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 |