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    • 1. 发明授权
    • Anti-oxidative tricyclic, condensed heterocyclic compound
    • 抗氧化三环,稠合杂环化合物
    • US5734067A
    • 1998-03-31
    • US809001
    • 1997-03-04
    • Shuji JinnoYasuyo KogureHiroyuki OnukiTakaaki Okita
    • Shuji JinnoYasuyo KogureHiroyuki OnukiTakaaki Okita
    • C07D313/14C07D337/14C07D493/04
    • C07D493/04C07D313/14C07D337/14
    • Providing a novel tricyclic, condensed heterocyclic compound having an anti-oxidative action and being promising for use in pharmaceutical agents, cosmetics, chemical products and the like. By chemical synthesis, a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula: ##STR1## (wherein X--Y represents CH.sub.2 --C.dbd.O, CH.sub.2 --CH.sub.2 or CH.dbd.CH; Z represents O, S, or S.dbd.O; R.sub.1 to R.sub.8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF.sub.3 ; and at least two of R.sub.1 to R.sub.4 are hydroxyl groups); and the salts thereof are provided. The compound has an anti-oxidative activity at the same degree as or higher than the activity of .alpha.-tocopherol, so the compound is promising as a therapeutic drug for a variety of diseases, such as cancer, arteriosclerosis, or liver diseases, in which it is believed that biological lipid peroxides may be involved.
    • PCT No.PCT / JP95 / 01975 Sec。 371日期1997年3月4日 102(e)1997年3月4日PCT PCT 1995年9月28日PCT公布。 WO96 / 10021 PCT出版物 日期1996年4月4日提供具有抗氧化作用的新型三环稠合杂环化合物,并且有希望用于药剂,化妆品,化学产品等。 通过化学合成,由下式表示的新型抗氧化三环稠合杂环化合物:其中XY表示CH 2 -C = O,CH 2 -CH 2或CH = CH; Z表示O,S或S = O; R 1〜R 8分别独立地表示选自氢原子,羟基,卤素基,低级烷基,低级烷氧基,低级烷基酮基和CF 3的化合物; R 1〜 R4为羟基); 并提供其盐。 该化合物具有与α-生育酚活性相同或更高的抗氧化活性,因此该化合物作为各种疾病如癌症,动脉硬化或肝脏疾病的治疗药物是有希望的,其中 相信可能涉及生物脂质过氧化物。
    • 2. 发明授权
    • Tracheal smooth muscle relaxant
    • 气管平滑肌松弛剂
    • US06180659B2
    • 2001-01-30
    • US09101842
    • 1998-08-31
    • Shinya YamashitaJiro TakeoShuji JinnoYasuyo KogureHiroyuki OnukiTakaaki OkitaJunichiro HataYasuhiro FukudaNaomi Ohtsuka
    • Shinya YamashitaJiro TakeoShuji JinnoYasuyo KogureHiroyuki OnukiTakaaki OkitaJunichiro HataYasuhiro FukudaNaomi Ohtsuka
    • A61K3138
    • C07D337/14A61K31/352A61K31/382C07D313/14Y10S514/826
    • The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient. [In the formula, X and Y each is any group selected from a group consisting of CH2, CHW1 (where W1 is halogen atom, hydroxyl group or lower alkoxy group) and C═O when the bond of X and Y is a single bond while, when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW2 (where W2 is lower alkyl group or lower alkylcarbonyl group); Z is O, S, S═O or SO2; and R1˜R8 each is selected from a group consisting of hydrogen atom, VR9 (where V is O, S, S═O or SO2; and R9 is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl group].
    • 本发明提供含有下述式(1)表示的化合物或其药理学上可接受的盐作为有效成分的气管平滑肌松弛剂。[式中,X和Y各自为选自CH 2, CHW1(其中W1为卤原子,羟基或低级烷氧基),当X和Y的键为单键时为C = O,而当为双键时,X和Y各自为选自 由CH和COW 2组成(其中W2是低级烷基或低级烷基羰基); Z是O,S,S = O或SO 2; R1〜R8各自选自氢原子,VR9(其中V为O,S,S = O或SO2; R9为氢原子,低级烷基,羟基低级烷基,低级酰基,三卤甲基 羧基低级烷基,羟基低级烷基,羟基低级烯基,羟基低级炔基,卤素原子,低级烷基,低级烷基酮,三卤代甲基,三甲基甲硅烷基乙炔基,硝基,氨基, N-羰基低级烷基,低级烷基苯基和苯基]。