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1. 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。

2. 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。

3. 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。

4. 发明授权

US4766120A Tetrazole derivatives, having a further unsaturated heterocyclic ring anti-ulcer composition containing the same and method for treating ulcers 失效
标题翻译：具有另外的含有其的不饱和杂环抗溃疡组合物的四氮唑衍生物和治疗溃疡的方法
公开(公告)号：US4766120A
公开(公告)日：1988-08-23
申请号：US868595
申请日：1986-05-30
申请人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
发明人： Minoru Uchida , Takao Nishi , Kazuyuki Nakagawa
IPC分类号： C07D257/04 , A61K31/41 , A61K31/535 , C07D413/06
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 or 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 compositon 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是任选的限定取代基，或者R 3或R 4可以与它们所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

US4435404A Carbostyril derivatives 失效
公开(公告)号：US4435404A
公开(公告)日：1984-03-06
申请号：US261177
申请日：1981-04-30
申请人： Takao Nishi , Tatsuyoshi Tanaka , Kazuyuki Nakagawa
发明人： Takao Nishi , Tatsuyoshi Tanaka , Kazuyuki Nakagawa
IPC分类号： A61K31/47 , A61K31/4704 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P29/00 , A61P43/00 , C07D213/38 , C07D215/06 , C07D215/22 , C07D215/227 , C07D309/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D215/227 , C07D213/38 , C07D215/22 , C07D309/04 , Y10S514/826 , Y10S514/926 , Y10S514/927
摘要： Novel carbostyril derivative and its salt represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a phenyl-lower alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## wherein A is a lower alkylene group; R.sup.3 is a lower alkyl group, a hydroxy lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or a benzoyloxy-lower alkyl group; and R.sup.4 is a C.sub.3-10 -cycloalkyl group which may have at least one hydroxyl group as the substituent(s) in the cycloalkyl ring, a C.sub.3-10 -cycloalkyl-lower alkyl group, a phenyl group, a phenyl-lower alkyl group which may have at least one lower alkoxy group as the substituent(s) in the phenyl ring, a lower alkyl group which may have at least one hydroxyl group as the substituent(s), a heterocyclic ring residue or a lower alkyl group having one heterocyclic ring residue as the substituent; further, R.sup.3, R.sup.4 and the adjacent nitrogen atom, as well as with or without another nitrogen atom, may form a group of the formula ##STR3## (wherein R.sup.5 is a phenyl group, a C.sub.3-10 -cycloalkyl group or a phenyl-lower alkyl group; and B is a methine group or a nitrogen atom); the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single or double bond; the substituted position of the group of the formula ##STR4## is any one of 5-, 6-, 7- or 8-position in the carbostyril skeleton; when the group of the formula ##STR5## is substituted at 5-, 6-, 7- or 8-position in the carbostyril skeleton, then R.sup.2 is a hydrogen atom or a lower alkyl group; alternatively, when R.sup.2 is a group of the formula ##STR6## then 5-, 6-, 7- and 8-positions in the carbostyril skeleton are hydrogen atoms and are not substituted with groups of the formula ##STR7## and when R.sup.3 is a lower alkyl group, then R.sup.4 should be neither of a C.sub.3-10 -cycloalkyl group, a C.sub.3-10 -cycloalkyl-lower alkyl group nor a lower alkyl group, having effects for preventing and treating thrombosis and embolism.

