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公开(公告)号:US4418192A
公开(公告)日:1983-11-29
申请号:US370212
申请日:1982-04-20
申请人: Hiroshi Tanaka , Takeo Yoshioka , Yasutaka Shimauchi , Toshikazu Oki , Tomoyuki Ishikura , Tomio Takeuchi , Hamao Umezawa
发明人: Hiroshi Tanaka , Takeo Yoshioka , Yasutaka Shimauchi , Toshikazu Oki , Tomoyuki Ishikura , Tomio Takeuchi , Hamao Umezawa
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号: C07H15/252
摘要: Disclosed are novel anthracyclinone glycosides represented by the chemical formula ##STR1## wherein R.sup.1 is hydrogen or methyl;R.sup.2 is hydrogen or hydroxyl;R.sup.3 is hydrogen or methoxycarbonyl;R.sup.4 is two hydrogen atoms or an oxygen atom;R.sup.5 is hydrogen, hydroxyl or --OCOX (wherein X is lower alkyl or aralkyl);R.sup.6 is amino, monomethylamino or dimethylamino;R.sup.7 is hydrogen or acetyl; andR.sup.8 is hydrogen or L-cinerulose A ##STR2## but, when R.sup.1 and R.sup.3 are hydrogen and methoxycarbonyl respectively, R.sup.2 is hydrogen; R.sup.4 is two hydrogen atoms; R.sup.5 is hydrogen; R.sup.6 is amino, monoethylamino or dimethylamino; R.sup.7 is acetyl; and R.sup.8 is L-cinerulose A,and their acid addition salts and a method for preparation thereof which consists of treating O-alpha-L-cinerulosyl-(1.fwdarw.4)-O-(3-O-acetyl-2-deoxy-alpha-L-fucosyl)-(1.fwdarw.4)-alpha-L-rhodosamine with corresponding aglycones.
摘要翻译: 公开了由化学式(IMAGE)(I)表示的新型蒽环酸苷,其中R1是氢或甲基; R2是氢或羟基; R3是氢或甲氧基羰基; R4是两个氢原子或氧原子; R5是氢,羟基或-OCOX(其中X是低级烷基或芳烷基); R6是氨基,单甲基氨基或二甲基氨基; R7是氢或乙酰基; 并且R 8是氢或L-果糖醛酸A,但是当R 1和R 3分别是氢和甲氧基羰基时,R 2是氢; R4是两个氢原子; R5是氢; R6是氨基,单乙基氨基或二甲基氨基; R7是乙酰基; R8为L-丝瓜糖苷A及其酸加成盐及其制备方法,其由O-α-L-脯氨酰基 - (1-> 4)-O-(3-O-乙酰基-2-脱氧 α-L-岩藻糖基) - (1→4)-alpha-L-罗丹明与相应的糖苷配基。
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公开(公告)号:US4612372A
公开(公告)日:1986-09-16
申请号:US754568
申请日:1985-07-12
申请人: Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
发明人: Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.
摘要翻译: 新型泰乐菌素衍生物由下式表示:其中R代表氢原子,乙酰基或丙酰基; X表示-CO-或-SO 2 - 基团; Y表示在2位或4位与苄基结合的氟原子,乙酰基,甲磺酰基,甲硫基,苯甲酰基或甲氧基; Z代表氢原子或D-霉菌素残留物:作为大环内酯类抗生素的泰乐菌素衍生物提供了改善的抗菌活性和提高体内吸收和排泄的能力。
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公开(公告)号:US4424342A
公开(公告)日:1984-01-03
申请号:US361175
申请日:1982-03-24
申请人: Toshikazu Oki , Akihiro Yoshimoto , Yasue Matsuzawa , Tomoyuki Ishikura , Hamao Umezawa , Tomio Takeuchi
发明人: Toshikazu Oki , Akihiro Yoshimoto , Yasue Matsuzawa , Tomoyuki Ishikura , Hamao Umezawa , Tomio Takeuchi
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , C07H15/24 , A61K31/71
CPC分类号: C07H15/252 , C12P19/56 , C12R1/465
摘要: Disclosed are an antitumor compound having the chemical structure ##STR1## or its acid addition salts; and its preparation method which consists of treating a compound represented by the chemical structure ##STR2## wherein R is a COCH.sub.3 or CH(OH)CH.sub.3 group, by a streptomycetes strain or its mutants.
摘要翻译: 公开了具有化学结构(I)或其酸加成盐的抗肿瘤化合物; 及其制备方法,该方法由化学结构(IMAGE)(II)表示的化合物
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公开(公告)号:US4373094A
公开(公告)日:1983-02-08
申请号:US288072
申请日:1981-07-29
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , A61K31/71 , C07H15/24
CPC分类号: C07H15/252 , C12P19/56 , C12R1/465
摘要: New anthracycline compounds, 2-hydroxy-aclacinomycins M, N, S and T having potent antitumor activity and low toxicity, and the processes for the preparation thereof from 2-hydroxy-aclacinomycin A by reduction or acid hydrolysis are disclosed.
