公开(公告)号：US4335129A

公开(公告)日：1982-06-15

申请号：US229183

申请日：1981-01-28

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

IPC分类号： C07D217/24 ,  C07D497/04 ,  C07D513/04 ,  C07D513/14 ,  A61K31/47

CPC分类号： C07D497/04 ,  C07D217/24 ,  C07D513/04 ,  C07D513/14 ,  Y10S514/916 ,  Y10S514/96 ,  Y10S514/962

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。

公开(公告)号：US4163844A

公开(公告)日：1979-08-07

申请号：US861980

申请日：1977-12-19

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

IPC分类号： C07D217/24 ,  C07D497/04 ,  C07D513/04 ,  C07D513/14 ,  C07D279/08

CPC分类号： C07D497/04 ,  C07D217/24 ,  C07D513/04 ,  C07D513/14 ,  Y10S514/916 ,  Y10S514/96 ,  Y10S514/962

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。

公开(公告)号：US4329455A

公开(公告)日：1982-05-11

申请号：US224968

申请日：1981-01-14

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

IPC分类号： C07D217/24 ,  C07D497/04 ,  C07D513/04 ,  C07D513/14 ,  C07D498/04

CPC分类号： C07D497/04 ,  C07D217/24 ,  C07D513/04 ,  C07D513/14 ,  Y10S514/916 ,  Y10S514/96 ,  Y10S514/962

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。

公开(公告)号：US4636516A

公开(公告)日：1987-01-13

申请号：US347982

申请日：1982-02-11

申请人： Kazuo Kubo ,  Yasuo Isomura ,  Shuichi Sakamoto ,  Hiroshige Homma

发明人： Kazuo Kubo ,  Yasuo Isomura ,  Shuichi Sakamoto ,  Hiroshige Homma

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/66 ,  C07D233/70 ,  C07D233/84 ,  C07D263/32 ,  C07D277/22 ,  C07D277/24 ,  C07D277/36 ,  C07D277/42 ,  C07D513/04 ,  C07D513/06 ,  C07D233/42 ,  A61K31/415 ,  A61K31/425

CPC分类号： C07D233/64 ,  C07D233/70 ,  C07D233/84 ,  C07D263/32 ,  C07D277/24 ,  C07D277/36 ,  C07D277/42 ,  C07D513/04 ,  C07D513/06

摘要： Novel 3,5-di-tert-butyl-4-hydroxyphenyl-substituted heterocyclic compounds shown by the formula ##STR1## wherein .circle.Het -- represents a specific heterocyclic group and the salts thereof.The compounds have an anti-inflammatory, an anti-pyretic, an analgesic, an anti-arthritic, and an immunoregulatory activity. Hence, they are particularly useful as an antirheumatics.

摘要翻译： 新颖的3,5-二叔丁基-4-羟基苯基取代的杂环化合物，其由式表示，其中＆cir＆Het-表示特定的杂环基团及其盐。 该化合物具有抗炎，抗热解，止痛，抗关节炎和免疫调节活性。 因此，它们作为抗风湿剂特别有用。

公开(公告)号：US4288438A

公开(公告)日：1981-09-08

申请号：US68073

申请日：1979-08-20

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/505

CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

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。

公开(公告)号：US4284778A

公开(公告)日：1981-08-18

申请号：US68172

申请日：1979-08-20

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

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。

公开(公告)号：US4186200A

公开(公告)日：1980-01-29

申请号：US876517

申请日：1978-02-09

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/415

CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

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

公开(公告)号：US4251533A

公开(公告)日：1981-02-17

申请号：US67918

申请日：1979-08-20

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/435 ,  C07D471/02

CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

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。

公开(公告)号：US4198512A

公开(公告)日：1980-04-15

申请号：US925217

申请日：1978-07-17

申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P25/04 ,  A61P29/00 ,  C07D217/24

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。