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公开(公告)号:US4190589A
公开(公告)日:1980-02-26
申请号:US902824
申请日:1978-05-04
IPC分类号: A61K31/34 , A61K31/365 , A61P31/04 , A61P35/00 , A61P35/02 , C07D493/10
CPC分类号: C07D493/10
摘要: Coriolin derivatives having antitumor activity and low toxicity represented by the following general formula: ##STR1## where R: --CO(CH.sub.2).sub.6 CH.sub.3 or --COCH(OH)(CH).sub.2).sub.5 CH.sub.3,X: .dbd.CH.sub.2 or --COOR',R': H or lower alkyl group.Y: OH or .dbd.O andZ: --OH or OCH.sub.3,as well as the process for producing the above derivatives are disclosed.
摘要翻译: 其中R:-CO(CH 2)6 CH 3或-COCH(OH)(CH)2)5CH 3,X:= CH 2或-COOR',R ':H或低级烷基。 Y:OH或= O和Z:-OH或OCH 3,以及制备上述衍生物的方法。
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公开(公告)号:US4185156A
公开(公告)日:1980-01-22
申请号:US942581
申请日:1978-09-15
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。
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公开(公告)号:US4167448A
公开(公告)日:1979-09-11
申请号:US916184
申请日:1978-06-16
申请人: Hamao Umezawa , Takaaki Aoyagi , Tomio Takeuchi , Masa Hamada
发明人: Hamao Umezawa , Takaaki Aoyagi , Tomio Takeuchi , Masa Hamada
CPC分类号: C07K5/0202 , C07K5/0808 , Y10S435/886
摘要: The present invention relates to new physiologically active peptides, derivatives thereof and a process for preparation thereof. In particular, it relates to new tetrapeptides designated amastatins A.sub.1, A.sub.2, A.sub.3, B.sub.1 and B.sub.2 and derivatives thereof which have an inhibitory effect on aminopeptidase A and also show stimulation of antibody formation and to a process for preparation thereof by cultivating a strain belonging to the genus Streptomyces.
摘要翻译: 本发明涉及新的生理活性肽及其衍生物及其制备方法。 具体地说,涉及对氨基肽酶A具有抑制作用的amastatin A1,A2,A3,B1和B2及其衍生物的新四肽,其也表现出抗体形成的刺激,以及通过培养属于 链霉菌属。
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公开(公告)号:US4147778A
公开(公告)日:1979-04-03
申请号:US797201
申请日:1977-05-16
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Masaaki Ishizuka , Hiroshi Naganawa , Toshikazu Oki , Taiji Inui
IPC分类号: C12P1/06 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7048 , A61P31/04 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , A61K31/71 , C07H15/24
CPC分类号: C12R1/465 , C07H15/252 , C12P19/56 , Y10S435/886
摘要: A novel anthracycline antibiotic complex designated herein as baumycin complex is produced by fermentation of a baumycin-producing strain of Streptomyces, e.g. Streptomyces coeruleorubidus ME 130-A4 (FERM-P3540, ATCC 31276). The complex and four bioactive components thereof designated baumycin A.sub.1, A.sub.2, B.sub.1 and B.sub.2 are useful as antibacterial and antitumor agents.
摘要翻译: 本文称为鲍曼霉素复合物的新型蒽环类抗生素复合物是通过发酵生产巴霉素的链霉菌菌株,例如, Streptomyces coeruleorubidus ME 130-A4(FERM-P3540,ATCC 31276)。 其中称为baumycin A1,A2,B1和B2的复合物和四种生物活性成分可用作抗细菌剂和抗肿瘤剂。
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公开(公告)号:US4105658A
公开(公告)日:1978-08-08
申请号:US659319
申请日:1976-02-19
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Shinichi Kondo , Masaaki Ishizuka , Hiroshi Naganawa
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Shinichi Kondo , Masaaki Ishizuka , Hiroshi Naganawa
IPC分类号: C07G11/00
CPC分类号: A61K36/06 , C07G11/00 , Y10S435/886
摘要: There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukemia L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).
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86.
