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公开(公告)号:US4463171A
公开(公告)日:1984-07-31
申请号:US502480
申请日:1983-06-09
申请人: Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
发明人: Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号: C07H17/08
摘要: Compounds of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkanoyl group;R.sup.3 represents a hydrogen atom or the group --COCH.sub.2 R.sup.5 in which R.sup.5 represents a lower alkyl group or an aryl or pyridyl group bonded through a sulfur atom;R.sup.4 represents a methyl group which may be substituted by aryl, pyridyl, pyridylthio, hydroxyl or arylthioamino, an aryl group, a nitrile group, a 5- or 6-membered heterocyclic group having 1 to 4 hetero atoms selected from nitrogen and sulfur atoms, or a tetrahydropyranyl group which may be substituted by methoxy;A represents the group --OCO--, --OSO.sub.2 --, --O-- or --S--, or A and R.sup.4, taken together, represent a halogen atom, a nitrile group or a group of the formula ##STR2## in which R.sup.6 represents two lower alkyl groups, the group ##STR3## or an alkylene group having 4 to 6 carbon atoms which may have in the chain an oxygen atom or a lower alkyl-substituted nitrogen atom; and said aryl group and heterocyclic group may optionally be substituted by a methyl, methoxy or nitro group, and when R.sup.1 represents a lower alkyl group,R.sup.3 does not represent a lower alkyl group,or their salts.These novel derivatives of macrolide antibiotics have excellent antibacterial activity.
摘要翻译: 下列通式的化合物:其中R 1和R 2表示氢原子或低级烷酰基; R3表示氢原子或基团-COCH2R5,其中R5表示低级烷基或通过硫原子键合的芳基或吡啶基; R 4表示可以被芳基,吡啶基,吡啶硫基,羟基或芳硫基氨基,芳基,腈基,具有1-4个选自氮和硫原子的杂原子的5或6元杂环基取代的甲基, 或可被甲氧基取代的四氢吡喃基; A代表基团-OCO-,-OSO 2 - , - O-或-S-,或A和R 4一起代表卤素原子,腈基或式(IMAGE)基团,其中R6代表二 低级烷基,基团
或具有4-6个碳原子的亚烷基,其可以在链中具有氧原子或低级烷基取代的氮原子; 并且所述芳基和杂环基可任选被甲基,甲氧基或硝基取代,并且当R 1表示低级烷基时,R 3不表示低级烷基或其盐。 这些大环内酯类抗生素的新型衍生物具有优良的抗菌活性。 -
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:US4355026A
公开(公告)日:1982-10-19
申请号:US300874
申请日:1981-09-11
IPC分类号: C07C50/24 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C43/215 , C07C45/00 , C07C45/26 , C07C67/00 , C07D307/32 , C07D309/30 , C07H13/08 , C07H15/252 , A61K31/71 , A61K31/65 , C07H15/24
CPC分类号: C07D307/32 , C07C43/215 , C07C45/26 , C07D309/30 , C07H13/08 , C07H15/252 , Y02P20/55 , Y10S514/908
摘要: New 4-demethoxy-11-deoxydaunomycin and 4-demethoxy-11-deoxyadriamycin anthracycline derivatives have been prepared and found to be useful antimicrobial and antitumor agents.
摘要翻译: 已经制备了新的4-脱甲氧基-11-脱氧果阿霉素和4-脱甲氧基-11-脱氧阿霉素蒽环类衍生物,发现它们是有用的抗微生物剂和抗肿瘤剂。
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4.
公开(公告)号:US4925877A
公开(公告)日:1990-05-15
申请号:US17108
申请日:1987-02-20
IPC分类号: A01N37/18 , A01N47/40 , A61K31/16 , A61K31/165 , A61K31/24 , A61K31/275 , C07C233/16
CPC分类号: C07C251/00
摘要: The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity. ##STR1## (in which R.sup.1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of 1 to 3;X represents a hydrogen atom or a halogen atom;Y represents a group of formula --CH.dbd.CH--NC, --CH.dbd.CH--NHR.sup.2 or --CH.sub.2 --CH.sub.2 --NHR.sup.2(where R.sup.2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R.sup.1 O).sub.n group is 2,5-dihydroxy group and Y is --CH.dbd.CH--NHCHO or --CH.sub.2 --CH.sub.2 --NHCHO).The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).
