发明名称 (PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES
摘要 The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R<SUP>1</SUP>, R<SUP>2 </SUP>and R<SUP>3 </SUP>are independently H or (C<SUB>1-4</SUB>)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C<SUB>1-4</SUB>)alkyl, (C<SUB>1-4</SUB>)alkyloxy, (C<SUB>1-4</SUB>)alkyloxy(C<SUB>1-4</SUB>)alkyl, CF<SUB>3</SUB>, halogen, nitro, cyano, NR<SUP>4</SUP>R<SUP>5</SUP>, NR<SUP>4</SUP>COR<SUP>6</SUP>, and CONR<SUP>4</SUP>R<SUP>5</SUP>; R<SUP>4 </SUP>and R<SUP>5 </SUP>are independently H or (C<SUB>1-4-</SUB>)alkyl; or R<SUP>4 </SUP>and R<SUP>5 </SUP>form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR<SUP>6</SUP>; R<SUP>6 </SUP>is (C<SUB>1-4</SUB>)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C<SUB>1-4</SUB>)alkyl, (C<SUB>1-4</SUB>)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
申请公布号 US2008262221(A1) 申请公布日期 2008.10.23
申请号 US20080024597 申请日期 2008.02.01
申请人 N.V. ORGANON 发明人 GROVE SIMON JAMES ANTHONY;ADAM-WORALL JULIA;ZHANG MINGQIANG;GILFILLAN ROBERT
分类号 C07D498/04;A61K31/553;A61P9/00;A61P15/10;A61P17/02;A61P25/00;A61P25/08;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P25/32;A61P43/00;C07D498/14 主分类号 C07D498/04
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