Patent ID: 6444669
Filing Date: 2002-09-03
Classification: A61P,C07D

Abstract:
A pharmaceutical composition, comprising one or more compounds of the following formula I: in whichR1, R1â€² are independently selected from H, F, Cl, Br, I, CF3, NO2, CN, COOH, COO(C1-C6)-alkyl, CONH2, CONH(C1-C6)-alkyl, CON[(C1-C6)-alkyl]2, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, Oâ€”(C1-C6)-alkyl, wherein one or more of the hydrogens of the alkyl radicals may be replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH3, OC(O)H, Oâ€”CH2â€”Ph, NH2, NHâ€”COâ€”CH3 or N(COOCH2Ph)2; â€ƒSO2â€”NH2, SO2NH(C1-C6)-alkyl, SO2N[(C1-C6)-alkyl]2, Sâ€”(C1-C6)-alkyl, Sâ€”(CH2)n-phenyl, SOâ€”(C1-C6)-alkyl, SOâ€”(CH2)n-phenyl, SO2â€”(C1-C6)-alkyl, SO2â€”(CH2)n-phenyl, wherein n is 0-6 and the phenyl radical may be substituted up to two times by F, Cl, Br, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl or NH2; â€ƒNH2, NHâ€”(C1-C6)-alkyl, N[(C1-C6)-alkyl]2, NHâ€”(CO)â€”(C1-C7)alkyl, phenyl, biphenylyl, Oâ€”(CH2)n-phenyl, where n is 0-6, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, wherein any of the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may be substituted one to three times by F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N[(C1-C6)-alkyl]2, SO2â€”CH3, COOH, COOâ€”(C1-C6)-alkyl or CONH2; â€ƒ1,2,3-triazol-5-yl, wherein the triazole ring may be substituted in the 1-, 2- or 3-position by methyl or benzyl; or tetrazol-5-yl, where the tetrazole ring may be substituted in the 1- or 2 position by methyl or benzyl; R2 is H, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (CH2)n-phenyl, (CH2)n-thienyl, (CH2)n-pyridyl, (CH2)n-furyl, C(O)â€”(C1-C6)-alkyl, C(O)â€”(C3-C6)-cycloalkyl, C(O)â€”(CH2)n-phenyl, C(O)â€”(CH2)n-thienyl, C(O)â€”(CH2)n-pyridyl or C(O)â€”(CH2)n-furyl, wherein n is 0-5 and in which any of phenyl, thienyl, pyridyl or furyl may be substituted up to two times by Cl, F, CN, CF3, (C1-C3)-alkyl, OH or Oâ€”(C1-C6)-alkyl; R3 is H, (C1-C6)-alkyl, F, CN, N3, Oâ€”(C1-C6)-alkyl, (CH2)n-phenyl, (CH2)n-thienyl, (CH2)n-pyridyl (CH2)n-furyl, where n is 0-5 and in which phenyl, thienyl, pyridyl or furyl may be substituted up to two times by Cl, F, CN, CF3, (C1-C3)-alkyl, OH or Oâ€”(C1-C6)-alkyl; â€ƒOC(O)CH3, (C2-C6)-alkynyl, (C2-C6)-alkenyl, COO(C1-C6)-alkyl, C(O)OH, C(O)NH2, C(O)NHCH3 or C(O)N(CH3)2; R4 is (CH2)nâ€”R5, wherein n is 0-6; R5 is phenyl, biphenylyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-thienyl, 2- or 3-furyl, 2-, 4- or 5-thiazolyl, 2-, 4- or 5-oxazolyl, 1-pyrazolyl, 3- or 5-isoxazolyl, 2- or 3-pyrrolyl, 2- or 3-pyridazinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl, 2-(1,3,5-triazinyl), 2- or 5-benzimidazolyl, 2-benzothiazolyl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, tetrazol-5-yl, indol-3-yl, indol-5-yl or N-methylimidazol-2-, -4- or -5-yl; and R5 is substituted by â€ƒNHâ€”SO2â€”(C1-C6)-alkyl or NHâ€”SO2-phenyl, wherein the phenyl ring may be substituted up to two times by F, Cl, CN, OH, (C1-C6)-alkyl, Oâ€”(C1-C6)-alkyl, CF3, COOH, COO(C1-C6)-alkyl, CONH2, (CH2)nâ€”SO2â€”(C1-C6)-alkyl, wherein n is 1-6, (CH2)mâ€”SO2â€”NH2, (CH2)mâ€”SO2â€”NHâ€”(C1-C6)-alkyl, (CH2)mâ€”SO2â€”N[(C1-C6)-alkyl]2 or (CH2)mâ€”SO2â€”N(&boxH;CHâ€”N(CH3)2), wherein m is 0-6; and R5 may be further substituted by F, Cl, Br, OH, CF3, NO2, CN, OCF3, Oâ€”(C1-C6)-alkyl, Sâ€”(C1-C6)-alkyl, SOâ€”(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, COOH, COO(C1-C6)-alkyl, COO(C3-C6)-cycloalkyl, CONH2, CONH(C1-C6)-alkyl, CON[(C1-C6)-alkyl]2, CONH(C3-C6)-cycloalkyl, NH2, NHâ€”COâ€”(C1-C6)-alkyl, NHâ€”CO-phenyl, pyrrolidin-1-yl, morpholin-1-yl, piperidin-1-yl, piperazin-1-yl, 4-methylpiperazin-1-yl, (CH2)n-phenyl, Oâ€”(CH2)n-phenyl, Sâ€”(CH2)n-phenyl, SO2â€”(CH2)n-phenyl, wherein n is 0-3; â€ƒand its physiologically acceptable salts and physiologically functional derivatives and further comprising one or more anorectic active ingredients.