Substituted benzoate derivatives
    3.
    发明授权
    Substituted benzoate derivatives 失效
    取代苯甲酸酯衍生物

    公开(公告)号:US5473096A

    公开(公告)日:1995-12-05

    申请号:US93953

    申请日:1993-07-21

    摘要: The present invention relates to the compounds of the formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, hydroxy, acyloxy, or halogen; R.sup.9 is hydrogen, hydroxy, acyloxy, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, or lower alkylamino which is optionally substituted; E.sup.1 is hydrogen, or an ester residue; m is an integer of from 1 to 4;or a pharmaceutically acceptable salt thereof. The compounds of the present invention exhibit phospholipase A.sub.2 inhibitory activity, and can be used in treating inflammatory conditions.

    摘要翻译: 本发明涉及下式的化合物:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8独立地为氢,任选取代的低级烷基,任选取代的低级烷氧基, 羟基,酰氧基或卤素; R9是氢,羟基,酰氧基,任选被取代的低级烷基,任选被取代的低级烷氧基或任选被取代的低级烷基氨基; E1是氢或酯残基; m为1〜4的整数, 或其药学上可接受的盐。 本发明化合物表现出磷脂酶A2抑制活性,可用于治疗炎性病症。

    Triazolo-4,1-benzoxazepines having CNS activity
    6.
    发明授权
    Triazolo-4,1-benzoxazepines having CNS activity 失效
    具有中枢神经系统活性的三氮唑-4,1-苯并氧氮杂

    公开(公告)号:US4476133A

    公开(公告)日:1984-10-09

    申请号:US397855

    申请日:1982-07-13

    CPC分类号: C07D267/14

    摘要: 4,1-Benzoxazepines of the following formula are novel central nervous system: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl;X is hydrogen, halogen, or nitro;Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl)

    摘要翻译: 下式的4,1-苯并氧氮杂是新的中枢神经系统:其中R是氢或C1至C5烷基; X是氢,卤素或硝基; Y是苯基,2-卤代苯基,4-卤代苯基,2-三氟甲基苯基或吡啶基; 并且是下列基团:其中Q是氧,硫或亚肼基,条件是当Y是苯基或2-卤代苯基且R是氢时,Q是 氧还不硫; R1是氢,卤素,C1至C5烷基,C1至C5烷硫基,5-或6-元杂环或被选自卤素,羟基,巯基,C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基,C 1至C 5烷硫基,C 7至C 9芳烷基二硫代,C 2至C 10二烷基氨基,C 3至C 15二烷基氨基烷氧基,C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时,Y

    4,1-Benzoxazepines and compositions
    10.
    发明授权
    4,1-Benzoxazepines and compositions 失效
    4,1-苯并氧氮杂和组合物

    公开(公告)号:US4374842A

    公开(公告)日:1983-02-22

    申请号:US250299

    申请日:1981-04-02

    CPC分类号: C07D267/14

    摘要: 4,1-Benzoxazepines of the following formula are central nervous system drugs: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl).

    摘要翻译: 下式的4,1-苯并氧氮杂是中枢神经系统药物:其中R是氢或C1至C5烷基; X是氢,卤素或硝基; Y是苯基,2-卤代苯基,4-卤代苯基,2-三氟甲基苯基或吡啶基; 并且是下列基团:其中Q是氧,硫或亚肼基,条件是当Y是苯基或2-卤代苯基且R是氢时,Q是 氧还不硫; R1是氢,卤素,C1至C5烷基,C1至C5烷硫基,5-或6-元杂环或被选自卤素,羟基,巯基,C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基,C 1至C 5烷硫基,C 7至C 9芳烷基二硫代,C 2至C 10二烷基氨基,C 3至C 15二烷基氨基烷氧基,C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 并且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时,Y不为苯基或2-卤代苯基)。