发明名称 N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATIONAND USE THEREOF
摘要 Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N- aryldiazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. T he aryl group can be a five or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variet y of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic choligernic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treat ed and/or prevented. The compounds and compositions can also be used to allevia te pain. The compounds can: ( I ) alter the number of nicotinic cholinergic receptors of the brain of the patient, ( ii ) exhibit neuroprotective effect s and ( iii ) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blo od pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effectsupon skeletal muscle).</SDOAB >
申请公布号 CA2491506(A1) 申请公布日期 2004.01.15
申请号 CA20032491506 申请日期 2003.06.27
申请人 TARGACEPT, INC. 发明人 SCHMIDT, JEFFREY D.;MILLER, CRAIG H.;BHATTI, BALWINDER S.
分类号 A61K31/4439;A61K31/444;A61K31/506;A61P1/02;A61P1/04;A61P1/16;A61P19/02;A61P25/00;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P29/00;A61P31/04;A61P31/10;A61P31/12;A61P31/18;A61P37/06;A61P43/00;C07D453/00;C07D471/10;C07D487/10;C07D487/20;(IPC1-7):C07D487/10;C07D453/02;C07D471/20;A61K31/40;A61K31/435 主分类号 A61K31/4439
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