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1. 发明授权

US4072683A 3,4-Dihydrocarbostyril derivatives 失效
标题翻译： 3,4-二氢喹诺酮衍生物
公开(公告)号：US4072683A
公开(公告)日：1978-02-07
申请号：US630631
申请日：1975-11-10
申请人： Kazuyuki Nakagawa , Minoru Uchida , Hiroaki Oka
发明人： Kazuyuki Nakagawa , Minoru Uchida , Hiroaki Oka
IPC分类号： C07D215/26 , C07D215/22 , A61K31/47
CPC分类号： C07D215/26
摘要： Novel (3'-alkylamino-2'-hydroxy)propoxy-3,4-dihydrocarbostyril derivatives having .beta.-adrenergic nerves blocking activity and hypotensive activity and useful as a remedy for angina pectoris, irregular pulse and hypertension, etc., represented by the formula, ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or aralkyl and R.sub.2 is C.sub.1 -C.sub.4 alkyl, are prepared by reacting a 3,4-dihydrocarbostyril derivative represented by the formula, ##STR2## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl or aralkyl, with an epihalogenohydrin represented by the formula, ##STR3## wherein X is halogen, reacting the resulting product with an alkylamine represented by the formula,R.sub.2 -- NH.sub.2wherein R.sub.2 is as defined above, and, if necessary, reducing the resulting product.
摘要翻译：具有β-肾上腺素能神经阻断活性和降血压活性的新型（3'-烷基氨基-2'-羟基）丙氧基-3,4-二氢喹诺酮衍生物，可用作心绞痛，不规则脉搏和高血压等的补救剂，由其中R 1是氢，C 1 -C 4烷基或芳烷基，R 2是C 1 -C 4烷基的式，其中R 1是C 1 -C 4烷基，其由下式表示的3,4-二氢喹诺酮衍生物，或芳烷基，与下式表示的表卤代醇，其中X是卤素，使得到的产物与由式R2-NH2表示的烷基胺反应，其中R2如上所定义，如果需要，还原所得的产物。

2. 发明授权

US4216220A Platelet aggregation inhibiting 2-oxyindoles, their compositions and method of use 失效
标题翻译：抑制2-羟基吲哚的血小板聚集体，其组成和使用方法
公开(公告)号：US4216220A
公开(公告)日：1980-08-05
申请号：US806926
申请日：1977-06-15
申请人： Kazuyuki Nakagawa , Minoru Uchida , Kimiaki Oka
发明人： Kazuyuki Nakagawa , Minoru Uchida , Kimiaki Oka
IPC分类号： C07D209/34 , C07D215/22 , C07D215/227 , C07D215/26 , C07D209/04
CPC分类号： C07D215/227 , C07D209/34 , C07D215/26 , Y10S514/822
摘要： 2-Oxyindole derivatives represented by the following general formula: ##STR1## where R.sub.1 is selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, benzyl and phenethyl; A is --CH.dbd.CH-- or ##STR2## wherein R.sub.2 or R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1-4 alkyl; R.sub.4 is --OR.sub.5, wherein R.sub.5 is selected from the group consisting of hydrogen, C.sub.1-8 alkyl, cyclohexyl, benzyl and phenethyl, or ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m+n being no more than 11. The 2-oxyindole derivatives have excellent effects on the inhibition of platelet aggregation.
摘要翻译：由下列通式表示的2-氧吲哚衍生物：其中R 1选自氢，C 1-4烷基，C 2-4链烯基，苄基和苯乙基; A是-CH = CH-或其中R 2或R 3可以相同或不同，并且选自氢和C 1-4烷基; R 4是-OR 5，其中R 5选自氢，C 1-8烷基，环己基，苄基和苯乙基，或其中R 6和R 7可以相同或不同，并且选自氢，C 1-4烷基，苄基，苯乙基和氮原子一起选自哌啶子基，吗啉代，哌嗪基或噻唑基的杂环基; m和n各自为零或m + n不大于11的正整数。2-氧吲哚衍生物对抑制血小板聚集具有优异的效果。

