公开(公告)号：US5073553A

公开(公告)日：1991-12-17

申请号：US440069

申请日：1989-11-22

申请人： Tetsuhide Kamijo ,  Arao Ujiie ,  Naoyuki Tsutsumi ,  Atsushi Tsubaki

发明人： Tetsuhide Kamijo ,  Arao Ujiie ,  Naoyuki Tsutsumi ,  Atsushi Tsubaki

IPC分类号： C07D491/04 ,  C07D491/048

CPC分类号： C07D491/04

摘要： Benzofuro[3,2-c]quinoline compounds of the formula: ##STR1## wherein A represents a group of the formula of --CH.sub.2) .sub.m or --CH.sub.2 CH(OH)CH.sub.2 --; Y represents an N,N-di-alkylamino group, an N-mono-alkylamino group or a nitrogen atom-containing aliphatic geterocyclic group; n represents 0 or 1; m represents an integer of from 1 to 3, and pharmaceutically acceptable acid addition salts thereof, possess a strong inhibitory action on bone resorption, a stimulatory effect on ossification.

公开(公告)号：US5023261A

公开(公告)日：1991-06-11

申请号：US321248

申请日：1989-03-09

申请人： Tetsuhide Kamijo ,  Arao Ujiie ,  Hiromu Harada ,  Naoyuki Tsutsumi ,  Atsushi Tsubaki ,  Toshiaki Yamaguchi ,  Hideo Nagata

发明人： Tetsuhide Kamijo ,  Arao Ujiie ,  Hiromu Harada ,  Naoyuki Tsutsumi ,  Atsushi Tsubaki ,  Toshiaki Yamaguchi ,  Hideo Nagata

IPC分类号： A61K31/435 ,  A61K31/47 ,  A61P19/10 ,  A61P43/00 ,  C07D491/04 ,  C07D491/048

CPC分类号： C07D491/04

摘要： Benzofuro[3,2-c]quinoline compounds of the general formula: ##STR1## wherein (1) each of R.sup.1 and R.sup.2 is the same, and represent a group of the formula of --OR.sup.3 in which R.sup.3 represents a carbamoyl group, an N-mono-alkylcarbamoyl group, an N,N-dialkylcarbamoyl group, an alkylsulfonyl group, a formyl group or an aliphatic acyl group which may have an alkoxycarbonyl group as a substituent; m represents zero, 1 or 2; n represents zero or 1; with the proviso that n is not zero when m is zero,(2) each of R.sup.1 and R.sup.2 is different, and represent a hydroxy group or an N,N-di-alkylcarbamoyloxy group; m represents 1 or 2; n represents 1, possess a strong inhibitory action on bone resorption and a stimulatory effect on ossification. Some benzofuro[3,2-c]quinoline compounds of the above general formula also possess a stimulatory effect on longitudinal bone growth, and thus are useful for the prevention or treatment of osteoporosis.

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.

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.

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。

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。

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。

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.

公开(公告)号：US4863904A

公开(公告)日：1989-09-05

申请号：US789597

申请日：1985-10-21

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： C07C51/487 ,  C07C57/38 ,  C07C57/40 ,  C07C59/66 ,  C07C59/68 ,  C07C65/34 ,  C07D209/18 ,  C07D233/54 ,  C07K5/078

CPC分类号： C07D233/64 ,  C07C51/487 ,  C07C57/38 ,  C07C57/40 ,  C07C59/66 ,  C07C59/68 ,  C07C65/34 ,  C07D209/18 ,  C07K5/06147 ,  Y10S530/86

摘要： Dipeptides are described which are represented by the formula ##STR1## wherein the various substituents are defined hereinbelow. These compounds have a strong inhibitory efect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin-associated hypertension.

摘要翻译： 描述了由式（IMAGE）表示的二肽，其中各种取代基如下所定义。 这些化合物对人肾素具有强烈的抑制作用，可用作治疗高血压，特别是肾素相关性高血压的治疗活性剂。

公开(公告)号：US4656269A

公开(公告)日：1987-04-07

申请号：US852260

申请日：1986-04-15

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 ,  C07D413/12

CPC分类号： C07D233/64 ,  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。