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    Method for the preparation of 4'-0-tetrahydropyranyladriamycin b
    2.
    发明授权
    Method for the preparation of 4'-0-tetrahydropyranyladriamycin b 失效
    制备4'-O-四氢吡喃阿霉素的方法b

    公开(公告)号：US4818818A

    公开(公告)日：1989-04-04

    申请号：US925774

    申请日：1986-10-30

    申请人： Hamao Umezawa, deceased ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Yoshikazu Takahashi

    发明人： Hamao Umezawa, deceased ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Yoshikazu Takahashi

    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。

    Physiologically active erbstatin analogue compounds and compositions
    4.
    发明授权
    Physiologically active erbstatin analogue compounds and compositions 失效
    生理活性的erbstatin类似物和组合物

    公开(公告)号：US4925877A

    公开(公告)日：1990-05-15

    申请号：US17108

    申请日：1987-02-20

    申请人： Hamao Umezawa, deceased ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Kunio Isshika ,  Masaya Imoto

    发明人： Hamao Umezawa, deceased ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Kunio Isshika ,  Masaya Imoto

    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）。

    Derivatives of macrolide antibiotics
    6.
    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。

    Novel macrolactone derivatives and process of producing them
    10.
    发明授权
    Novel macrolactone derivatives and process of producing them 失效
    新型大分子内酯衍生物及其制备方法

    公开(公告)号：US4196280A

    公开(公告)日：1980-04-01

    申请号：US883301

    申请日：1978-03-03

    申请人： Sumio Umezawa ,  Hamao Umezawa ,  Kuniaki Tatsuta

    发明人： Sumio Umezawa ,  Hamao Umezawa ,  Kuniaki Tatsuta

    IPC分类号： C07D313/00 ,  C07D407/06 ,  C07H15/04 ,  C07H17/08

    CPC分类号： C07H15/04 ,  C07D313/00 ,  C07D407/06 ,  C07H17/08

    摘要： By protecting the aldehyde group of a macrolide series antibiotics with a cyclic acetal or thioacetal, novel macrolide derivatives can be produced from the macrolide series antibiotics by releasing successively, the sugar moieties bonded to the macrolide antibiotics.The novel macrolide derivatives obtained by this invention, that is, the derivatives of a macrolide series antibiotics produced by releasing partially or wholly the sugar moieties bonded are useful as intermediates for producing novel macrolide series antibiotics.

    摘要翻译： 通过用环缩醛或硫缩醛保护大环内酯类抗生素的醛基，可以通过依次释放大环内酯类抗生素，与大环内酯类抗生素结合的糖部分，产生新型大环内酯衍生物。 通过本发明获得的新型大环内酯衍生物，即通过部分或全部释放部分键合产生的大环内酯类抗生素衍生物可用作生产新型大环内酯类抗生素的中间体。