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1. 发明授权

US4486597A Method for the production of nuclear substituted cinnamoylanthranilic acid derivatives 失效
标题翻译：制备核取代肉桂酰邻氨基苯甲酸衍生物的方法
公开(公告)号：US4486597A
公开(公告)日：1984-12-04
申请号：US577758
申请日：1984-02-07
申请人： Kinji Iizuka , Tetsuhide Kamino , Ryoji Yamamoto , Hiromu Harada
发明人： Kinji Iizuka , Tetsuhide Kamino , Ryoji Yamamoto , Hiromu Harada
IPC分类号： C07C231/00 , C07C231/12 , C07C235/38 , C07D295/02 , C07D295/027 , C07C99/00
CPC分类号： C07D295/027
摘要： The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3,4-dimethoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of piperidine to provide an intermediate salt precipitate, and the salt is treated with an acidic reagent to yield N-(3,4-dimethoxycinnamoyl)anthranilic acid product.
摘要翻译：本发明提供了制备核取代肉桂酰邻氨基苯甲酸化合物的改进方法。该方法的实例是在哌啶存在下，在惰性溶剂介质中3,4-二甲氧基苯甲醛与2-羧基丙二酸的反应，得到中间体盐沉淀物，盐用酸性试剂处理，得到N-（3 ，4-二甲氧基肉桂酰基）邻氨基苯甲酸产物。

2. 发明授权

US4623724A Method for the production of nuclear substituted cinnamoylanthranilic acid salts 失效
标题翻译：制备核取代肉桂酰邻氨基苯甲酸盐的方法
公开(公告)号：US4623724A
公开(公告)日：1986-11-18
申请号：US640588
申请日：1984-08-14
申请人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
发明人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
IPC分类号： C07C231/00 , C07C231/12 , C07C235/38 , C07D295/02 , C07D295/027 , C07D295/00
CPC分类号： C07D295/027
摘要： The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3,4-dimethoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of piperidine to provide an intermediate salt precipitate, and the salt is treated with an acidic reagent to yield N-(3,4-dimethoxycinnamoyl)anthranilic acid product.

3. 发明授权

US4587356A Process for the production of nuclear substituted cinnamoylanthranilic acid derivatives 失效
标题翻译：制备核取代肉桂酰邻氨基苯甲酸衍生物的方法
公开(公告)号：US4587356A
公开(公告)日：1986-05-06
申请号：US654231
申请日：1984-09-25
申请人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
发明人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
IPC分类号： C07D295/02 , C07D295/027 , C07C99/00
CPC分类号： C07D295/027
摘要： The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.
摘要翻译：本发明提供了制备核取代肉桂酰邻氨基苯甲酸化合物的改进方法。该方法的实例是在惰性溶剂介质中，在摩尔过量的哌啶存在下，3-羟基-4-甲氧基苯甲醛与2-羧基丙二酸的反应，得到高纯度的中间盐沉淀物，盐用酸性试剂洗脱N-（3-羟基-4-甲氧基肉桂酰）邻氨基苯甲酸产物。

4. 发明授权

US4469865A 1,3-Disubstituted imidazoles 失效
标题翻译： 1,3-二取代的咪唑
公开(公告)号：US4469865A
公开(公告)日：1984-09-04
申请号：US423332
申请日：1982-09-24
申请人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
发明人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
IPC分类号： C07D233/60 , C07D233/61 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： 1,3-Disubstituted imidazoles of the general formula (I): ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, Y is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or an dialkoxymethyl group having 3 to 13 carbon atoms, Z is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, n is zero or 1. The said compounds are intermediates for producing the imidazole derivatives of the general formula (V) above which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutical agents for treatment of diseases caused by thromboxane A.sub.2.
摘要翻译：通式（I）的1,3-二取代咪唑：其中A和B可以相同或不同，并且各自是具有1至8个碳的直链或支链亚烷基或亚烯基原子，Y为碳原子数2〜10的酰基，碳原子数2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基，Z为氰基或碳原子数为2〜7的烷氧基羰基， X是卤素原子，n是0或1.所述化合物是用于生产上述通式（V）的咪唑衍生物的中间体，其具有对凝血恶烷合成酶的强和特异性抑制作用，因此可用作治疗药物血栓素A2引起的疾病。

