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公开(公告)号:EP0507534A1
公开(公告)日:1992-10-07
申请号:EP92302786.6
申请日:1992-03-30
发明人: Sato, Fumiyasu , Tsubaki, Atsushi , Hokari, Hiroshi , Tanaka, Nobuyuki , Saito, Masaru, Kissei Dai-san Seiyuryo , Akahane, Kenji , Kobayashi, Michihiro
IPC分类号: C07D209/08 , C07D209/44 , C07D217/06 , C07D409/06 , A61K31/395
CPC分类号: C07D409/06 , C07D209/08 , C07D209/44 , C07D217/06
摘要: Succinic acid compounds of the formula:
wherein A represents a heterocyclic group, a 3 to 8-membered cycloalkyl group or a phenyl group which may have one or more substituents selected from the group of a halogen atom, a lower alkyl group having 1 to 6 carbon atoms and a lower alkoxy group having 1 to 6 carbon atoms; B represents a bicyclic amino group which may have 1 or 2 unsaturated bonds, with the proviso that B bonds to the carbon atom of the carbonyl group at the nitrogen atom; R represents a hydrogen atom or combines each other to form a chemical bond; R 1 represents a hydrogen atom, a lower alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 10 carbon atoms; when there is an asymmetric carbon atom, enantiomers thereof and racemic mixtures thereof; when there are geometrical isomers, each geometrical isomer, E-isomers thereof, Z-isomers thereof, cis-isomers thereof and trans-isomers thereof; and pharmaceutically acceptable salts thereof, enhance insulin secretion and possess a hypoglycemic activity, and are thus useful for the treatment of diabetes.摘要翻译: 具有下式的琥珀酸化合物:其中A表示杂环基,3至8元环烷基或苯基,其可以具有一个或多个选自以下的取代基:卤素原子,具有 1至6个碳原子和1至6个碳原子的低级烷氧基; B表示可以具有1或2个不饱和键的双环氨基,条件是B与氮原子上的羰基的碳原子键合; R表示氢原子或彼此结合形成化学键; R 1表示氢原子,碳原子数1〜6的低级烷基或碳原子数7〜10的芳烷基。 当存在不对称碳原子时,其对映异构体和其外消旋混合物; 当存在几何异构体时,每种几何异构体,其异构体,其Z-异构体,其顺式异构体和其反式异构体; 和其药学上可接受的盐,增强胰岛素分泌并具有降血糖活性,因此可用于治疗糖尿病。
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公开(公告)号:EP0507534B1
公开(公告)日:1996-02-28
申请号:EP92302786.6
申请日:1992-03-30
发明人: Sato, Fumiyasu , Tsubaki, Atsushi , Hokari, Hiroshi , Tanaka, Nobuyuki , Saito, Masaru, Kissei Dai-san Seiyuryo , Akahane, Kenji , Kobayashi, Michihiro
IPC分类号: C07D209/08 , C07D209/44 , C07D217/06 , C07D409/06 , A61K31/395
CPC分类号: C07D409/06 , C07D209/08 , C07D209/44 , C07D217/06
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公开(公告)号:EP0244083A3
公开(公告)日:1989-11-15
申请号:EP87302613.2
申请日:1987-03-26
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07D233/64 , A61K31/415
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.
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公开(公告)号:EP0190891A3
公开(公告)日:1988-04-20
申请号:EP86300666
申请日:1986-01-31
发明人: Iizuka, Kinji , Kubota, Tetsuhiro , Kamijo, Tetsuhide , Umeyama, Hideaki , Akahane, Kenji , Kiso, Yoshiaki
IPC分类号: C07D233/64 , A61K31/415
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.
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公开(公告)号:EP0206807A3
公开(公告)日:1988-01-20
申请号:EP86304849
申请日:1986-06-24
发明人: Iizuka, Kinji , Kubota, Tetsuhiro , Umeyama, Hideaki , Kamijo, Tetsuhide , Akahane, Kenji , Kiso, Yoshiaki
IPC分类号: C07D233/61 , C07D403/06 , A61K31/415
CPC分类号: C07D233/64 , C07D403/12 , Y10S530/86
摘要: Novel amino acid derivatives useful as a therapeutic agent are disclosed. The amino acid derivatives have a 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。 氨基酸衍生物口服给药时具有肾素抑制作用,可用于治疗高血压,特别是与肾素相关的高血压。
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公开(公告)号:EP0252727A1
公开(公告)日:1988-01-13
申请号:EP87306015.6
申请日:1987-07-08
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07D233/64 , C07D401/14
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.
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可药用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。
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公开(公告)号:EP0216539A2
公开(公告)日:1987-04-01
申请号:EP86306751.8
申请日:1986-09-02
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07D295/18 , C07D207/16 , C07D209/20 , C07C103/50
CPC分类号: C07D295/185 , C07D207/16 , C07D209/20
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.
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公开(公告)号:EP0181110A2
公开(公告)日:1986-05-14
申请号:EP85307555.4
申请日:1985-10-18
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07K5/06 , C07D233/64 , C07D403/02 , A61K37/02 , A61K31/415
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
wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof.
These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.-
公开(公告)号:EP0216539A3
公开(公告)日:1988-10-26
申请号:EP86306751
申请日:1986-09-02
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07D295/18 , C07D207/16 , C07D209/20 , C07C103/50 , A61K31/16 , A61K31/535 , A61K31/40
CPC分类号: C07D295/185 , C07D207/16 , C07D209/20
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,尤其是肾素相关性高血压。
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公开(公告)号:EP0181110A3
公开(公告)日:1988-05-11
申请号:EP85307555
申请日:1985-10-18
发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
IPC分类号: C07K05/06 , C07D233/64 , C07D403/02 , A61K37/02 , A61K31/415
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
wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof. These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.
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