发明名称 Neurotransmitter releasers useful for cognition enhancement
摘要 Compounds of the following formula have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man involving learning and cognition, where subnormal levels of this neurochemical are found <IMAGE> wherein R1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl; R2 is alkyl of 1 to 10 carbons, cycloalkyl of 3 to 8 carbons, 2-,3-, or 4-pyridyl, Phe or Phe-W; Phe is a phenyl group; W is F, Cl, Br, R4, -OH, -OR4, -NO2, -NH2, -NHR4, -NR4R4, -CN, -S(O)m -R4; R3 is H, F, Cl, Br, -CN, -OH, -NO2, -NH2, -CF3, -NHR4, -NR4R4, R4, -OR4, -S(O)m -R4 R4 is alkyl of 1 to 4 carbons, CH2Phe- or Phe-; R5 is -(CH2)n-Y or -OCOR4; Y is NH2, -NHR4, -NR4R4, -NHCOR4, -NHCO2R4, F, Cl, Br, OR4, -S(O)mR4, -CO2H, -CO2R4, -CN, -CONR4R4, -CON HR4, CONHR4, -CONH2, -COR4; -CH=CHCO2R4, OCOR4, CO 3BOND CCO2R4, -CH=CHR4, or -C 3BOND CR4; m is 0, 1 or 2; n is 1 to 7; and physiologically suitable salts thereof.
申请公布号 US5414004(A) 申请公布日期 1995.05.09
申请号 US19930124523 申请日期 1993.09.20
申请人 THE DU PONT MERCK PHARMACEUTICAL COMPANY 发明人 WILKERSON, WENDELL W.;EARL, RICHARD A.;VOSS, MATTHEW E.
分类号 C07D239/26;A61K31/44;A61K31/4409;A61K31/4418;A61K31/4427;A61K31/443;A61K31/495;A61P25/28;C07D213/24;C07D213/44;C07D213/50;C07D213/55;C07D213/57;C07D213/61;C07D241/12;C07D401/06;C07D403/06;C07D405/06;C07D405/12;(IPC1-7):A61K31/44;C07D401/14 主分类号 C07D239/26
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