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公开(公告)号:US4393228A
公开(公告)日:1983-07-12
申请号:US880180
申请日:1978-02-22
IPC分类号: C07D303/48 , C07D407/02 , C07D407/12 , C07D411/12
CPC分类号: C07D303/48
摘要: The epoxysuccinic acid derivatives of this invention are prepared by esterification of an epoxysuccinic acid or a halide thereof, by partial hydrolysis of an epoxysuccinic acid diester, by amidation of an epoxysuccinic acid monoester, or by hydrolysis of an epoxysuccinic acid amide monoester. These epoxysuccinic acid derivatives have excellent thiol protease inhibitory activity and anti-inflammatory activity without the acceleration of vascular permeability.
摘要翻译: 本发明的环氧琥珀酸衍生物通过环氧琥珀酸或其卤化物的酯化,环氧琥珀酸二酯的部分水解,环氧琥珀酸单酯的酰胺化,或通过环氧琥珀酸酰胺单酯的水解而制得。 这些环氧琥珀酸衍生物具有优异的硫醇蛋白酶抑制活性和抗炎活性,而不加速血管通透性。
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公开(公告)号:US4333879A
公开(公告)日:1982-06-08
申请号:US109410
申请日:1980-01-03
申请人: Masaharu Tamai , Takashi Adachi , Shigeo Morimoto , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
发明人: Masaharu Tamai , Takashi Adachi , Shigeo Morimoto , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
IPC分类号: C07D303/48 , A61K31/335 , A61K31/336 , A61K38/00 , A61P43/00 , C07K5/06 , C07K5/062 , C07K5/065 , C07K14/81 , C07C103/52 , C07D405/12
CPC分类号: C07K5/06078 , C07K5/06043 , A61K38/00
摘要: An epoxysuccinic acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, alkyl having 1-2 carbon atoms, cycloalkyl having 5-6 carbon atoms or benzyl, R.sup.2 is alkyl having 3-4 carbon atoms or benzyl, R.sup.3 is hydrogen or methyl, and R.sup.4 is alkyl having 1-10 carbon atoms, phenyl, benzyl, phenethyl or cycloalkyl having 3-6 carbon atoms or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached form a 5-6 membered heterocyclic ring, or said heterocyclic ring substituted with a protected carboxy.
摘要翻译: 其中R 1为氢,碱金属,具有1-2个碳原子的烷基,具有5-6个碳原子的环烷基或苄基,R2为具有3-4个碳原子的烷基或苄基,R3表示下式的环氧琥珀酸衍生物 氢或甲基,R4为具有1-10个碳原子的烷基,苯基,苄基,苯乙基或具有3-6个碳原子的环烷基或R3和R4与它们所连接的氮原子一起形成5-6元杂环 环或被保护的羧基取代的所述杂环。
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公开(公告)号:US4474800A
公开(公告)日:1984-10-02
申请号:US149312
申请日:1980-05-13
申请人: Masaharu Tamai , Shigeo Morimoto , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
发明人: Masaharu Tamai , Shigeo Morimoto , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
IPC分类号: C07D303/48 , A61K31/335
CPC分类号: C07D303/48
摘要: An epoxysuccinyl amino acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, benzyl or cycloalkyl having 5 to 6 carbon atoms, R.sup.2 is alkyl having 3 to 4 carbon atoms, R.sup.3 is hydrogen, benzyloxycarbonyl, acetyl or benzoyl, and n is an integer of 2 to 7. The subject compounds exhibit inhibitory activity towards thiol protease, especially, calcium-activated neutral thiol protease which exists in excess in muscle tissues of mammals afflicted with muscular dystrophy.
摘要翻译: 式中,R 1为氢,碱金属,苄基或碳原子数5〜6的环烷氧基烷基氨基酸衍生物,R2为碳原子数3〜4的烷基,R3为氢,苄氧羰基,乙酰基或苯甲酰基, n是2至7的整数。本发明化合物对于硫酸蛋白酶,特别是对于患有肌营养不良的哺乳动物的肌肉组织中存在过量的钙激活的中性硫醇蛋白酶表现出抑制活性。
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公开(公告)号:US4418075A
公开(公告)日:1983-11-29
申请号:US320113
申请日:1981-11-10
申请人: Masaharu Tamai , Shigeo Morimoto , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
发明人: Masaharu Tamai , Shigeo Morimoto , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
IPC分类号: A61K31/335 , A61K31/336 , A61K31/34 , A61P43/00 , C07D303/48 , C12N9/99
CPC分类号: C07D303/48 , Y10S514/907
摘要: An epoxysuccinyl amino acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen or alkali metal, R.sup.2 is isobutyl, R.sup.3 is hydrogen or benzyloxycarbonyl, and n is an integer of 5 to 7. The subject compounds exhibit inhibitory activity towards thiol protease, especially, calcium-activated neutral thiol protease which exists in excess in muscle tissues of mammals afflicted with muscular dystrophy.
