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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
    3.
    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）。

    DNA segment containing streptomycin resistance gene and being capable of controlling expression of said gene
    8.
    发明授权
    DNA segment containing streptomycin resistance gene and being capable of controlling expression of said gene 失效
    含有链霉素抗性基因并能够控制所述基因表达的DNA片段

    公开(公告)号：US5202427A

    公开(公告)日：1993-04-13

    申请号：US659469

    申请日：1991-02-25

    申请人： Hamao Umezawa, deceased ,  Yoji Umezawa, heir ,  Yoji Umezawa, heir ,  Yoshiro Okamo, heir

    发明人： Hamao Umezawa, deceased ,  Yoji Umezawa, heir ,  Yoji Umezawa, heir ,  Yoshiro Okamo, heir

    IPC分类号： C12N9/12 ,  C12N15/76

    CPC分类号： C12N15/76 ,  C12N9/12

    摘要： A DNA segment of this invention is a DNA fragment of a length of about 3.8 kb which is obtained by excising with a restriction endonuclease Bgl II a hybrid plasmid pST 141 having a length of about 12.6 kb of Streptomyces griseus 4-1 strain (FERM P-7984, namely, FERM BP-1198) to give a Bgl II-Bgl II DNA fragment, and then excising with a restriction endonuclease Sph I the resultant Bgl II-Bgl II DNA fragment having a length of about 7.0 kb and having the restriction endonuclease sites as shown in the restriction endonuclease map of FIG. 1 . This DNA fragment is a DNA which contains a streptomycin resistance gene and contains, in the vicinity of this gene, such a DNA region possessing a function to control the expression of the streptomycin resistance gene. An insertion of this DNA fragment having a length of about 3.8 kb into a suitable actinomycetes plasmid vector can produce such a hybrid plasmid which acts reliably as a selected marker of the streptomycin resistance.

    摘要翻译： 本发明的DNA片段是长约3.8kb的DNA片段，其通过用限制性内切核酸酶Bgl II切割具有长度为约12.6kb的灰色链霉菌4-1菌株（FERM P）的杂交质粒pST141获得 -7984，即FERM BP-1198），得到Bgl II-Bgl II DNA片段，然后用限制性内切核酸酶SphI切割得到长度为约7.0kb并具有约束条件的所得Bgl II-Bgl II DNA片段 如图1的限制性内切核酸酶图所示的内切核酸酶位点。 1。 该DNA片段是含有链霉素抗性基因的DNA，该基因附近含有具有控制链霉素抗性基因表达功能的DNA区域。 将具有约3.8kb长度的该DNA片段插入合适的放线菌质粒载体中可以产生这样的杂交质粒，其可靠地作为链霉素抗性的选择标记物起作用。