发明名称 SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
摘要 This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R<SUP>6</SUP>)-, -S-, -S(O)-, or -S(O<SUB>2</SUB>)-; R<SUP>1</SUP> is selected from the group consisting of aryl and heteroaryl; R<SUP>2</SUP> is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R<SUP>3</SUP> is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R<SUP>4</SUP> and R<SUP>5</SUP> is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR<SUP>8</SUP>R<SUP>9</SUP>, -N(R<SUP>6</SUP>)-(CH<SUB>2</SUB>)<SUB>b</SUB>-NR<SUP>8</SUP>R<SUP>9</SUP>, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
申请公布号 WO2006004880(A3) 申请公布日期 2007.03.08
申请号 WO2005US23187 申请日期 2005.06.28
申请人 SCHERING CORPORATION;JOSIEN, HUBERT, B.;CLADER, JOHN, W.;BARA, THOMAS, A.;XU, RUO;LI, HONGMEI;PISSARNITSKI, DMITRI;ZHAO, ZHIQIANG 发明人 JOSIEN, HUBERT, B.;CLADER, JOHN, W.;BARA, THOMAS, A.;XU, RUO;LI, HONGMEI;PISSARNITSKI, DMITRI;ZHAO, ZHIQIANG
分类号 C07D265/30;A61K31/5377;A61P25/28;C07D413/12;C07D451/02;C07D487/08 主分类号 C07D265/30
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