摘要翻译: 本发明提供了具有优异的酪氨酸特异性蛋白激酶抑制活性,抗肿瘤活性和抗菌活性的通式(I)的新的生理活性物质抑制剂类似物化合物。 (I)(其中R 1表示氢原子,低级烷酰基或低级烷基; n表示1〜3的正整数; X表示氢原子或卤素原子; Y表示 式-CH = CH-NC,-CH = CH-NHR 2或-CH 2 -CH 2 -NH 2(其中R 2表示甲酰基或低级烷酰基;除了X是氢原子,(R 1 O)n 基团是2,5-二羟基,Y是-CH = CH-NHCHO或-CH 2 -CH 2 -NHCHO),本发明还提供一种酪氨酸特异性蛋白激酶抑制剂,杀伤剂或杀菌剂,其含有至少一种化合物 所述式(I)。
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公开(公告)号:US4374980A
公开(公告)日:1983-02-22
申请号:US357970
申请日:1982-03-15
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号: C07H15/252
摘要: Disclosed is 3'-deamino-3'-morpholino-carminomycin, a new anthracycline glycoside having both antimicrobial and antitumor activity. Also disclosed is a new N-alkylation procedure for preparing the above compound as well as the known anthracyclines, 3'-deamino-3'-morpholino-adriamycin and 3'-deamino-3'-morpholino-daunomycin, in high yield.
摘要翻译: 公开了具有抗微生物和抗肿瘤活性的新的蒽环类苷酸3'-脱氨基-3'-吗啉代 - 黑麦草霉素。 还公开了以高产率制备上述化合物以及已知的蒽环类,3'-脱氨基-3'-吗啉代 - 阿霉素和3'-脱氨基-3'-吗啉代 - 道宁霉素的新的N-烷基化方法。
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6.
公开(公告)号:US4818818A
公开(公告)日:1989-04-04
申请号:US925774
申请日:1986-10-30
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号: C07H15/252
摘要: For the preparation of 4'-0-tetrahydropyranyladriamycin b, the 9,14-position of the starting adriamycin is previously protected with phenylboronic acid and then the 4'-position of the thus protected adriamycin is selectively tetrahydropyranylated. After the tetrahydropyranylation, the by-product of 4'-0-tetrahydropyranyladriamycin a is converted to the aimed product of 4'-0-tetrahydropyranyladriamycin b. The yield of the product of 4'-0-tetrahydropyranyladriamycin b is high.The present invention provides a method for the preparation of 4'-0-tetrahydropyranyladriamycin b, where 3,4-dihydro-2H-pyran is added to a reaction solution containing a 9,14-protected adriamycin as obtained by (a) reacting adriamycin and phenyl-boronic acid or (b) reacting 4'-0-tetrahydropyranyladriamycin b and phenylboronic acid in the presence of an acid catalyst, for 4'-tetrahydropyranylation of the said 9,14-protected adriamycin, and then, the 9,14-protected position of the resulting product is deprotected and 4'-0-tetrahydropyranyladriamycin b is isolated by chromatography with silica-gel.
摘要翻译: 为了制备4'-O-四氢吡喃阿霉素b,起始阿霉素的9,14位预先用苯基硼酸保护,然后由此保护的阿霉素的4'-位选择性地被四氢吡喃基化。 四氢吡喃基化后,4'-O-四氢吡喃阿霉素a的副产物转化为4'-O-四氢吡喃基阿霉素b的目标产物。 4'-O-四氢吡喃阿霉素b的产物的产率高。 本发明提供了制备4'-O-四氢吡喃阿霉素b的方法,其中将3,4-二氢-2H-吡喃加入到含有9,14-保护的阿霉素的反应溶液中,其通过以下步骤获得:(a)使阿霉素 和苯基硼酸或(b)在酸催化剂存在下使4'-O-四氢吡喃阿霉素b和苯基硼酸反应,进行所述9,14受保护的阿霉素的4'-四氢吡喃基化,然后,9,14 将所得产物的保护位置脱保护,并用硅胶色谱分离4'-O-四氢吡喃基阿霉素b。
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公开(公告)号:US4303785A
公开(公告)日:1981-12-01
申请号:US117163
申请日:1980-01-31
IPC分类号: C07H15/252 , C07H15/24 , A61K31/71
CPC分类号: C07H15/252
摘要: New anthracycline derivatives of adriamycin and daunomycin prepared by the etherification of the C-4' and/or C-14 hydroxyl groups of the starting material glycosides are found to be useful antimicrobial and antitumor agents.
摘要翻译: 发现通过起始物质糖苷的C-4'和/或C-14羟基的醚化制备的阿霉素和道诺霉素的新蒽环类衍生物是有用的抗微生物剂和抗肿瘤剂。
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公开(公告)号:US4360664A
公开(公告)日:1982-11-23
申请号:US253489
申请日:1981-04-13
IPC分类号: C07H15/252 , C07H15/24
CPC分类号: C07H15/252
摘要: A new and improved process for the preparation of C-4' etherified anthracycline glycoside derivatives is provided. The new process involves fewer steps than the prior art process and gives the antibiotic end-products in higher yield.
摘要翻译: 提供了一种新的改进的C-4醚化蒽环苷衍生物的制备方法。 新方法涉及比现有技术方法更少的步骤,并以更高的产率给予抗生素最终产品。
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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: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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