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192 条记录 (耗时 0.026 秒)

    Peptides and acid addition salts thereof
    83.
    发明授权
    Peptides and acid addition salts thereof 失效
    肽及其酸加成盐

    公开(公告)号：US4185156A

    公开(公告)日：1980-01-22

    申请号：US942581

    申请日：1978-09-15

    申请人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Tetsushi Saino ,  Michinori Koyama

    发明人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Tetsushi Saino ,  Michinori Koyama

    IPC分类号： C07K14/81 ,  A61K20060101 ,  A61K31/19 ,  A61K38/00 ,  A61P29/00 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C279/14 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07C101/72 ,  A01N9/20

    CPC分类号： C07C51/377 ,  Y02P20/55

    摘要： The compounds of this invention represented by the following formula: ##STR1## (wherein R is hydrogen atom, an alkyl group having C.sub.1 to C.sub.4, a hydroxy group or a halogen atom) can be obtained by condensing the compounds represented by the following formula: ##STR2## wherein R is as defined above, X is hydrogen atom, and Y is hydrogen atom or an amino protecting group or reactive derivatives thereof with (S)-arginine according to a method commonly employed in the peptide chemistry.The peptides according to this invention have strong inhibitory activity against aminopeptidase B, can raise immunity of the organisms and prove useful for inhibiting transfer of cancer and relapse thereof. Also, when used jointly with Bleomycin which is an antitumor agent, they can greatly enhance the antitumor effect of said agent.

    摘要翻译： 由下式表示的本发明化合物：其中R为氢原子，具有C1〜C4的烷基，羟基或卤素原子的化合物可以通过将下式表示的化合物缩合得到： 根据肽化学通常使用的方法，其中R如上定义，X​​为氢原子，Y为氢原子或氨基保护基或其与（S） - 精氨酸的反应性衍生物。 根据本发明的肽对氨基肽酶B具有很强的抑制活性，可以提高生物体的免疫力，并证明可用于抑制癌症的转移和复发。 此外，当与作为抗肿瘤剂的博来霉素联合使用时，它们可以大大增强所述药剂的抗肿瘤效果。

    Biologically active substance, bestatin, and production thereof
    87.
    发明授权
    Biologically active substance, bestatin, and production thereof 失效
    生物活性物质，生物活性物质及其生产

    公开(公告)号：US4029547A

    公开(公告)日：1977-06-14

    申请号：US690456

    申请日：1976-05-27

    申请人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Masa Hamada ,  Yoshiro Okami

    发明人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tomio Takeuchi ,  Masa Hamada ,  Yoshiro Okami

    IPC分类号： C12P13/04 ,  C12P21/02 ,  C12D9/00

    CPC分类号： C12P21/02 ,  C12P13/04 ,  Y10S435/803 ,  Y10S435/886

    摘要： This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).

    摘要翻译： 本发明提供了一种名为bestatin的新化合物，其抑制氨基肽酶B，亮氨酸氨肽酶和博来霉素水解酶，增强博来霉素的抗肿瘤作用，具有化学名称[（2S，3R）-3-氨基-2-羟基-4-苯基丁酰基] - L-亮氨酸并具有以下结构：＆lt; IMAGE＆gt;并且还提供其制备方法，其包括培养在需氧条件下在营养培养基中产生海参蛋白的链霉菌菌株，直到对所述培养物 培养基，然后从所述培养基中回收所述的bestatin。 优选的菌株是橄榄链霉菌FERM-P No.2590（A.T.C.C. 31159）。