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DÉRIVÉS DE TÉTRAHYDRONAPHTALÈNE, PROCÉDÉS DE PRODUCTION DESDITS DÉRIVÉS ET LEUR UTILISATION COMME ANTI-INFLAMMATOIRES
专利权人:
BAYER PHARMA AKTIENGESELLSCHAFT
发明人:
BERGER, MARKUS.,REHWINKEL, HARTMUT.,SCHAECKE, HEIKE.,BAEURLE, STEFAN.,SCHMEES, NORBERT.
申请号:
EP07723399.7
公开号:
EP1994005B9
申请日:
2007.03.15
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
Die Erfindung betrifft mehrfach substituierteTetrahydronaphthalinderivate der Formel (Ia) Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer.Stereoisomer of poly-substiuted tetrahydronaphthalene derivative (I) or its salts with physiologically compatible anion, are new. Stereoisomer of tetrahydronaphthalene derivative of formula (I) or its salts with physiologically compatible anion, excluding 6-fluoro-1-[(2-methylquinolin-5-yl)amino]-4-ethyl-2-(trifluoromethyl)-1,2,3,4-tetrahydronaphthalene-2,5-diol, are new. Either R 1>;, R 2>;1-10C-alkyl, 1-10C-alkoxy (both optionally substituted), H, OH, halo, 1-10C-alkylthio, 1-5C-perfluoroalkyl, CN or NO 2; or R 1>;+R 2>;-O-(CH 2) n-O, -O-(CH 2) n-CH 2-, -O-CH=CH, -(CH 2) n + 2, -NH-(CH 2) n + 1, -N(1-3C-alkyl)-(CH 2) n + 1, -NH-N=CH- or NR 8>;R 9>;, where the terminal O, C and/or N are attached directly to adjacent carbon of the ring; n : 1 or 2; R 8>;, R 9>;H, 1-5C-alkyl or (CO)-1-5C-alkyl; R 3>;1-10C-alkyl, 1-10C-alkoxy (both optionally substituted), H, OH, halo, 1-10C-alkylthio, 1-5C-perfluoroalkyl or CN; R4 : 1-3 of OH, halo, 1-3 of 1-10C-alkyl-substituted 1-5C-alkoxy, optionally substituted 3-7C-cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or 1-5C-alkyl (optionally substituted by 1-3 of OH or 1-3 of COOR 1>; 3>;), 1-5C-alkoxy, NR 8>;R 9>;, exomethylene, O or optionally 1-4 N and/or 1-2 O, 1-2 S or 1-2 keto group containing mono- or bicyclic heteroaryl (where these groups are linked with the amine of the tetrahydronaphthalene system and can be hydrated); R 5>;1-10C-alkyl, optionally partially or completely fluorinated 1-10C-alkyl, 3-7C-cycloalkyl, (1-8C)-alkyl(3-7C)-cycloalkyl, (2-8C)-alkenyl(3-7C)-cycloalkyl, heterocyclyl, 1-8C-alkylheterocyclyl, 2-8C-alkenylheterocyclyl, aryl, 1-8C-alkylaryl, 2-8C-alkenylaryl, 2-8C-alkynylaryl, optionally substituted 1-2 keto group, 1-2 of (1-5C)-alkyl, 1-2 of 1-5C-alkoxy, 1-3 halo, 1-2 exomethylene, 1-3
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