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公开(公告)号:US4496717A
公开(公告)日:1985-01-29
申请号:US444170
申请日:1982-11-24
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
摘要: Novel erythromycin B derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each hydrogen or methyl, and the pharmaceutically acceptable acid addition salts thereof are disclosed. They exhibit excellent in vivo antibacterial activity against Gram-positive bacteria.
摘要翻译: 其中R1和R2相同或不同并且各自为氢或甲基的新颖的红霉素B衍生物及其药学上可接受的酸加成盐。 它们对革兰氏阳性菌表现出优异的体内抗菌活性。
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公开(公告)号:US4476298A
公开(公告)日:1984-10-09
申请号:US444171
申请日:1982-11-24
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
摘要: Novel erythromycin A derivatives of the formula ##STR1## wherein R is hydrogen or methyl, and the pharmaceutically acceptable acid addition salts thereof are disclosed. They exhibit excellent antibacterial activity against erythromycin resistant bacteria, Gram-positive bacteria and Mycoplasma species.
摘要翻译: 公开了其中R是氢或甲基的式“IMAGE”的新型红霉素A衍生物及其药学上可接受的酸加成盐。 它们对红霉素抗性细菌,革兰氏阳性菌和支原体物种具有优异的抗菌活性。
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公开(公告)号:US4833236A
公开(公告)日:1989-05-23
申请号:US43470
申请日:1987-04-28
申请人: Shigeo Morimoto , Yoko Takahashi , Yoshiaki Watanabe , Takashi Adachi , Toshifumi Asaka , Kaoru Sota
发明人: Shigeo Morimoto , Yoko Takahashi , Yoshiaki Watanabe , Takashi Adachi , Toshifumi Asaka , Kaoru Sota
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号: C07H17/08
摘要: Erythromycin derivatives represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a hydroxy group, R.sup.3 is a hydrogen atom, a lower alkanoyl group, an alkoxycarbonyl group or an alkylsuccinyl group, and the salts thereof are disclosed. These compounds have antibacterial activity.
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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:US4975370A
公开(公告)日:1990-12-04
申请号:US43536
申请日:1987-04-28
申请人: Joji Sasaki , Kazutoshi Mizoue , Takashi Adachi , Takatoshi Nagate , Shigeo Morimoto , Sadafumi Omura
发明人: Joji Sasaki , Kazutoshi Mizoue , Takashi Adachi , Takatoshi Nagate , Shigeo Morimoto , Sadafumi Omura
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C12P19/62 , C12R1/785
CPC分类号: C07H17/08 , C12P19/62 , C12R1/785 , Y10S435/822 , Y10S435/931
摘要: Mucor circinelloides f. griseo-cyanus IFO 4563 is cultivated in a medium containing 6-O-methylerythromycin A as a substrate to obtain 14-hydroxy-6-O-methyl-erythromycin A. This compound and its salt have anti-bacterial activity.
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公开(公告)号:US4382889A
公开(公告)日:1983-05-10
申请号:US335700
申请日:1981-12-30
申请人: Masahuru Tamai , Takashi Adachi , Shigeo Morimoto , Kiyoshi Oguma , Kazunori Hanada , Sadafumi Omura
发明人: Masahuru 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
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, cycloalkyl having 3-6 carbon atoms or a group of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl having 1-4 carbon atoms or said alkyl substituted with hydroxy, methylmercapto, phenyl, hydroxyphenyl, indolyl, an optionally protected carboxy, an optionally protected amino or an optionally protected guanidino, and R.sup.6 is hydroxy, alkalimetaloxy, alkoxy having 1-2 carbon atoms, benzyloxy, amino or dimethylamino, 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,R 4是具有1-10个碳原子的烷基,苯基,苄基,苯乙基,具有3-6个碳原子的环烷基或下式的基团:其中R5是氢,具有1-4个碳原子的烷基或 所述烷基被羟基,甲基巯基,苯基,羟基苯基,吲哚基,任选保护的羧基,任选保护的氨基或任选被保护的胍基取代,R 6是羟基,碱金属氧基,具有1-2个碳原子的烷氧基,苄氧基,氨基或二甲基氨基, 或者R 3和R 4与它们所连接的氮原子一起形成5-6元杂环,或被被保护的羧基取代的所述杂环。
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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:US4331803A
公开(公告)日:1982-05-25
申请号:US266060
申请日:1981-05-19
CPC分类号: C07H17/08
摘要: Novel erythromycin compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, and a pharmaceutically acceptable salt thereof are disclosed. They exhibit excellent antibacterial activity against Gram-positive bacteria, acid stability and in vivo activity.
摘要翻译: 公开了其中R1是氢或甲基的式“IMAGE”及其药学上可接受的盐的新型红霉素化合物。 它们对革兰氏阳性菌表现出优异的抗菌活性,酸稳定性和体内活性。
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公开(公告)号:US4990602A
公开(公告)日:1991-02-05
申请号:US283387
申请日:1988-12-12
申请人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Toshifumi Asaka , Yoshiaki Watanabe , Kaoru Sota , Kazuto Sekiuchi
发明人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Toshifumi Asaka , Yoshiaki Watanabe , Kaoru Sota , Kazuto Sekiuchi
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.
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