摘要翻译: 公开了新的蒽环类化合物,具有有效的抗肿瘤活性和低毒性的2-羟基 - 阿拉伯霉素M,N,S和T,并且通过还原或酸水解由2-羟基 - 阿拉伯霉素A制备它们的方法。
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公开(公告)号:US4592999A
公开(公告)日:1986-06-03
申请号:US514678
申请日:1983-07-18
申请人: Hamao Umezawa , Tomio Takeuchi , Kageaki Kouno , Tomoyuki Ishikura , Akihiro Yoshimoto , Yukio Takatsuki , Hiroyasu Tobe
发明人: Hamao Umezawa , Tomio Takeuchi , Kageaki Kouno , Tomoyuki Ishikura , Akihiro Yoshimoto , Yukio Takatsuki , Hiroyasu Tobe
IPC分类号: C12P17/06 , C07H15/252 , C12P19/56 , C12R1/465
CPC分类号: C07H15/252 , C12P19/56 , C12R1/465 , Y10S435/886
摘要: This invention is to provide a new microbial process for producing daunomycin by a mutant strain belonging to the genus Streptomyces.
摘要翻译: 本发明提供一种用于通过属于链霉菌属的突变菌株生产道诺霉素的新的微生物方法。
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公开(公告)号:US3988315A
公开(公告)日:1976-10-26
申请号:US596682
申请日:1975-07-16
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Akira Takamatsu , Toshikazu Oki
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Akira Takamatsu , Toshikazu Oki
IPC分类号: C07H15/252 , C12P1/06 , C12P19/56 , C07H17/08
CPC分类号: C07H15/252 , Y10S435/886
摘要: New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.
摘要翻译: 新型抗肿瘤剂名为阿沙利霉素A和B,它们是蒽环类苷并抑制各种微生物的生长,例如金黄色葡萄球菌,黄曲霉,牛磺酸棒状杆菌,并抑制小鼠和肝癌中白血病L1210和P388和淋巴瘤6C3HED等动物肿瘤的生长 在大鼠中通过发酵属于链霉菌属(Streptomyces)的微生物来产生,其被命名为马链霉菌(Streptomyces galilaeus)(MA144-M1和ATCC 31133); 它们通过用于回收抗生素的常规方法从肉汤中回收。
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公开(公告)号:US4474945A
公开(公告)日:1984-10-02
申请号:US405917
申请日:1982-08-06
IPC分类号: C07H15/252 , C12P19/56 , C07H17/08 , C12N1/00 , C12P19/62
CPC分类号: C07H15/252 , C12P19/56 , C12R1/465 , Y10S514/908
摘要: New anthracycline compounds, 2-hydroxyaclacinomycin B having potent antitumor activity and lower toxicity, and a process for producing 2-hydroxyaclacinomycins A, B, and N by fermentation.
摘要翻译: 新的蒽环类化合物,具有有效抗肿瘤活性和较低毒性的2-羟基阿拉伯霉素B,以及通过发酵生产2-羟基卡曲霉素A,B和N的方法。
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公开(公告)号:US4192915A
公开(公告)日:1980-03-11
申请号:US898065
申请日:1978-04-20
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
IPC分类号: C07H15/252 , C12P19/56 , C12D9/14
CPC分类号: C12R1/465 , C07H15/252 , C12P19/56 , C12R1/48 , Y10S435/886 , Y10S435/888
摘要: New antitumor agents designated rhodirubin A and B, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria and mammalian tumors, are produced by fermentation of rhodirubin-producing strains of Streptomyces, e.g. Streptomyces sp. ME 505-HEI (ATCC 31273).
摘要翻译: 通过发酵罗丹明生产菌株Streptomyces,例如,通过发酵来产生称为罗丹霉素A和B的新型抗肿瘤药物,其是蒽环类苷并抑制革兰氏阳性细菌和哺乳动物肿瘤的生长。 链霉菌属 ME 505-HEI(ATCC 31273)。
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公开(公告)号:US4127714A
公开(公告)日:1978-11-28
申请号:US823052
申请日:1977-08-09
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
IPC分类号: C12P19/56 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号: C07H15/252 , Y10S435/886
摘要: New antitumor agents designated rhodirubin A and B, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria and mammalian tumors, are produced by fermentation of rhodirubin-producing strains of Streptomyces, e.g. Streptomyces sp. ME 505-HEI (ATCC 31273).
摘要翻译: 通过发酵罗丹明生产菌株Streptomyces,例如,通过发酵来产生称为罗丹霉素A和B的新型抗肿瘤药物,其是蒽环类苷并抑制革兰氏阳性细菌和哺乳动物肿瘤的生长。 链霉菌属 ME 505-HEI(ATCC 31273)。
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公开(公告)号:US4612371A
公开(公告)日:1986-09-16
申请号:US756876
申请日:1985-07-18
申请人: Akihiro Yoshimoto , Shizuka Fujii , Katsuro Kubo , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
发明人: Akihiro Yoshimoto , Shizuka Fujii , Katsuro Kubo , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , C07H15/24
CPC分类号: C07H15/252
摘要: Novel anthracycline antibiotics characteristic of Ring A of the anthracycline skeleton are produced by microorganisms belonging to the genus Streptomyces and are useful as anti-cancer agents. The antibiotics designated D-788-6 to -10 are shown by general formula: ##STR1## wherein Y represents a group shown by: ##STR2##
摘要翻译: 蒽环霉素骨架A环特征的新型蒽环类抗生素由属于链霉菌属的微生物产生,可用作抗癌剂。 称为D-788-6至-10的抗生素由以下通式表示:其中Y代表如下所示的基团:
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