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    • 4. 发明授权
    • 3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and
derivatives, their preparations and medicines containing them
    • 3,4-二氢-4-氧代-3-(2-丙烯基)-1-酞嗪乙酸及其衍生物,其制剂和含有它们的药物
    • US5489592A
    • 1996-02-06
    • US211427
    • 1994-06-20
    • Francois CollongesHerve DumasPhilippe DurbinDaniel Guerrier
    • Francois CollongesHerve DumasPhilippe DurbinDaniel Guerrier
    • A61K31/50A61P3/08A61P13/02A61P15/00A61P25/02A61P27/02A61P27/12A61P43/00C07C17/00C07C17/14C07C17/16C07C17/26C07C17/38C07C22/04C07C22/08C07C25/02C07C25/13C07C25/24C07C45/44C07C45/56C07D237/32C07D241/44C07D333/12C07D409/06
    • C07D409/06C07C17/00C07C17/14C07C17/16C07C17/2635C07C17/38C07C22/04C07C22/08C07C25/02C07C25/24C07C45/44C07C45/565C07D237/32C07D333/12
    • Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) ##STR1## in which R.sub.1 R.sub.2 and R.sub.3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R.sub.4 residue such as defined below, except when R.sub.4 is H; R.sub.4 and R.sub.5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R.sub.4 and R.sub.5 do not simultaneously denote H; R.sub.6 stands for hydroxy or alkoxy radical; R.sub.7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by analiphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R.sub.8 or a cyano group; n is equal to 0,1 or 2; R.sub.8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. This invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.
    • PCT No.PCT / FR92 / 00920 Sec。 371日期:1994年6月20日 102(e)日期1994年6月20日PCT提交1992年10月2日PCT公布。 公开号WO93 / 07109 日期1994年4月15日。新型3,4-二氢-4-氧代-3(丙-2-烯基)-1-对乙酰乙酸及式(I)的衍生物其中R1R2和R3相同 或不同的,代表H,卤素或直链或支链的脂肪族,饱和或不饱和基团,除非是R4是H,而是被至少一个卤素或R4残基取代或不被定义如下。 R 4和R 5相同或不同,代表H,直链或支链脂族基团,饱和或不饱和的芳基或杂芳基,所述基团被至少一个基团取代,例如氟,氯,溴,甲基 或三氟甲基,其中R 4和R 5不同时表示H; R6代表羟基或烷氧基; R7代表H,卤素,直链或支链脂族饱和或不饱和基团,烷氧基,所述基团被脂肪族或卤代基团取代,或不被取代或未取代的氨基取代或未取代的氨基S(O)n R8或氰基; n等于0,1或2; R 8是脂族,直链或支链基团,芳基或杂芳基,氨基,所述基团被脂肪族或卤代基取代。 本发明还涉及所述酸及其药学上可接受的碱加成盐的任选互变异构形式。 还描述了制备所述化合物和含有它们的药物的方法。