发明名称 7-aza-bicyclo[2.2.1]-heptane derivatives, their preparation and use according to their affinity for neuronal nicotinic acetylcholine receptors
摘要 <p>Compounds of the formula <CHEM> wherein R<1>, R<2>, R<3> and R<4> are selected, independently from hydrogen, -CO2R<5>, aryl and heteroaryl, wherein said aryl is selected from phenyl and naphthyl and said heteroaryl is selected from pyrazinyl, benzofuranyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, 1,2,5-thiadiazolyl, quinazolinyl, pyridazinyl, pyrazinyl, cinnolinyl, phthalazinyl, quinoxalinyl, xanthinyl, hypoxanthinyl, pteridinyl, 5-azacytidinyl, 5-azauracilyl, triazolopyridinyl, imidazolopyridinyl, pyrrolopyrimidinyl, pyrazolopyrimidinyl, oxazolyl, isoxazoyl, thiazolyl, isothiazolyl, furanyl, pyrazolyl, pyrrolyl, tetrazolyl, triazolyl, thienyl, imidazolyl, pyridinyl, and pyrimidinyl, and wherein said phenyl and said heteroaryl may optionally be substituted with from one to three substituents, and are preferably substituted with one or two substituents, independently selected form (C1-C6)alkyl optionally substituted with from one to seven fluorine atoms, halo, phenyl, benzyl, hydroxy, acetyl, amino, cyano, nitro, (C1-C6)alkoxy optionally substituted with from one to seven fluorine atoms, (C1-C6)alkylamino and Ä(C1-C6)alkylÜ2amino; R<6> is hydrogen or (C1-C6)alkyl; with the proviso that: (a) at least one of R<1>, R<2>, R<3>, and R<4> must be aryl or heteroaryl; (b) when neither R<1> nor R<2> is hydrogen, R<1> and R<2> are in the "exo" configuration; (c) R<1> and R<2> can not both be -CO2R<5>; (d) if either R<3> or R<4> is CO2R<5> and R<5> is an alkyl or alkoxyalkyl group, then one of R<1> and R<2> must be aryl or heteroaryl; and (e) if either R<1> or R<2> is CO2R<5> and R<5> is an alkyl or alkoxyalkyl group, then one of R<3> and R<4> must be aryl or heteroaryl; and their pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.</p>
申请公布号 EP0955301(A3) 申请公布日期 2001.04.18
申请号 EP19990302306 申请日期 1999.03.25
申请人 PFIZER PRODUCTS INC. 发明人 YOHANNES, DANIEL;BUNDESMANN, MARK WERNER
分类号 A61K31/00;A61K31/40;A61K31/407;A61K31/41;A61K31/415;A61K31/4155;A61K31/4164;A61K31/4178;A61K31/4192;A61K31/4196;A61K31/42;A61K31/422;A61K31/4245;A61K31/425;A61K31/427;A61K31/433;A61K31/44;A61K31/4427;A61K31/4439;A61K31/495;A61K31/498;A61K31/50;A61K31/501;A61K31/505;A61K31/506;A61P1/00;A61P1/04;A61P3/00;A61P3/04;A61P9/00;A61P9/06;A61P9/12;A61P21/00;A61P25/00;A61P25/04;A61P25/06;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P25/34;A61P29/00;A61P35/00;C07D487/08;C07D519/00;(IPC1-7):C07D487/08 主分类号 A61K31/00
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