Benzopyrans, their production and pharmaceutical compositions containing them
    5.
    发明公开
    Benzopyrans, their production and pharmaceutical compositions containing them 失效
    Benzopyrane,ihre Herstellung und sie enthaltende pharmazeutische Zusammensetzungen。

    公开(公告)号:EP0042299A1

    公开(公告)日:1981-12-23

    申请号:EP81302700.0

    申请日:1981-06-16

    摘要: Benzopyrans represented by the formula
    wherein A represents a direct bond or -CH 2 O-

    R 1 represents a C 3 -C 5 alkyl group, a hydroxy-(C 3 -C 5 alkyl) group, a lower alkyl-amino-lower alkyl group, a ni- trato-(C 3 -C 5 alkyl) group or a phenyl-(C 1 -C 5 ) alkyl group where the phenyl may be substituted by a lower alkoxy group, R 2 represents hydrogen, halogen, OH, N0 2 , a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group or an acetyl group, R 3 represents hydrogen or N0 2 , B represents a direct bond, a C 1 -C 7 alkylene group, a -O-lower alkylene group or a -CONH-lower alkylene group, and
    n represents 1 or 2; and their acid addition salts are useful, for example, in reducing heart beat rate, myocardial oxygen consumption and blood pressure.

    摘要翻译: 苯并吡喃由下式表示:其中A表示直接键或-CH 2 O-,R 1表示C 3 -C 5烷基,羟基 - (C 3 -C 5烷基),低级烷基 - 氨基 - 低级烷基 ,硝基 - (C 3 -C 5烷基)基或苯基 - (C 1 -C 5)烷基,其中苯基可以被低级烷氧基取代,R 2表示氢,卤素,OH,NO 2,氨基甲酰基,低级 烷基,低级烷氧基,低级亚烷基氧基或乙酰基,R 3表示氢或NO 2,B表示直接键,C 1 -C 7亚烷基,-O-低级亚烷基或-CONH-低级亚烷基 组,... n表示1或2; 并且它们的酸加成盐可用于例如降低心跳率,心肌耗氧量和血压。

    Benzoylpiperazine esters and a process for their production
    10.
    发明公开
    Benzoylpiperazine esters and a process for their production 失效
    苯甲酰基哌嗪酮和维他芬

    公开(公告)号:EP0098713A2

    公开(公告)日:1984-01-18

    申请号:EP83303583.5

    申请日:1983-06-22

    摘要: Benzoylpiperazine esters and acid addition salts thereof are disclosed, which esters have the following formula:
    wherein A represents a single bond or an alkylene group, vinylene group, -O-alkylene group or methine group, R 1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenathrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isooxazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R 2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group; except the case where A is a single bond, R l is
    and R 2 is a methyl group. The esters exhibit excellent chymotrypsin inhibitive activity.

    摘要翻译: 公开了苯甲酰哌嗪酯及其酸加成盐,该酯具有下式:其中A表示单键或亚烷基,亚乙烯基,-O-亚烷基或次甲基,R 1表示双环碳 可以被低级烷基,低级烷氧基,氧代基或硝基或卤素原子取代的环状残基,或者可以是部分饱和的; 可含有氧代基的芴残基; 亚芴基; 蒽残基; 可以被低级烷基取代的或可以部分饱和的苯硫醇残基; 可以被低级烷基或低级烷氧基取代的苯并呋喃残基或硫杂残基; 可以被氧代基或苯基取代并部分饱和的苯并吡喃残基或苯并嗪残基; 邻苯二甲酰亚胺残基; 苯并二氮残基; 可以被低级烷基或苯基取代的异恶唑残基; 或亚烷基二氧基苯残基或呫吨残基; R2代表烷基,环烷基,环烷基烷基或芳烷基; 除了A是单键的情况,R1是... ...,R2是甲基。 该酯表现出优异的糜蛋白酶抑制活性。