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32 条记录 (耗时 0.026 秒)

    Anthracycline antibiotics
    3.
    发明授权
    Anthracycline antibiotics 失效
    蒽环类抗生素

    公开(公告)号：US4918172A

    公开(公告)日：1990-04-17

    申请号：US252636

    申请日：1988-10-03

    申请人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

    发明人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

    IPC分类号： C07H15/252

    CPC分类号： C07H15/252

    摘要： Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is 1-hydroxyethyl group, R.sup.4 is hydrogen atom and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1, R.sup.2 and R.sup.4 are hydroxyl groups, R.sup.3 is ethyl group and X represents daunosamine-rhodenose, daunosamine-deoxyfucose, rhodosamine-rhodenose, N-monomethyldaunosamine-rhodenose or N-monomethyldaunosamine-deoxyfucose; orR.sup.1 is methoxy group, R.sup.2 is hydroxyl group, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.4 are hydroxy groups, R.sup.2 is hydrogen atom, R.sup.3 is ethyl group and X represents daunosamine-deoxyfucose, as well as pharmaceutically acceptable acid addition salts thereof. The antibiotics (I) have a carcinostatic activity and are useful as a carcinostatic for murine leukemia L1210 cells in culture.

    Tylosin derivatives
    7.
    发明授权
    Tylosin derivatives 失效
    泰乐菌素衍生物

    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。

    Derivatives of macrolide antibiotics
    10.
    发明授权
    Derivatives of macrolide antibiotics 失效
    大环内酯类抗生素衍生物

    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。