发明申请
US20100087425A1 Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors
审中-公开
取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂
- 专利标题: Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors
- 专利标题(中): 取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂
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申请号: US12633286申请日: 2009-12-08
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公开(公告)号: US20100087425A1公开(公告)日: 2010-04-08
- 发明人: Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitaki , Zhiqiang Zhao
- 申请人: Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitaki , Zhiqiang Zhao
- 专利权人: Schering Corp.
- 当前专利权人: Schering Corp.
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D413/14 ; C07D413/12 ; C07D417/12 ; C07D417/14 ; A61K31/541 ; A61P25/00 ; A61P25/28
摘要:
This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 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; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and aryl heterocycloalkyl; 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.
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