5. 发明授权

US4461905A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4461905A
公开(公告)日：1984-07-24
申请号：US413204
申请日：1982-08-30
申请人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
发明人： Kinji Iizuka , Tetsuhide Kamijo , Ryoji Yamamoto , Hiromu Harada
IPC分类号： C07D233/54 , C07D233/60 , C07D521/00
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The imidazole derivatives of the general formula: ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, D is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or a dialkoxymethyl group having 3 to 13 carbon atoms, Q is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, Z is ##STR2## (wherein E is a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms, Y is an oxygen atom or a sulfur atom and may be connected with either A or B), n is zero or 1, with the proviso that n is 1 when Y connects with B.These compounds are novel compounds and are useful as intermediates in producing 1-substituted imidazole derivatives which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutically active agents for treatment of diseases caused by thromboxane A.sub.2.
摘要翻译：具有以下通式的咪唑衍生物：其中A和B可以相同或不同，并且各自是具有1至8个碳原子的直链或支链亚烷基或亚烯基，D是具有2个碳原子数为2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基，Q为氰基或碳原子数2〜7的烷氧基羰基，X为卤素原子，Z为< IMAGE>（其中E是氢原子，卤素原子，具有1至6个碳原子的烷基或具有1至6个碳原子的烷氧基，Y是氧原子或硫原子，并且可以与A 或B），n为0或1，条件是当Y与B连接时n为1。这些化合物是新化合物，可用作生产1-取代咪唑衍生物的中间体，其具有对凝血恶烷合成酶的强和特异性抑制作用因此可用作治疗活性剂治疗由血栓素A2引起的疾病。

6. 发明授权

US4711958A Morpholine containing amino acid derivatives 失效
标题翻译：含有氨基酸衍生物的吗啉
公开(公告)号：US4711958A
公开(公告)日：1987-12-08
申请号：US32693
申请日：1987-04-01
申请人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
发明人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
IPC分类号： C07D233/54 , C07D233/64 , C07D295/18
CPC分类号： C07D233/64 , Y10S530/86
摘要： Amino acid derivatives represented by formula ##STR1## wherein His represents an L-histidyl group, X represents a straight or branched alkoxy group having 1 to 7 carbon atoms, a straight or branched alkylamino group having 1 to 7 carbon atoms, a cycloalkyloxy group having 3 to 7 carbon atoms, a morpholino group, said alkoxy group having one or more halogen atoms as substituents; or a pharmaceutically acceptable salt, are useful in the treatment of hypertension.
摘要翻译：由式表示的氨基酸衍生物，其中His表示L-组氨酰基，X表示碳原子数为1〜7的直链或支链烷氧基，碳原子数1〜7的直链或支链烷基氨基，环烷氧基， 3至7个碳原子，吗啉代基，所述烷氧基具有一个或多个卤素原子作为取代基; 或药学上可接受的盐可用于治疗高血压。

7. 发明授权

US4841067A Novel amino acid derivatives 失效
标题翻译：新型氨基酸衍生物
公开(公告)号：US4841067A
公开(公告)日：1989-06-20
申请号：US233962
申请日：1988-08-19
申请人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
发明人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
IPC分类号： C07C55/30 , C07D233/54 , C07D233/64 , C07D303/36
CPC分类号： C07D233/64 , C07C55/30 , C07D303/36 , Y10S530/86
摘要： Novel amino acid derivatives useful as a therapeutic agent are disclosed. These amino acid derivatives and the pharmaceutically acceptable salts thereof have a human renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.
摘要翻译：公开了可用作治疗剂的新型氨基酸衍生物。这些氨基酸衍生物及其药学上可接受的盐在口服给药时具有人肾素抑制作用，可用于治疗高血压，特别是肾素相关性高血压。

