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Combination of selected analgesics with COX II inhibitors
专利权人:
Grünenthal GmbH
发明人:
HAASE, Günter,KÖGEL, Babette-Yvonne,FRIDERICHS, Elmar,SCHIENE, Klaus,JAHNEL, Ulrich
申请号:
DK03775368
公开号:
DK1562567T3
申请日:
2003.11.18
申请国别(地区):
DK
年份:
2017
代理人:
摘要:
Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII). Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII), where (A) is a phenyl-substituted tertiary amine of formulae (I)-(III), as racemates, pure or mixed stereoisomers (particularly enantiomers or diastereoisomers), optionally in the form of acids, bases, salts or solvates, preferably hydrates. [Image] X : hydroxy, fluoro, chloro, hydrogen or OCOR 7>;; R 1>;1-4C linear, branched, saturated or unsaturated alkyl, optionally substituted one or more times, in (I), or 1-4C alkyl, benzyl, trifluoromethyl, hydroxy, benzyloxy. 1-3C alkoxy, chloro or fluoro in (II); R 2>; and R 3>;hydrogen or 1-4C alkyl (as for R 1>;) or together form an optionally substituted 4-7C cycloalkyl; R 9>;-R 1>; 3>;hydrogen, fluoro, chloro, bromo, iodo, (di)fluoromethyl, trifluoromethyl, hydroxy, thiol, OR 1>; 4>;, trifluoromethoxy, SR 1>; 4>;, NR 1>; 7>;R 1>; 8>;, (trifluoro)methyl- sulfinyl or -sulfonyl, cyano, COOR 1>; 4>;, nitro, CONR 1>; 7>;R 1>; 8>;, 1-6C alkyl (as above) or phenyl, optionally substituted one or more times; R 1>; 4>;1-6C alkyl, pyridyl, thienyl, thiazolyl, phenyl, benzyl, phenethyl (all optionally substituted one or more times), PO(O-1-4C alkyl)-2, COO1-5C alkyl, CONH(1-3C alkylphenyl), CO(1-5C)alkyl, COCHR 1>; 7>;-NHR 1>; 8>;, or CO-phenylene-R 1>; 5>;; R 1>; 5>;ortho-OCO(1-3C)alkyl, or meta- or para-CH 2N(R 1>; 6>;) 2; R 1>; 6>;1-4C alkyl or morpholino, and all alkyl in R 1>; 4>;-R 1>; 6>; are optionally substituted one or more times; R 1>; 7>; and R 1>; 8>;hydrogen, 1-6C alkyl (as above), phenyl, benzyl or phenethyl, all optionally substituted one or more times; R 1>; 0>; with either of R 9>; or R 1>; together : a OCH 2O, OCH 2CH 2O, OCH=CH, CH=CHO, CH=CMeO, OCMe=CH, (CH 2) 4 or OCH=CHO ring; proviso: in (III), when R 9>;, R 1>; 1>; and R 1&
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