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192 条记录 (耗时 0.019 秒)

    Anthracycline antibiotics
    52.
    发明授权
    Anthracycline antibiotics 失效
    蒽环类抗生素

    公开(公告)号：US4207313A

    公开(公告)日：1980-06-10

    申请号：US838617

    申请日：1977-10-03

    申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

    发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Toshikazu Oki ,  Taiji Inui

    IPC分类号： C07H15/252 ,  C12P19/56 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252 ,  C12P19/56 ,  C12R1/465 ,  C12R1/48 ,  Y10S435/886 ,  Y10S435/888

    摘要： New anthracycline glycosides designated MA 144-G1, -G2, -L, -S1, -N1, -U1 and -Y which inhibit the growth of gram-positive bacteria and experimental animal tumors are produced by fermentation of certain species of Streptomyces and by the chemical or enzymatic conversion of certain anthracycline glycosides. New microbiological and chemical processes are also provided for preparation of the anthracycline glycosides MA 144-S2 and -U2 which have been found to be identical with the previously reported anthracyclines, marcellomycin and musettamycin.

    摘要翻译： 名称为MA 144-G1，-G2，-L，-S1，-N1，-U1和-Y的新型蒽环类苷，其抑制革兰氏阳性细菌和实验动物肿瘤的生长，是通过某些种类的链霉菌的发酵和 某些蒽环类苷的化学或酶转化。 还提供了新的微生物和化学方法用于制备蒽环类甙MA 144-S2和-U 2，其已被发现与先前报道的蒽环霉素，马塞罗霉素和musettamycin相同。

    Process for recovering macromomycin
    53.
    发明授权
    Process for recovering macromomycin 失效
    马来霉素回收方法

    公开(公告)号：US4164567A

    公开(公告)日：1979-08-14

    申请号：US801492

    申请日：1977-05-31

    申请人： Hamao Umezawa ,  Tomio Takeuchi

    发明人： Hamao Umezawa ,  Tomio Takeuchi

    IPC分类号： C12P1/06 ,  A61K35/00

    CPC分类号： C12R1/465 ,  C12P1/06

    摘要： There is provided a process for recovering macromomycin (hereinafter referred to as MCR) which comprises adding coagulants or coagulants and neutralizers to a culture filtrate saturated with ammonium sulfate and collecting the resulting precipitate containing MCR in a high yield at low centrifugal force. From the precipitate obtained, MCR powders can be prepared according to the methods described in U.S. Pat. No. 3,595,954 and others.

    摘要翻译： 提供了一种用于回收大分子霉素（以下称为MCR）的方法，该方法包括将凝结剂或凝结剂和中和剂加入到用硫酸铵饱和的培养物滤液中，并以低离心力以高产率收集含有MCR的沉淀。 从得到的沉淀物中，可以根据美国专利No. 第3,595,954号等。

    Isocoformycin and a process for the production thereof
    54.
    发明授权
    Isocoformycin and a process for the production thereof 失效
    异青霉素及其制备方法

    公开(公告)号：US4163839A

    公开(公告)日：1979-08-07

    申请号：US858928

    申请日：1977-12-09

    申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Masami Shimazaki

    发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Shinichi Kondo ,  Masami Shimazaki

    IPC分类号： C07H19/052 ,  C07H19/16 ,  C07H19/04 ,  A61K31/70

    CPC分类号： C07H19/16 ,  C07H19/052

    摘要： A novel, unique nucleoside, 3-.beta.-D-ribofuranosyl-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-7-ol, named isocoformycin, of the formula ##STR1## is provided by ring expansion of derivatives of 9-.beta.-D-ribofuranosyl-6-hydroxymethyl-1,6-dihydropurine. Isocoformycin markedly inhibits deaminating enzymes which inactivate formycin and adenine arabinoside (also known as ara-A and Vidarabine). Formycin and adenine arabinoside are used as antiviral and antitumor agents in mammals and birds and isocoformycin is advantageous to prolong the activity and effect of formycin and adenine arabinoside.

    摘要翻译： 一种新颖独特的核苷，3β-D-呋喃核糖基-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂-醇，命名为异青霉素，式为“IMAGE” 由9-β-D-呋喃核糖基-6-羟甲基-1,6-二氢嘌呤衍生物的环扩展提供。 异青霉素显着抑制脱氨酶，其使得霉菌和阿拉伯糖腺苷（也称为ara-A和阿糖腺苷）失活。 霉菌素和阿拉伯糖腺苷在哺乳动物和鸟类中用作抗病毒和抗肿瘤剂，异青霉素有利于延长霉素和阿拉伯糖腺苷的活性和作用。

    N-methylphenylserine alkyl ester derivatives and uses thereof
    56.
    发明授权
    N-methylphenylserine alkyl ester derivatives and uses thereof 失效
    N-甲基苯基丝氨酸烷基酯衍生物及其用途

    公开(公告)号：US5288898A

    公开(公告)日：1994-02-22

    申请号：US56619

    申请日：1993-05-04

    申请人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

    发明人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

    IPC分类号： A61K31/195 ,  C07C229/36 ,  A61K31/24

    CPC分类号： A61K31/195

    摘要： As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an .alpha.-adrenergic and .beta.-adrenergic agent to stimulate the .alpha.-adrenergic and .beta.-adrenergic functions of the central nervous system of mammalian animals and are expectable to be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the .alpha.- and/or .beta.-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C.sub.1 -C.sub.6) alkyl esters are preferred amongst the new compounds of this invention.

    摘要翻译： 由于新化合物现在提供作为（α） - 肾上腺素能和（β） - 肾上腺素能药物有效的N-甲基-3-（3,4-二羟基苯基）丝氨酸烷基酯，以刺激（α） - 肾上腺素能和（β ） - 哺乳动物中枢神经系统的肾上腺素能功能，并且预期可用于通过减少（α） - 和/或（β） - 肾上腺素能神经元的生物活性或功能引起的病症的治疗性治疗。 N-甲基-L-苏式-3-（3,4-二羟基苯基）丝氨酸（C1-C6）烷基酯在本发明的新化合物中是优选的。

    Method for the preparation of 4'-0-tetrahydropyranyladriamycin b
    59.
    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。