8. 发明授权

US4870183A Novel amino acid derivatives 失效
标题翻译：新型氨基酸衍生物
公开(公告)号：US4870183A
公开(公告)日：1989-09-26
申请号：US267612
申请日：1988-11-02
申请人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
发明人： Kinji Iizuka , Tetsuhide Kamijo , Tetsuhiro Kubota , Kenji Akahane , Hideaki Umeyama , Yoshiaki Kiso
IPC分类号： A61K31/415 , A61P9/12 , A61P43/00 , C07D233/54 , C07D233/64 , C07D401/14 , C07D405/14
CPC分类号： C07D233/64 , C07D401/14 , C07D405/14 , Y10S530/86
摘要： Novel amino acid derivatives useful as a therapeutic agent are disclosed. These amino acid derivatives and the pharmaceutically acceptable salts thereof have a human renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.

9. 再颁专利

USRE32944E Aromatic carboxylic amide derivatives 失效
标题翻译：芳香族羧酰胺衍生物
公开(公告)号：USRE32944E
公开(公告)日：1989-06-06
申请号：US802486
申请日：1977-06-01
申请人： Kozaburo Harita , Yukiyoshi Ajisawa , Kinji Iizuka , Yukihiko Kinoshita , Tetsuhide Kamijo , Michihiro Kobayashi
发明人： Kozaburo Harita , Yukiyoshi Ajisawa , Kinji Iizuka , Yukihiko Kinoshita , Tetsuhide Kamijo , Michihiro Kobayashi
IPC分类号： C07C233/33 , A61K31/195 , A61P37/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/55 , C07C235/38 , C07D317/60
CPC分类号： A61K31/195 , C07C233/12
摘要： Novel aromatic carboxylic amides of the general formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is a hydrogen atom or an alkyl group having 1-4 carbon atoms, R.sub.3 and R.sub.4 are hydrogen atoms or together form another chemical bond, each X is a hydroxyl group, a halogen atom, an alkyl group having 1-4 carbon atoms and an alkoxy group containing 1-4 carbon atoms, and n is an integer of 1-3 with the proviso that when .[.Xs.]. .Iadd.X's .Iaddend.are alkyl or alkoxy groups, they may be connected together to form a ring, as well as pharmaceutically acceptable salts thereof.These compounds possess a strong antiallergenic action and are thus useful for treatment of asthma, hay fever, .[.anticaria.]. .Iadd.urticaria .Iaddend.and atopic dermatitis.The above aromatic carboxylic amides can be prepared by reacting a reactive functional derivative of the general formula: ##STR2## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the same meanings given above, with an aminobenzoic acid of the formula: ##STR3## and, if desired, converting the resulting amide into the corresponding salts.

10. 发明授权

US4320134A Inhibiton of thromboxane synthetase with 1-substituted imidazole compounds 失效
标题翻译：用1-取代咪唑化合物抑制血栓素合成酶
公开(公告)号：US4320134A
公开(公告)日：1982-03-16
申请号：US14001
申请日：1979-02-21
申请人： Kinji Iizuka , Kenji Akahane , Yukio Kamijo , Denichi Momose , Yukiyoshi Ajisawa
发明人： Kinji Iizuka , Kenji Akahane , Yukio Kamijo , Denichi Momose , Yukiyoshi Ajisawa
IPC分类号： C07D233/56 , C07D233/60 , C07D521/00 , A61K31/415
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , Y10S514/822 , Y10S514/826
摘要： The imidazole compounds of the general formula (I): ##STR1## wherein Y is a carboxyl group, a hydroxymethyl group, an N-di or -mono alkyl substituted or unsubstituted carbamoyl group, a cyano group, or an N-di or -mono alkyl substituted or unsubstituted aminomethyl group, and n is an integer of 3 to 20; and pharmaceutically acceptable salts thereof. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.
摘要翻译：通式（I）的咪唑化合物：其中Y是羧基，羟甲基，N-二或一烷基取代或未取代的氨基甲酰基，氰基或N- 二或一烷基取代或未取代的氨基甲基，n为3至20的整数; 及其药学上可接受的盐。这些化合物对来自兔血小板微粒体的血栓素合成酶具有强烈的抑制作用，并且可用作炎症，高血压，血栓，脑中风和哮喘的治疗活性剂。

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