3. 再颁专利

USRE34722E Quinoline amino acid derivatives of carbostyril compounds 失效
标题翻译：喹诺酮类喹诺酮类氨基酸衍生物
公开(公告)号：USRE34722E
公开(公告)日：1994-09-06
申请号：US937382
申请日：1992-08-31
申请人： Minoru Uchida , Makoto Komastu , Kazuyuki Nakagawa
发明人： Minoru Uchida , Makoto Komastu , Kazuyuki Nakagawa
IPC分类号： C07C205/57 , C07D209/38 , C07D215/18 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/12 , A61K31/47
CPC分类号： C07D215/227 , C07C205/57 , C07D209/38 , C07D215/18 , C07D215/26 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/12
摘要： Disclosed are carbostyril derivatives and their salts of the formulas ##STR1## The compounds have anti-peptic ulcer effects, and are useful as a treating agent for curing peptic ulcers in the digestive system, such as ulcers in the stomach and in the duodenum. The compounds particularly have prophylaxis and curing effects for treating chronic ulcers, for example experimental acetic acid-induced ulcers and cautery ulcers, with both low toxicity and few side-effects. Also disclosed are processes for preparing the compounds and for preparing pharmaceutical compositions containing them.
摘要翻译：公开了喹诺酮衍生物及其下式的盐。该化合物具有抗消化性溃疡作用，并且可用作治疗消化系统中消化性溃疡的治疗剂，例如胃和十二指肠溃疡。所述化合物特别具有用于治疗慢性溃疡的预防和治疗效果，例如实验性乙酸诱导的溃疡和烧灼性溃疡，具有低毒性和少量副作用。还公开了制备化合物和制备含有它们的药物组合物的方法。

4. 发明授权

US4540703A Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers 失效
标题翻译：四唑衍生物，含有其的抗溃疡组合物和治疗溃疡的方法
公开(公告)号：US4540703A
公开(公告)日：1985-09-10
申请号：US333806
申请日：1981-12-23
申请人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
发明人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
IPC分类号： C07D295/14 , A61K31/395 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P1/04 , A61P7/02 , A61P29/00 , C07D257/04 , A61K31/41
CPC分类号： C07D257/04
摘要： Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio; l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.
摘要翻译：下式的四唑衍生物：其中R 1是任选的限定取代基; A是硫或低级亚烷基 - 硫基; l为0或1; B是低级亚烷基; R 2是羟基，低级烷氧基或基团：其中R 3和R 4是任选的定义的取代基，或者R 3和R 4可以与它们连接的氮原子一起形成定义的杂环基，和其药学上可接受的盐具有针对消化性溃疡和/或十二指肠溃疡以及抗炎活性的预防或治疗活性，并且可用作抗溃疡或抗炎药物; 制备四唑衍生物的方法; 和含有所述四唑衍生物的药物组合物。

5. 发明授权

US4372953A Tetrazole derivatives, and anti-ulcer composition containing the same 失效
标题翻译：四唑衍生物和含有其的抗溃疡组合物
公开(公告)号：US4372953A
公开(公告)日：1983-02-08
申请号：US239044
申请日：1981-02-27
申请人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
发明人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
IPC分类号： A61K31/41 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , C07C45/00 , C07C45/46 , C07C49/327 , C07C49/84 , C07D207/32 , C07D207/333 , C07D213/50 , C07D213/70 , C07D213/71 , C07D215/22 , C07D215/227 , C07D257/04 , C07D257/06 , C07D271/10 , C07D271/113 , C07D285/12 , C07D285/135 , C07D307/46 , C07D307/68 , C07D333/22 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D401/06 , C07D401/14
CPC分类号： C07D207/333 , C07C45/004 , C07C45/46 , C07C49/327 , C07C49/84 , C07D213/50 , C07D213/70 , C07D213/71 , C07D215/227 , C07D257/04 , C07D257/06 , C07D271/113 , C07D285/135 , C07D307/46 , C07D307/68 , C07D333/22
摘要： Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkykl, phenyl or a group of the formula: --S(O).sub.l --A--(X).sub.m --R.sup.3, and R.sup.2 is hydrogen, a lower alkyl, phenyl or a cycloalkyl when R.sup.1 is the group --S(O).sub.l --A--(X).sub.m --R.sup.3, or R.sup.2 is a group of the formula: --B--CO--R.sup.4 when R.sup.1 is a lower alkyl or phenyl and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and are useful as an anti-ulcer drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.
摘要翻译：具有下式的四唑衍生物：其中R1是低级烷基，苯基或下式的基团-S（O）1A-（X）m -R 3，并且R 2是氢，低级烷基，当R 1是基团-S（O）1 A（X）m -R 3时，或R 2是下式的基团，当R 1是低级烷基或苯基时，R 2是下式的基团：其具有针对消化性溃疡和/或十二指肠溃疡的预防或治疗活性，并且可用作抗溃疡药物; 制备四唑衍生物的方法; 和含有所述四唑衍生物的药物组合物。

