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    • 8. 发明授权
    • Amino naphthyridine compounds as anti-rhoumatic agents
    • 氨基萘啶化合物作为抗风湿剂
    • US5464781A
    • 1995-11-07
    • US244369
    • 1994-06-03
    • Bernard J. ArmitageJohn G. BowenMalcolm J. CrossleyIan M. HunneyballBruce W. LeslieThomas K. MillerMichael Spowage
    • Bernard J. ArmitageJohn G. BowenMalcolm J. CrossleyIan M. HunneyballBruce W. LeslieThomas K. MillerMichael Spowage
    • A61K31/435A61K31/44A61P29/00C07D471/04
    • C07D471/04
    • This invention relates to compounds of formula I and pharmaceutically acceptable salts thereof ##STR1## in which R.sub.1 represents hydrogen, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonyalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy alkoxycarbonyl or alkanoylamino; R.sub.2 represents hydrogen, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R.sub.3 represents hydrogen or alkyl; R.sub.4 represents hydrogen, halo, alkoxycarbonyl, a benzyloxycarbonyl, alkanoyl, benzoyl, carbamoyl, alkyl, carboxy, hydroxyalkyl or alkylthio; R.sub.5 represents hydrogen or alkyl; R.sub.6 represents hydrogen, alkyl [optionally substituted by one or more of the following: hydroxy, halo or an amino group of formula --NR.sub.12 R.sub.13 ], a C.sub.3-12 alicyclic hydrocarbon group, phenyl, (cycloalkyl)alkyl or benzyl; R.sub.7 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl, carboxy, or alkoxy; R.sub.8 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl or alkoxy; and R.sub.9 represents hydrogen or alkyl; which are antirheumatic agents. Compositions containing these compounds and processes to make them are also disclosed.
    • PCT No.PCT / EP92 / 02901 Sec。 371日期:1994年6月3日 102(e)日期1994年6月3日PCT提交1992年10月12日PCT公布。 公开号WO93 / 13097 本发明涉及式I化合物及其药学上可接受的盐类,羟基,羧基烯基,烷氧基碳烯基,羟基烷基,羧基烷基,烷氧基羰基烷基,烷氧基,卤代烷基,羧基烷氧基羰基或烷酰基氨基; R2代表氢,卤素,烷氧基,羟基,烷酰氧基或苯氧基; R3表示氢或烷基; R4代表氢,卤素,烷氧基羰基,苄氧基羰基,烷酰基,苯甲酰基,氨基甲酰基,烷基,羧基,羟烷基或烷硫基。 R5代表氢或烷基; R 6表示氢,任选被一个或多个下列基团取代的烷基:羟基,卤素或式-NR 12 R 13的氨基],C 3-12脂环族烃基,苯基,(环烷基)烷基或苄基; R7表示氢,卤素,三氟甲基,三氟甲氧基,烷基,羧基或烷氧基; R8代表氢,卤素,三氟甲基,三氟甲氧基,烷基或烷氧基; 和R9代表氢或烷基; 它们是抗风湿剂。 还公开了含有这些化合物的组合物和制备它们的方法。