2â€”NHâ€”(C1-C8)-alkyl, SO2â€”NHâ€”(C3-C8) -cycloalkyl; NHâ€”SO2â€”N H2, NHâ€”SO2â€”(C1-C8)-alkyl, NHâ€”SO2â€”(C3-C8) cycloalkyl, Oâ€”CH2â€”COOH, Oâ€”CH2â€”H2â€”COâ€”O(C1-C8)-alkyl, COOH, COâ€”O(C1-C 8-alkyl, COâ€”Oâ€”(C3-C8)-cycloalkyl, COâ€”NH2, COâ€”NH(C 1-C8)-alkyl, COâ€”N [(C1-C8)-alkyl]2, (C1-8)-alkyl, or (C3-C8)-cycloalkyl, where in the alkyl groups in each case one to seven hydrogen atoms may be replaced by fluorine; R9 is (C1-C2)-alkyl, or (C3-C8)-cycloalkyl, where in the alkyl radicals one to seven hydrogen atoms may be replaced by fluorine; COâ€”O(C1-C6)-alkyl, COâ€”O(C3-C8)-cycloalkyl, C(O)â€”(C1-C8)-alkyl, C(O)â€”(C3-C8)-cycloalkyl, C(O)-phenyl, C(O)â€”CH(NHR12)â€”(C1-C8)-alkyl, phenyl, 1- or 2-naphthyl, or biphenyl, where the aryl radicals may be substituted up to two times by F, Cl, Br, CN, OH, (C1-C4)-alkyl, CF3, Oâ€”(C1-C4)-alkyl, S(O)2-0(C1-C6)-alkyl, NH2, NHâ€”SO2(C1-C4)-alkyl, â€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O(C1-C8)-alkyl, COOH, COâ€”Oâ€”(C1-C4-alkyl, COâ€”NH2; (CH2)â€”R10; (CH2)sâ€”R11, where s=2 or 3; R10 is (C1-C12)-alkyl, or (C3-C8)-cycloalkyl, where in the alkyl radicals one to seven hydrogen atoms may be replaced by fluorine; COOH, CONH2, COâ€”O(C1-C6)-alkyl, COâ€”O(C3-C8)-cycloalkyl; phenyl, 1- or 2-naphthyl, biphenyl, where the aryl radicals 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€”SO2-(C1-C4)-alkyl, Oâ€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O (C1-C8)-alkyl, COOH, COâ€”Oâ€”(C1-C4-alkyl, COâ€”NH2; R11 is (C1-C12)-alkyl, or (C3-C8)-cycloalkyl, where in the alkyl radicals one to seven hydrogen atoms may be replaced by fluorine; COOH, CONH2, COâ€”O(C1-C6)-alkyl, COâ€”O(C3-C8)-cycloalkyl; phenyl, 1- or 2-naphthyl, or biphenyl, where the aryl radicals 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, Oâ€”CH2â€”COOH, Oâ€”CH2â€”COâ€”O(C1-C8) -alkyl, COOH, COâ€”Oâ€”(C1-C4)-alkyl, or COâ€”NH2; R12 is H, C(O)â€”(C1-C6)-alkyl; and their physiologically acceptable salts.