Novel fused derivatives of 2-pyridones
    2.
    发明授权
    Novel fused derivatives of 2-pyridones 失效
    2-吡啶酮的新型融合衍生物

    公开(公告)号:US4186200A

    公开(公告)日:1980-01-29

    申请号:US876517

    申请日:1978-02-09

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4##when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, and the pharmacologically acceptable non-toxic salts thereof. The compounds described above are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,R 1和R 2中的一个表示低级烷基,苯基,卤代苯基或低级烷氧基苯基,另一方表示氢原子,低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子,低级烷基,苯基或苯基低级烷基; X表示氧原子,硫原子,亚氨基或由下式表示的基团,其中m表示1或2,R4表示低级烷基,羟基低级烷基,环烷基或苯基低级烷基 组; Y表示可以被低级烷基,三亚甲基,四亚甲基,可被低级烷基取代的亚乙烯基取代的亚乙基,或者R5表示氢原子的低级烷基 基,三氟甲基或苯基; 说X是所示的组

    Nitrogen-containing heterocyclic compounds
    3.
    发明授权
    Nitrogen-containing heterocyclic compounds 失效
    含氮杂环化合物

    公开(公告)号:US4251533A

    公开(公告)日:1981-02-17

    申请号:US67918

    申请日:1979-08-20

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4## when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, 1/7and the pharmacologically acceptable non-toxic salts thereof.The compounds described above are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,R 1和R 2中的一个表示低级烷基,苯基,卤代苯基或低级烷氧基苯基,另一方表示氢原子,低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子,低级烷基,苯基或苯基低级烷基; X表示氧原子,硫原子,亚氨基或由下式表示的基团,其中m表示1或2,R4表示低级烷基,羟基低级烷基,环烷基或苯基低级烷基 组; Y表示可以被低级烷基,三亚甲基,四亚甲基,可被低级烷基取代的亚乙烯基取代的亚乙基,或者R5表示氢原子的低级烷基 基,三氟甲基或苯基; 当所述R 1和R 2中的一个为低级烷基且另一个为氢原子,所述Y为亚乙基时,X为所示的基团,其药理学上可接受的无毒性盐 。 上述化合物是强镇痛抗炎剂。

    Nitrogen-containing heterocyclic ring derivatives and analgesic and
anti-inflammatory compositions and methods employing them
    4.
    发明授权
    Nitrogen-containing heterocyclic ring derivatives and analgesic and anti-inflammatory compositions and methods employing them 失效
    含氮杂环衍生物和使用它们的镇痛和抗炎组合物和方法

    公开(公告)号:US4288438A

    公开(公告)日:1981-09-08

    申请号:US68073

    申请日:1979-08-20

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## (wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group); and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group); said X is the group shown by ##STR4## when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, and the pharmacologically acceptable non-toxic salts thereof.The compounds described above are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,R 1和R 2中的一个表示低级烷基,苯基,卤代苯基或低级烷氧基苯基,另一方表示氢原子,低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子,低级烷基,苯基或苯基低级烷基; X表示氧原子,硫原子,亚氨基或由下式表示的基团(其中m表示1或2,R4表示低级烷基,羟基低级烷基,环烷基或苯基低级 烷基); Y表示可以被低级烷基,三亚甲基,四亚甲基,可被低级烷基取代的亚乙烯基取代的亚乙基或其中R5表示氢原子,低级烷基 烷基,三氟甲基或苯基); 当所述R 1和R 2中的一个为低级烷基且另一个为氢原子且所述Y为亚乙基时,所述X为所示的基团及其药学上可接受的无毒盐。 上述化合物是强镇痛抗炎剂。

    Nitrogen-containing heterocyclic ring derivatives
    5.
    发明授权
    Nitrogen-containing heterocyclic ring derivatives 失效
    含氮杂环衍生物

    公开(公告)号:US4284778A

    公开(公告)日:1981-08-18

    申请号:US68172

    申请日:1979-08-20

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by a lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4## when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, and the pharmacologically acceptable non-toxic salts thereof. The compound described above are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,R 1和R 2中的一个表示低级烷基,苯基,卤代苯基或低级烷氧基苯基,另一方表示氢原子,低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子,低级烷基,苯基或苯基低级烷基; X表示氧原子,硫原子,亚氨基或由下式表示的基团,其中m表示1或2,R4表示低级烷基,羟基低级烷基,环烷基或苯基低级烷基 组; Y表示可以被低级烷基,三亚甲基,四亚甲基,可被低级烷基取代的亚乙烯基取代的亚乙基,或者R5表示氢原子的低级烷基 基,三氟甲基或苯基; 当所述R 1和R 2中的一个为低级烷基且另一个为氢原子且所述Y为亚乙基时,所述X为所示的基团及其药学上可接受的无毒盐。 上述化合物是强镇痛抗炎剂。

