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1. 发明授权

US4283408A Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them 失效
标题翻译：胍基噻唑化合物，制备方法和含有它们的胃抑制组合物
公开(公告)号：US4283408A
公开(公告)日：1981-08-11
申请号：US107629
申请日：1979-12-27
申请人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61P1/00 , A61P1/04 , A61P43/00 , C07D277/40 , C07D277/48 , C07D277/38
CPC分类号： C07D277/48 , C07D277/40
摘要： Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
摘要翻译：新型的胍基噻唑化合物，其通式为：其中R表示氢原子或低级烷基，R1表示氨基，低级烷基，卤代低级烷基，取代或未取代的芳基，单 - 或二 - 低级烷基氨基，芳基氨基或芳烷基氨基，R 2表示氢原子，低级烷基，低级烯基或低级炔基，Y表示硫原子或亚甲基，m和n 各自表示1-3的整数，其药理学上可接受的酸加成盐可用作胃酸分泌抑制剂。

2. 发明授权

US4727082A Dihydropyridine compounds and pharmaceutical compositions containing them 失效
标题翻译：二氢吡啶化合物和含有它们的药物组合物
公开(公告)号：US4727082A
公开(公告)日：1988-02-23
申请号：US908350
申请日：1986-09-17
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
IPC分类号： C07D211/82 , A61K31/44 , A61K31/455 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/28 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07C317/00 , C07C323/00 , C07D211/90
摘要： A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.CH--), or a ethynylene group (--C.dbd.C--); B represents a single bond or --CH.sub. 2 O--; and m and n, which are the same or different, each represents 0 or an integer of 1 to 5.The compounds are useful for the treatment of various cardiovascular disorders, since they possess both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities.
摘要翻译：下列通式（I）的二氢吡啶化合物或其盐：其中R 1和R 2相同或不同，各自表示C1至C10烷基，低级烷基其被氧原子或被C3-C6脂环族基团取代的低级烷基取代; R 3和R 4相同或不同，各自表示低级烷基; R 5和R 6相同或不同，分别表示氢原子，硝基，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基或低级烷基亚磺酰基 ; R 7和R 8相同或不同，各自表示氢原子，卤素原子，氰基，低级烷氧基或低级烷酰氨基，或者可以与R 8结合形成萘基，相邻苯基; A表示单键，亚乙烯基（-CH = CH-）或亚乙炔基（-C = C-）; B表示单键或-CH 2 O-; 和m和n相同或不同，各自表示0或1至5的整数。该化合物可用于治疗各种心血管疾病，因为它们具有Ca 2+拮抗剂和肾上腺素能β受体阻断活性。

3. 发明授权

US4186200A Novel fused derivatives of 2-pyridones 失效
标题翻译： 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
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

4. 发明授权

US4251533A Nitrogen-containing heterocyclic compounds 失效
标题翻译：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
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。

5. 发明授权

US4198512A 1-Oxo-1,2-dihydroisoquinoline derivatives 失效
标题翻译： 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
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。

6. 发明授权

US4335129A Thiazolo[3,2-6]isoquinolines, compositions and use thereof 失效
标题翻译：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
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。

7. 发明授权

US4163844A Nitrogen-containing heterocyclic compounds 失效
标题翻译：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
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。

8. 发明授权

US4288438A Nitrogen-containing heterocyclic ring derivatives and analgesic and anti-inflammatory compositions and methods employing them 失效
标题翻译：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
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。

9. 发明授权

US4284778A Nitrogen-containing heterocyclic ring derivatives 失效
标题翻译：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
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。

10. 发明授权

US4329455A 1,3-Oxazino(3,2-b)isoquinoline-6-ones 失效
标题翻译： 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
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。

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