发明名称 Derivatives of 4,5,6,7-tetrahydroimidazo-[4,5-c]pyridinyl-6-carboxylic acid
摘要 This invention pertains to a method for treating a condition of nausea and vomiting in a mammal which comprises administering a therapeutically effective amount of a 4,5,6,7-tetrahydroimidazo[4,5-c]pyridinyl-6-carboxylic acid derivative represented by the formula: <IMAGE> (1) wherein R1 and R2 are hydrogen or lower-alkyl; R3 is selected from the group consisting of hydrogen, lower-alkyl, nitro, amino, cyano, and alkylmercapto; R4 and R5 are selected from the group consisting of hydrogen, lower-alkyl, aryl, and aryl lower-alkyl, or R4 and R5 together with the carbon atom to which they are attached form a 5- or 6-member saturated hydrocarbon ring; R6 is selected from the group consisting of hydrogen, lower-alkyl, aryl lower-alkyl, formyl, lower-alkyl carbonyl, and aryl carbonyl; R7 is selected from the group consisting of phenyl, thienyl, indolyl, indazolyl, benzo[b]furanyl, benzo[b]thiophenyl, and R8R9-N-; R8 is selected from the group consisting of 8-[1,2,3,4,-tetrahydroquinolinyl], pyridinyl, 3-quinolinyl, 2-naphthalinyl, 2-thiazolyl, 2-benzothiazolyl, 4-[2,1,3]benzothiadiazolyl, 2-(4,5,6,7-tetrahydrobenzo)thiazolyl, 7-(2,2-dimethyl-2,3-dihydrobenzo)furanyl, and phenyl; R9 is hydrogen or lower-alkyl; R8R9-N- is selected from the group consisting of 1-indolinyl, 1-(3,3-dimethylindolinyl), and 1-(1,2,3,4-tetrahydroquinolinyl); wherein the groups represented by R7 other than R8R9N- may be unsubstituted or substituted with one or more substituents selected from the group consisting of lower-alkyl, lower-alkoxy, di-lower-alkylamino, and aryloxy, and the groups represented by R8 and the radical R8R9N- may have one or more substituents selected from the group consisting of hydroxy, halogen, lower-alkyl, lower-alkoxy, amino, mono- or di-lower-alkylamino, lower-alkyl carbonyl, lower-alkoxy carbonyl, and aryloxy; wherein each aryloxy group may be unsubstituted or substituted with substituents independently selected from the group consisting of lower-alkyl, lower-alkoxy, halogen, and trifluoromethyl with the proviso that, when R8 is phenyl, said phenyl group contains at least one substituent.
申请公布号 US5262537(A) 申请公布日期 1993.11.16
申请号 US19930033522 申请日期 1993.03.19
申请人 ANAQUEST, INC. 发明人 HUANG, BAO-SHAN;FENG, DANGING D.;GALL, MARTIN;EVANS, SUZANNE M.;PARADKAR, VIDYADHAR M.;NAIR, RAGHUNATHAN V.;LATHAM, TAMARA B.
分类号 C07D471/04;(IPC1-7):A61K31/445;A61K31/415;C07D471/10 主分类号 C07D471/04
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