    1-Oxo-1,2-dihydroisoquinoline derivatives
    6.
    发明授权
    1-Oxo-1,2-dihydroisoquinoline derivatives 失效
    1-氧代-1,2-二氢异喹啉衍生物

    公开(公告)号:US4198512A

    公开(公告)日:1980-04-15

    申请号:US925217

    申请日:1978-07-17

    CPC分类号: C07D217/24

    摘要: Novel 1-oxo-1,2-dihydroisoquinoline compounds of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a phenyl lower alkyl group; R.sub.2 represents a lower alkyl group; R.sub.3 represents a hydrogen atom, a lower alkanoyl group, a lower alkyl group or a hydroxy lower alkyl group; and n is 0, 1 or 2 and the pharmacologically acceptable non-toxic salts thereof.The compounds of this invention are strong analgesic anti-inflammatory agents.

    摘要翻译: 新颖的式Ⅰ-1-氧代-1,2-二氢异喹啉化合物,其中R1代表低级烷基或苯基低级烷基; R2表示低级烷基; R3表示氢原子,低级烷酰基,低级烷基或羟基低级烷基; 和n为0,1或2及其药理学上可接受的无毒盐。 本发明的化合物是强镇痛抗炎剂。

    1,3-Oxazino(3,2-b)isoquinoline-6-ones
    7.
    发明授权
    1,3-Oxazino(3,2-b)isoquinoline-6-ones 失效
    1,3-二氮杂双环(3,2-b)异喹啉-6-酮

    公开(公告)号:US4329455A

    公开(公告)日:1982-05-11

    申请号:US224968

    申请日:1981-01-14

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.7 represents a hydrogen atom, a halogen atom, a lower alkanoyl group, a phenyl group, a phenyl lower alkyl group, a lower alkyl group, a hydroxy lower alkyl group, a di lower alkylamino lower alkyl group, a pyrrolidino lower alkyl group, a piperidino lower alkyl group, a morpholino lower alkyl group, or a 4-lower alkylpiperazino lower alkyl group;(1) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are hydrogen atom and n is 0, said Y is a group shown by ##STR3## and (2) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are hydrogen atom, at least one of said R.sub.5 and R.sub.6 is the aforesaid group other than hydrogen atom, and n is 0, said Y is oxygen atom or a group shown by ##STR4## and the pharmacologically acceptable non-toxic salts thereof. The compounds are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,Y表示氧原子,硫原子,或者由下式表示的基团(式中,m为1或2)表示的新型含氮杂环化合物。 n表示0或1; R 1和R 4可以相同或不同,各自表示氢原子,低级烷基或低级烯基; R2和R3可以相同或不同,分别表示氢原子,羟基,低级烷酰氧基,低级烷基或低级烯基; 所述R2和R3可进一步形成双键; R 5和R 6可以相同或不同,分别表示氢原子,卤素原子,羟基,硝基,氨基,低级烷氧基,单或二低级烷基氨基或低级 烷基; 所述R 5和R 6可以进一步形成低级亚烷基二氧基; R7表示氢原子,卤素原子,低级烷酰基,苯基,苯基低级烷基,低级烷基,羟基低级烷基,二低级烷基氨基低级烷基,吡咯烷子基低级烷基 哌啶子基低级烷基,吗啉代低级烷基或4-低级烷基哌嗪基低级烷基; (1)当所述R 1,R 2,R 3,R 4,R 5,R 6和R 7为氢原子并且n为0时,所述Y为通过表示的基团和(2)当所述R 1,R 2,R 3,R 4和 R 7为氢原子,所述R 5和R 6中的至少一个为除氢原子以外的上述基团,n为0,Y为氧原子或由其表示的基团及其药理学上可接受的无毒盐。 这些化合物是强镇痛消炎药。

    Thiazolo[3,2-6]isoquinolines, compositions and use thereof
    8.
    发明授权
    Thiazolo[3,2-6]isoquinolines, compositions and use thereof 失效
    噻唑并[3,2-6]异喹啉,组合物及其用途