摘要翻译: 式IMAMA的环氧琥珀酰基氨基酸衍生物,其中R 1是氢或碱金属,R 2是异丁基,R 3是氢或苄氧基羰基,n是5到7的整数。本发明化合物对硫醇蛋白酶表现出抑制活性,特别是 ,钙激活的中性硫醇蛋白酶,其在肌肉营养不良的哺乳动物的肌肉组织中过量存在。
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公开(公告)号:US4507232A
公开(公告)日:1985-03-26
申请号:US562439
申请日:1983-12-16
申请人: Masaharu Tamai , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura , Nobuhiko Katunuma
发明人: Masaharu Tamai , Takashi Adachi , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura , Nobuhiko Katunuma
IPC分类号: C07K1/113 , A61K38/00 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/083 , C12Q1/37 , C07C103/52
CPC分类号: C12Q1/37 , C07K5/06034 , C07K5/06078 , C07K5/06095 , C07K5/0808 , A61K38/00 , C12Q2337/12 , C12Q2337/22 , C12Q2337/30 , G01N2333/96466 , Y02P20/55
摘要: This invention is directed to novel peptide derivatives. Said peptide derivatives are useful as a substrate for the activity assay of enzymes of the group EC 3. 4. 22, for example, cathepsin L, cathepsin B and cathepsin H. Said peptide derivatives which contain L-methionine radical are prepared according to the methods conventional in peptide chemistry. As typical examples are mentioned D-leucyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate, .beta.-alanyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate and succinyl-L-tyrosyl-L-methionine-p-nitroanilide.
摘要翻译: 本发明涉及新型肽衍生物。 所述肽衍生物可用作组EC 3. 4.22的酶的活性测定的底物,例如组织蛋白酶L,组织蛋白酶B和组织蛋白酶H.所述含有L-甲硫氨酸基团的肽衍生物根据 肽化学中常规的方法。 作为典型实例,提及D-亮氨酰-L-酪氨酰-L-甲硫氨酸-β-萘甲酰胺甲酸盐,β-丙氨酰-L-酪氨酰-L-甲硫氨酸-β-萘甲酰胺甲酸盐和琥珀酰-L-酪氨酰-L-甲硫氨酸-p 硝基苯胺。
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公开(公告)号:US4387238A
公开(公告)日:1983-06-07
申请号:US263586
申请日:1981-05-14
申请人: Masami Goi , Kazuya Kameo , Jiro Sawada , Kazunori Hanada , Masaharu Tamai , Kiyoshi Oguma
发明人: Masami Goi , Kazuya Kameo , Jiro Sawada , Kazunori Hanada , Masaharu Tamai , Kiyoshi Oguma
IPC分类号: A61K31/335 , A61K31/336 , A61K31/395 , A61P3/00 , A61P3/14 , C07D303/48 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D405/06 , C07D405/10 , C07D409/12 , C07D413/06
CPC分类号: C07D303/48
摘要: The epoxysuccinamic acid compounds of the present invention are prepared by reaction of monoesters of epoxysuccinic acid or monoesters of epoxysuccinic acid chloride with amino compounds. These epoxysuccinamic acid compounds have excellent anti-inflammatory activity, thiol protease inhibitory activity, muscular dystrophy inhibitory activity and anti-hypertensive activity without acceleration of vascular permeability.
摘要翻译: 本发明的环氧琥珀酸化合物是通过环氧琥珀酸的单酯或环氧琥珀酰氯的单酯与氨基化合物的反应来制备的。 这些环氧琥珀酸化合物具有优异的抗炎活性,硫醇蛋白酶抑制活性,肌营养不良抑制活性和抗高血压活性,而不加速血管通透性。
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