公开(公告)号:US4071411A
公开(公告)日:1978-01-31
申请号:US692827
申请日:1976-06-04
申请人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Akira Takamatsu , Toshikazu Oki
发明人: Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Akira Takamatsu , Toshikazu Oki
IPC分类号: C07H15/252 , C12D9/14
CPC分类号: C07H15/252 , Y10S435/803 , Y10S435/822 , Y10S435/834 , Y10S435/837 , Y10S435/839 , Y10S435/843 , Y10S435/849 , Y10S435/852 , Y10S435/86 , Y10S435/869 , Y10S435/875 , Y10S435/883 , Y10S435/886 , Y10S435/922 , Y10S435/924
摘要: New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.
摘要翻译: 新型抗肿瘤剂名为阿沙利霉素A和B,它们是蒽环类苷并抑制各种微生物的生长,例如金黄色葡萄球菌,黄曲霉,牛磺酸棒状杆菌,并抑制小鼠和肝癌中白血病L1210和P388和淋巴瘤6C3HED等动物肿瘤的生长 在大鼠中通过发酵属于链霉菌属(Streptomyces)的微生物来产生,其被命名为马链霉菌(Streptomyces galilaeus)(MA144-M1和ATCC 31133); 它们通过用于回收抗生素的常规方法从肉汤中回收。
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公开(公告)号:US4032635A
公开(公告)日:1977-06-28
申请号:US660731
申请日:1976-02-24
申请人: Hamao Umezawa , Tomio Takeuchi , Akira Takamatsu , Shunro Mori
发明人: Hamao Umezawa , Tomio Takeuchi , Akira Takamatsu , Shunro Mori
IPC分类号: A61K31/165 , A61K31/19 , A61K31/22 , A61K31/60 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/75 , C07C233/80
CPC分类号: A61K31/60
摘要: Compounds having the formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) exhibit suppressive activity to various immune responses and can be employed in the therapy of immunological diseases, especially autoimmune diseases.One example is 3',5'-dichloro-2,4'-dihydroxybenzanilide having the formula ##STR2## AND ANOTHER IS 3',5'-DICHLORO-2,2'-DIHYDROXYBENZANILIDE HAVING THE FORMULA ##STR3##
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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
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:< IMAGE>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)。
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公开(公告)号:US4009155A
公开(公告)日:1977-02-22
申请号:US503553
申请日:1974-09-05
申请人: Hamao Umezawa , Tomio Takeuchi , Hironobu Iinuma , Osamu Tanabe
发明人: Hamao Umezawa , Tomio Takeuchi , Hironobu Iinuma , Osamu Tanabe
IPC分类号: C07G11/00 , C07C105/00
CPC分类号: C07G11/00 , Y10S435/911
摘要: There is disclosed a new antibiotic called calvatic acid having the structure p-carboxyphenyl-azoxycarbonitrile and processes for its production by fermentation and processes for its recovery and purification. This substance is effective in inhibiting the growth of Gram-positive bacteria and carcinoma.
摘要翻译: 公开了具有对羧基苯基 - 氮氧化羰基结构的新生抗生素,称为蓖麻酸,其通过发酵及其回收和纯化方法生产。 该物质有效抑制革兰氏阳性菌和癌细胞的生长。
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公开(公告)号:US3974184A
公开(公告)日:1976-08-10
申请号:US490839
申请日:1974-07-23
申请人: Hamao Umezawa , Tomio Takeuchi , Hideo Chimura , Tsutomu Sawa , Masa Hamada
发明人: Hamao Umezawa , Tomio Takeuchi , Hideo Chimura , Tsutomu Sawa , Masa Hamada
IPC分类号: C12P17/06 , C07D311/36 , C07D311/38 , C12N9/99 , C12P1/06
CPC分类号: C07D311/38 , Y10S435/826
摘要: This invention relates to the novel compounds 3',5,7-trihydroxy-4',6-dimethoxy-isoflavone, 3'5,7-trihydroxy-4',8-dimethoxy-isoflavone and 3',7-dihydroxy-4',6,8-trimethoxy-isoflavone which are powerful inhibitors of catechol-O-methyl transferase (COMT) and to their production by fermentation of Actinomyces roseolus.
摘要翻译: 本发明涉及新化合物3',5,7-三羟基-4',6-二甲氧基异黄酮,3'5,7-三羟基-4',8-二甲氧基异黄酮和3',7-二羟基-4 ',6,8-三甲氧基异黄酮,它们是儿茶酚-O-甲基转移酶(COMT)的强大抑制剂,以及它们通过玫瑰红放线菌发酵的生产。
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