    公开(公告)号:US4335129A

    公开(公告)日:1982-06-15

    申请号:US229183

    申请日:1981-01-28

    摘要: Nitrogen containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl groups, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents by hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.7 represents a hydrogen atom, a halogen atom, a lower alkanoyl group, a phenyl group, a phenyl lower alkyl group, a lower alkyl group, a hydroxy lower alkyl group, a di lower alkylamino lower alkyl group, a pyrrolidino lower alkyl group, a piperidino lower alkyl group, a morpholino lower alkyl group, or a 4-lower alkylpiperazino lower alkyl group;(1) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are hydrogen atom and n is O, said Y is a group shown by ##STR3## and (2) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are hydrogen atom, at least one of said R.sub.5 and R.sub.6 is the aforesaid group other than hydrogen atom, and n is O, said Y is oxygen atom or a group shown by ##STR4## and the pharmacologically acceptable non-toxic salts thereof.

    摘要翻译: 式中,Y表示氧原子,硫原子,或由下式表示的基团(式中,m为1或2)表示的含氮杂环化合物。 n表示0或1; R 1和R 4可以相同或不同,各自表示氢原子,低级烷基或低级烯基; R2和R3可以相同或不同,分别表示氢原子,羟基,低级烷酰氧基,低级烷基或低级烯基; 所述R2和R3可进一步形成双键; R 5和R 6可以相同或不同,各自表示氢原子,卤素原子,羟基,硝基,氨基,低级烷氧基,一或二低级烷基氨基或低级 烷基; 所述R 5和R 6可以进一步形成低级亚烷基二氧基; R7表示氢原子,卤素原子,低级烷酰基,苯基,苯基低级烷基,低级烷基,羟基低级烷基,二低级烷基氨基低级烷基,吡咯烷子基低级烷基 哌啶子基低级烷基,吗啉代低级烷基或4-低级烷基哌嗪基低级烷基; (1)当所述R 1,R 2,R 3,R 4,R 5,R 6和R 7为氢原子并且n为O时,所述Y为通过表示的基团和(2)当所述R 1,R 2,R 3,R 4和 R7是氢原子,R5和R6中的至少一个是除氢原子以外的上述基团,n是O,Y是氧原子或由其表示的基团及其药理学上可接受的无毒盐。

    Nitrogen-containing heterocyclic compounds
    9.
    发明授权
    Nitrogen-containing heterocyclic compounds 失效
    含氮杂环化合物

    公开(公告)号:US4163844A

    公开(公告)日:1979-08-07

    申请号:US861980

    申请日:1977-12-19

    摘要: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.7 represents a hydrogen atom, a halogen atom, a lower alkanoyl group, a phenyl group, a phenyl lower alkyl group, a lower alkyl group, a hydroxy lower alkyl group, a di lower alkylamino lower alkyl group, a pyrrolidino lower alkyl group, a piperidino lower alkyl group, a morpholino lower alkyl group, or a 4-lower alkylpiperazino lower alkyl group;(1) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are hydrogen atom and n is 0, said Y is a group shown by ##STR3## and (2) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are hydrogen atom, at least one of said R.sub.5 and R.sub.6 is the aforesaid group other than hydrogen atom, and n is 0, said Y is oxygen atom or a group shown by ##STR4## and the pharmacologically acceptable non-toxic salts thereof. The compounds are strong analgesic anti-inflammatory agents.

    摘要翻译: 式中,Y表示氧原子,硫原子,或者由下式表示的基团(式中,m为1或2)表示的新型含氮杂环化合物。 n表示0或1; R 1和R 4可以相同或不同,各自表示氢原子,低级烷基或低级烯基; R2和R3可以相同或不同,分别表示氢原子,羟基,低级烷酰氧基,低级烷基或低级烯基; 所述R2和R3可进一步形成双键; R 5和R 6可以相同或不同,分别表示氢原子,卤素原子,羟基,硝基,氨基,低级烷氧基,单或二低级烷基氨基或低级 烷基; 所述R 5和R 6可以进一步形成低级亚烷基二氧基; R7表示氢原子,卤素原子,低级烷酰基,苯基,苯基低级烷基,低级烷基,羟基低级烷基,二低级烷基氨基低级烷基,吡咯烷子基低级烷基 哌啶子基低级烷基,吗啉代低级烷基或4-低级烷基哌嗪基低级烷基; (1)当R 1,R 2,R 3,R 4,R 5,R 6和R 7为氢原子并且n为0时,所述Y为通过表示的基团,(2)当所述R 1,R 2,R 3,R 4和 R 7为氢原子,所述R 5和R 6中的至少一个为除氢原子以外的上述基团,n为0,Y为氧原子或由其表示的基团及其药理学上可接受的无毒盐。