发明名称 DISUBSTITUTED POLYCYCLIC SYSTEMS AS COGNITION ENHANCERS
摘要 Compounds of formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found. The compounds of this invention can be described as shown in formula (I), where Q is (II), (III) and (IV); R<1> is 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl; R<2> and R<3> are independently H, F, Cl, Br, NO2, OH, -R<4>, -O-R<4>, -CO2R<4>, -COR<4>, -CONH2, -CONHR<4>, -CONR<4>R<4'>, -S(O)m2-R<4>, NH2, CF3, NHR<4>, NR<4>R<4'>; R<4> and R<4'> are independently H, alkyl of 1 to 4 carbons, CH2Phe-W or Phe-W; Phe is a phenyl group; R<5> is -(CH2)n-Y or -OCOR<4>; Y is H, OH, NH2, NHR<4>, NR<4>R<4'>, NHCOR<4>, NHCO2R<4>, NHS(O)2R<4>; F, Cl, Br, OR<4>, S(O)mR<4>, -CO2H, -CO2R<4>, -CN, -CONR<4>R<4'>, -CONHR<4>, -CONH2, -COR<4>; -CH=CHCO2R<4>, -OCOR<4>, Phe, Phe-W, -C=CCO2R<4>, -CH=CHR<4>, or -C=C-R<4>; W is F, Cl, Br, R<4>, OR<4>, NO2, NH2, NHR<4>, NR<4>R<4>, CN, S(O)m-R<4>; m is 0, 1 or 2; n is 1 to 7; and hydrates and physiologically suitable salts thereof.
申请公布号 WO9314092(A1) 申请公布日期 1993.07.22
申请号 WO1992US11293 申请日期 1992.12.30
申请人 THE DU PONT MERCK PHARMACEUTICAL COMPANY 发明人 WILKERSON, WENDELL, WILKIE;TELEHA, CHRISTOPHER, ALLAN
分类号 C07D239/26;A61K31/435;A61K31/44;A61K31/4409;A61K31/4418;A61K31/4427;A61K31/505;A61P25/00;A61P25/28;C07D213/06;C07D213/16;C07D213/24;C07D213/26;C07D213/30;C07D213/38;C07D213/40;C07D213/42;C07D213/53;C07D213/55;C07D213/56;C07D213/57;C07D213/61;C07D241/12;C07D401/06;C07D471/04 主分类号 C07D239/26
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