6. 发明授权

US4694017A 2-amido 3(oxindol-3-yl)propionic acids having antiulcer activity 失效
标题翻译：具有抗溃疡活性的2-酰氨基3（羟吲哚-3-基）丙酸
公开(公告)号：US4694017A
公开(公告)日：1987-09-15
申请号：US610574
申请日：1984-05-15
申请人： Minoru Uchida , Makoto Komatsu , Kazuyuki Nakagawa
发明人： Minoru Uchida , Makoto Komatsu , Kazuyuki Nakagawa
IPC分类号： C07D209/20 , C07D209/34 , A61K31/405
CPC分类号： C07D209/34 , C07D209/20
摘要： Novel oxindole derivative and salt thereof represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group; R.sup.2 is a hydrogen atom or a lower alkyl group; R.sup.3 is a hydrogen atom, a cycloalkylcarbonyl group, a benzoyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group on the phenyl ring, or a phenyl-lower alkanoyl group which may have halogen atoms as the substituents on the phenyl ring; provided that when R.sup.4 is a hydrogen atom, then R.sup.3 should be neither a hydrogen atom nor a lower alkyl group.The novel oxindole derivative and salt thereof possesses anti-peptic ulcer effects and are useful as anti-peptic ulcer agents.
摘要翻译：其中R1为氢原子，低级烷基，低级烯基，低级炔基或苯基 - 低级烷基的通式为的新型羟基吲哚衍生物及其盐。 R2是氢原子或低级烷基; R3是氢原子，环烷基羰基，可以具有1〜3个选自苯基环上的卤素原子，低级烷基和低级烷氧基的取代基的苯甲酰基，或苯基 - 低级烷酰基可以具有卤素原子作为苯环上的取代基的基团; 条件是当R 4为氢原子时，R 3既不是氢原子也不是低级烷基。新羟吲哚衍生物及其盐具有抗消化性溃疡作用，可用作抗消化性溃疡药。

7. 发明授权

US4578381A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US4578381A
公开(公告)日：1986-03-25
申请号：US510241
申请日：1983-07-01
申请人： Minoru Uchida , Makoto Komastu , Kazuyuki Nakagawa
发明人： Minoru Uchida , Makoto Komastu , Kazuyuki Nakagawa
IPC分类号： C07C205/57 , C07D209/38 , C07D215/18 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/12 , A61K31/47
CPC分类号： C07D215/227 , C07C205/57 , C07D209/38 , C07D215/18 , C07D215/26 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/12
摘要： Disclosed are carbostyril derivatives and their salts of the formulas ##STR1## The compounds have anti-peptic ulcer effects, and are useful as a treating agent for curing peptic ulcers in the digestive system, such as ulcers in the stomach and in the duodenum. The compounds particularly have prophylaxis and curing effects for treating chronic ulcers, for example experimental acetic acid-induced ulcers and cautery ulcers, with both low toxicity and few side-effects. Also disclosed are processes for preparing the compounds and for preparing pharmaceutical compositions containing them.
摘要翻译：公开了喹诺酮衍生物及其下式的盐。该化合物具有抗消化性溃疡作用，并且可用作治疗消化系统中消化性溃疡的治疗剂，例如胃和十二指肠溃疡。所述化合物特别具有用于治疗慢性溃疡的预防和治疗效果，例如实验性乙酸诱导的溃疡和烧灼性溃疡，具有低毒性和少量副作用。还公开了制备化合物和制备含有它们的药物组合物的方法。