6. 发明授权

US4298739A Novel carbostyril derivatives 失效
标题翻译：新型喹诺酮衍生物
公开(公告)号：US4298739A
公开(公告)日：1981-11-03
申请号：US142057
申请日：1980-04-21
申请人： Takao Nishi , Hiraki Ueda , Kazuyuki Nakagawa
发明人： Takao Nishi , Hiraki Ueda , Kazuyuki Nakagawa
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26 , A61K31/47
CPC分类号： C07D215/227 , C07D215/26
摘要： Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, phenyl-C.sub.1-4 alkyl-; R.sup.2 is hydrogen, a halogen atom, hydroxy, phenyl-C.sub.1-4 alkoxy; R.sup.3 is hydrogen, hydroxy, C.sub.1-4 alkyl; R.sup.4 is C.sub.3-8 cycloalkyl, substituted or unsubstituted phenyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R.sup.5 is hydrogen, C.sub.1-8 alkyl, C.sub.2-4 alkenyl, phenyl, C.sub.3-8 cycloalkyl, phenyl-C.sub.1-4 alkyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond.
摘要翻译：具有血小板聚集抑制作用，抗炎作用，抗溃疡作用，血管扩张作用和磷酸二酯酶抑制作用的新型喹诺酮衍生物，可用于预防或治疗血栓，动脉硬化，高血压，哮喘等疾病，并且还可用作抗炎或抗溃疡其中R 1为氢，C 1-4烷基，C 2-4链烯基，苯基-C 1-4烷基 - ; R2是氢，卤素原子，羟基，苯基-C 1-4烷氧基; R3是氢，羟基，C1-4烷基; R4是C3-8环烷基，取代或未取代的苯基，C3-8环烷基-C1-4烷基，2-（3,4-二甲氧基苯基） - 乙基，R5是氢，C1-8烷基，C2-4烯基，苯基， C 3-8环烷基，苯基-C 1-4烷基，C 3-8环烷基-C 1-4烷基，m是1-3的整数，l和n可以相同或不同，分别为0或整数1 -7和n和n的总和不超过7，在喹诺酮骨架中3-和4-位的碳 - 碳键是单键或双键。

7. 发明授权

US4277479A Tetrazolylalkoxycarbostyril derivatives and pharmaceutical compositions containing them 失效
标题翻译：四唑基烷氧基吡啶三唑衍生物和含有它们的药物组合物
公开(公告)号：US4277479A
公开(公告)日：1981-07-07
申请号：US70710
申请日：1979-08-29
申请人： Takao Nishi , Kazuyuki Nakagawa
发明人： Takao Nishi , Kazuyuki Nakagawa
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/4725 , A61P1/04 , A61P7/02 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P25/28 , A61P29/00 , A61P43/00 , C07D257/04 , C07D403/12 , C12N9/99
CPC分类号： C07D257/04 , Y10S514/826
摘要： Novel tetrazolylalkoxycarbostyril derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a low alkenyl group, a lower alkanoyl group, a benzoyl group or phenylalkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## R.sup.3 is a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, a phenyl group or a phenylalkyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is either single or double bond; and the substituted position of a group of the formula, ##STR3## in the carbostyril skeleton is either 4-, 5-, 6-, 7- or 8-position provided that the only one such group of the formula can be substituted in the whole carbostyril skeleton, thus when R.sup.2 in 4-position is a group of the formula ##STR4## then 5-, 6-, 7- or 8-position will have no such substituted group; furthermore, the phenyl group in the above-mentioned benzoyl group, phenylalkyl group or phenyl group may have substituted group(s).The above-mentioned novel tetrazolylalkoxycarbostyril derivatives have pharmacological activities such as platelet aggregation inhibitory action, antiinflammatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful as anti-thrombosis agent, cerebral blood flow improving agent, antiinflammatory agent, antiulcer agent, anti-hypertensive agent and anti-asthmatic agent.
摘要翻译：式（I）的新型四唑基烷氧基吡咯烷腈衍生物：其中R 1为氢原子，低级烷基，低级烯基，低级烷酰基，苯甲酰基或苯基烷基; R2是氢原子，低级烷基或下式的基团R3是低级烷基，环烷基，环烷基烷基，苯基或苯基烷基; A是低级亚烷基; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键; 并且喹诺酮骨架中的一组式（）的取代位置是4-，5-，6-，7-或8-位，条件是式中唯一一个可以在因此当4-位上的R2是式“IMAGE”的基团时，则5-，6-，7-或8-位将不具有这样的取代基; 此外，上述苯甲酰基中的苯基，苯基烷基或苯基可以具有取代基。上述新型四唑基烷氧基吡咯烷腈衍生物具有药物活性，例如血小板聚集抑制作用，抗炎作用，抗溃疡作用，血管扩张作用和磷酸二酯酶抑制作用，可用作抗血栓形成剂，脑血流量改善剂，抗炎剂，抗溃疡剂，抗高血压药和抗哮喘药。

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. 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。

10. 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。

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