发明名称 Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
摘要 This invention discloses novel gamma secretase inhibitors of the formula: 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: 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 US2006040936(A1) 申请公布日期 2006.02.23
申请号 US20050168797 申请日期 2005.06.28
申请人 JOSIEN HUBERT B;CLADER JOHN W;BARA THOMAS A;XU RUO;LI HONGMEI;PISSARNITSKI DMITRI A;ZHAO ZHIQIANG 发明人 JOSIEN HUBERT B.;CLADER JOHN W.;BARA THOMAS A.;XU RUO;LI HONGMEI;PISSARNITSKI DMITRI A.;ZHAO ZHIQIANG
分类号 A61K31/5377;C07D413/02;C07D487/04 主分类号 A61K31/5377
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