8. 发明授权

US4738970A Benzimidazolyl-thio-tetrahydroquinolines and anti-peptic ulcer compositions containing the same 失效
标题翻译：苯并咪唑基 - 硫代四氢喹啉和含有它们的抗消化性溃疡组合物
公开(公告)号：US4738970A
公开(公告)日：1988-04-19
申请号：US62429
申请日：1987-06-16
申请人： Minoru Uchida , Seiji Morita , Masatoshi Chihiro , Kazuyuki Nakagawa
发明人： Minoru Uchida , Seiji Morita , Masatoshi Chihiro , Kazuyuki Nakagawa
IPC分类号： C07D213/80 , C07D215/04 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/60 , C07D401/12 , C07D471/04 , A61K31/415 , A61K31/47 , C07D215/36 , C07D235/04
CPC分类号： C07D213/80 , C07D215/04 , C07D215/233 , C07D215/26 , C07D215/60 , C07D401/12 , C07D471/04
摘要： Novel tetrahydroquinoline derivatives and salts thereof and novel imidazopyridine derivatives and salts thereof, both having excellent anti-peptic ulcer activities, and are useful as treating agents for peptic ulcers such as gastric ulcer, duodenum ulcer and the like.
摘要翻译：新颖的四氢喹啉衍生物及其盐以及新颖的咪唑并吡啶衍生物及其盐均具有优异的消化性溃疡活性，可用作胃溃疡，十二指肠溃疡等消化性溃疡的治疗剂。

9. 发明授权

US4663323A Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers 失效
标题翻译：四唑衍生物，含有其的抗溃疡组合物和治疗溃疡的方法
公开(公告)号：US4663323A
公开(公告)日：1987-05-05
申请号：US609333
申请日：1984-05-11
申请人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
发明人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
IPC分类号： C07D257/04 , A61K31/535 , C07D413/06 , C07D413/12
CPC分类号： C07D257/04
摘要： Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.
摘要翻译：下式的四唑衍生物：其中R 1是任选的限定取代基; A是硫或低级亚烷基 - 硫基，l是0或1; B是低级亚烷基; R 2是羟基，低级烷氧基或基团：其中R 3和R 4是任选的定义的取代基，或者R 3和R 4可以与它们连接的氮原子一起形成定义的杂环基，和其药学上可接受的盐具有针对消化性溃疡和/或十二指肠溃疡以及抗炎活性的预防或治疗活性，并且可用作抗溃疡或抗炎药物; 制备四唑衍生物的方法; 和含有所述四唑衍生物的药物组合物。

10. 发明授权

US4880815A Imidazopyridyl-alkylthio-pyridines and anti-peptic ulcer compositions containing the same 失效
标题翻译：咪唑并吡啶基 - 烷硫基 - 吡啶类和含有它们的抗消化性溃疡组合物
公开(公告)号：US4880815A
公开(公告)日：1989-11-14
申请号：US109207
申请日：1987-10-16
申请人： Minoru Uchida , Seiji Morita , Masatoshi Chihiro , Kazuyuki Nakagawa
发明人： Minoru Uchida , Seiji Morita , Masatoshi Chihiro , Kazuyuki Nakagawa
IPC分类号： C07D213/80 , C07D215/04 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/60 , C07D401/12 , C07D471/04
CPC分类号： C07D213/80 , C07D215/04 , C07D215/233 , C07D215/26 , C07D215/60 , C07D401/12 , C07D471/04
摘要： Novel tetrahydroquinoline derivatives and salts thereof and novel imidazopyridine derivatives and salts thereof, both having excellent anti-peptic ulcer activities, and are useful as treating agents for peptic ulcers such as gastric ulcer, duodenum ulcer and the like.

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