| 摘要 |
2,4-Disubstituted 5-sulfonyl-benzamides (or analogs) (I) are new. Sulfonyl-carboxamides of formula (I) (or their salts or functional derivatives) is claimed for the preparation of medicaments for treating or preventing hyperlipidemia or arteriosclerosis. X, R1-R3 = NR6R7, -(CH2)n-Ph', pyridylmethyl or 1-8C alkyl; or pyrrolidine, piperazine, piperazin-2-one, morpholine or tetrahydropyridine (all optionally substituted by Ph'', alkyl-Ph'', 1-8C alkyl, hydroxyalkyl, OPh'', SPh'', alkylcarbonyl or COPh''); n = 0-6; Ph' = phenyl (optionally substituted by 1-2 F, Cl, Br, CF3, NH2, CN, OCF3, alkoxy, alkylthio, alkyl, cycloalkyl, alkoxycarbonyl, cycloalkoxycarbonyl, CONH2 and mono- or dialkylcarbamoyl); Ph'' = phenyl (optionally substituted by 1-2 F, Cl, Br, OH, CF3, CN, OCF3, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkyl, cycloalkyl, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CONH2, mono- or dialkylcarbamoyl, cycloalkylcarbamoyl, NH2, alkylcarbonylamino and benzamido); R6, R7 = H, alkyl, alkoxyalkyl, alkoxy, cycloalkyl, alkylcarbonyl, alkyl-NH-CO-alkyl, mono- or dialkylaminoalkyl, alkyl-O-phenyl, CHO, COPh or -(CH2)n-Ar; Ar = phenyl, biphenyl, 1- or 2-naphthyl, 1- or 2-tetrahydrofuranyl, 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-, 4- or 5-isoxazolyl, cycloalkyl, piperidinyl, pyrrolidinyl, oxopyridinyl, 2- or 3-pyrrolyl, 2- or 3-pyridazinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl, 1,3,5-triazin-2-yl, 2-, 3- or 4-morpholinyl, 2- or 5-benzimidazolyl, 2-benzothiazolyl, 1,2,4-triazol-3-yl, 1,2,4-triazol-3-yl, tetrazol-5-yl, indol-3-yl, indol-5-yl or N-methyl-imidazol-2-, 4- or 5-yl (all optionally substituted by 1 or 2 of F, Cl, Br, OH, CF3, NO2, CN, OCF3, OCH2O, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkyl, cycloalkyl, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CONH2, mono- or dialkylcarbamoyl, cycloalkylcarbamoyl, NH2, alkylcarbonylamino, benzamido, pyrrolidin-1-yl, morpholin-1-yl, piperidin-1-yl, piperazin-1-yl, 4-methyl-piperazin-1-yl, -(CH2)m-Ph, -O(CH2)m-Ph, -S(CH2)m-Ph and -SO2(CH2)m-Ph); and m = 0-3; Unless specified otherwise alkyl moieties have 1-6C and cycloalkyl moieties 3-6C. An Independent claim is included for the preparation of (I). |
