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1.发明授权3-[(S)-1'-Phenylethylamino]propylaminobleomycin, non-toxic salt thereof, and method for producing same 失效3 - [（S）-1'-苯乙基氨基]丙基氨基倍巴青霉素，其无毒盐及其制备方法
公开(公告)号：US4195018A
公开(公告)日：1980-03-25
申请号：US915805
申请日：1978-06-15
申请人： Tomohisa Takita , Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Osamu Yoshioka , Hamao Umezawa
发明人： Tomohisa Takita , Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Osamu Yoshioka , Hamao Umezawa
IPC分类号： C07K9/00 , C07C103/52 , A61K37/10
CPC分类号： C07K9/003 , Y10S930/19 , Y10S930/27
摘要： Novel 3-[(S)-1'-phenylethylamino]propylaminobleomycin obtained by reacting a reactive derivative of the carboxyl group of bleomycinic acid with N-[(S)-1'-phenylethyl]-1,3-diaminopropane, a non-toxic salt of said novel bleomycin, and a method for producing the novel bleomycin. Because of much reduction in the side effect causing pulmonary fibrosis, the novel bleomycin is more useful than a commercial bleomycin complex which gives rise to said undesirable side effect.
摘要翻译： 通过使博来霉素酸的羧基的活性衍生物与N - [（S）-1'-苯基乙基] -1,3-二氨基丙烷反应而得到的新型3 - [（S）-1'-苯基乙基氨基] 所述新型博莱霉素的有毒盐，以及生产新型博来霉素的方法。 由于引起肺纤维化的副作用大大减少，新博莱霉素比商业博来霉素复合物更有用，这引起了不希望的副作用。
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2.发明授权3-[(S)-1'-phenylethylamino]propylaminobleomycin, non-toxic salt thereof, and method for producing same 失效3 - [（S）-1'-苯基乙基氨基]丙基氨基倍巴青霉素，其无毒盐及其制备方法
公开(公告)号：US4238391A
公开(公告)日：1980-12-09
申请号：US58526
申请日：1979-07-18
申请人： Tomohisa Takita , Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Osamu Yoshioka , Hamao Umezawa
发明人： Tomohisa Takita , Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Osamu Yoshioka , Hamao Umezawa
IPC分类号： C07K9/00 , C07C103/52
CPC分类号： C07K9/003 , Y10S930/19 , Y10S930/27
摘要： Novel 3-[(S)-1'-phenylethylamino]propylaminobleomycin obtained by reacting a reactive derivative of the carboxyl group of bleomycinic acid with N-[(S)-1'-phenylethyl]-1,3-diaminopropane, a non-toxic salt of said novel bleomycin, and a method for producing the novel bleomycin. Because of much reduction in the side effect causing pulmonary fibrosis, the novel bleomycin is more useful than a commercial bleomycin complex which gives rise to said undesirable side effect.
摘要翻译： 通过使博来霉素酸的羧基的活性衍生物与N - [（S）-1'-苯基乙基] -1,3-二氨基丙烷反应而得到的新型3 - [（S）-1'-苯基乙基氨基] 所述新型博莱霉素的有毒盐，以及生产新型博来霉素的方法。 由于引起肺纤维化的副作用大大减少，新博莱霉素比商业博来霉素复合物更有用，这引起了不希望的副作用。
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公开(公告)号：US4267102A
公开(公告)日：1981-05-12
申请号：US126123
申请日：1980-02-29
申请人： Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Tomohisa Takita , Hamao Umezawa
发明人： Akio Fujii , Takeyo Fukuoka , Yasuhiko Muraoka , Tomohisa Takita , Hamao Umezawa
IPC分类号： C07K9/00 , C07C103/52 , A61K37/00
CPC分类号： C07K9/003 , Y10S930/19
摘要： N-methylbleomycins represented by the general formula ##STR1## which are useful as antitumor agents and bactericides; a method of preparing the same; and intermediate products in the preparation thereof.
摘要翻译： 用作抗肿瘤剂和杀菌剂的通式为“IMAGE”的N-甲基梭菌素; 其制备方法; 和中间产物的制备。
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公开(公告)号：US4326054A
公开(公告)日：1982-04-20
申请号：US167439
申请日：1980-07-09
IPC分类号： C12P17/00 , A61K31/70 , A61K31/7028 , A61P31/04 , A61P35/00 , C07H15/26 , C07K9/00 , C12P19/44 , C12P19/60 , C12R1/465 , C07H11/02 , C07H13/12
CPC分类号： C12R1/465 , C07H15/26 , C07K9/003 , C12P19/60 , Y10S930/19 , Y10S930/27
摘要： Novel antibiotics cleomycins represented by the formula ##STR1## wherein R is a terminal amino residue of the cleomycin. These compounds are useful as a chemotherapeutic agent for treating cancer and bacterial infections.
摘要翻译： 由式
表示的新型抗生素cleomycins，其中R是克霉霉素的末端氨基残基。 这些化合物可用作治疗癌症和细菌感染的化学治疗剂。 -
公开(公告)号：US3953594A
公开(公告)日：1976-04-27
申请号：US386329
申请日：1973-08-07
申请人： Hamao Umezawa , Tomohisa Takita , Yasuhiko Muraoka , Akio Fujii
发明人： Hamao Umezawa , Tomohisa Takita , Yasuhiko Muraoka , Akio Fujii
摘要： This invention is concerned with the oxidative conversion of an unstable phleomycin group to a stable bleomycin group antibiotic having the partial structure: ##SPC1##By treatment with potassium ferricyanide or manganese dioxide.
摘要翻译： 本发明涉及不稳定的腐草霉素组与具有部分结构的稳定的博来霉素抗生素的氧化转化：
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公开(公告)号：US3984390A
公开(公告)日：1976-10-05
申请号：US337575
申请日：1973-03-02
申请人： Hamao Umezawa , Akio Fujii , Tomohisa Takita , Nobuyoshi Shimada
发明人： Hamao Umezawa , Akio Fujii , Tomohisa Takita , Nobuyoshi Shimada
IPC分类号： C12P21/00 , A61K35/74 , A61K38/00 , C07D277/56 , C07H15/26 , C07K9/00 , C12P1/06 , C12P19/58 , C12R1/465 , C07C103/52
CPC分类号： C07K9/003 , Y10S435/886 , Y10S930/19
摘要： By adding a specific amine in culturing under aerobic conditions actinomycetales capable of producing phleomycin group antibiotics, which have been inoculated into a nutrient medium to produce antitumor phleomycin group antibiotics, it is possible to obtain specific phleomycin group antibiotics having a side chain structure corresponding to said amine. The phleomycin group antibiotics thus produced are collected from the culture medium in a conventional way.
摘要翻译： 通过在需氧条件下培养特定的胺，其能够产生已经接种到营养培养基中以产生抗腐霉素腐霉素组抗生素的福来霉素组抗生素的放线菌素，可以获得具有对应于所述抗生素的侧链结构的特定的腐草霉素组抗生素 胺。 以常规方式从培养基中收集由此产生的腐草霉素组抗生素。
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公开(公告)号：USRE30451E
公开(公告)日：1980-12-16
申请号：US41996
申请日：1979-05-24
申请人： Hamao Umezawa , Kenji Maeda , Tomohisa Takita , Yuya Nakayama , Akio Fujii , Nobuyoshi Shimada , Hideo Chimura
发明人： Hamao Umezawa , Kenji Maeda , Tomohisa Takita , Yuya Nakayama , Akio Fujii , Nobuyoshi Shimada , Hideo Chimura
摘要： A novel process for producing antibiotics bleomycins by innoculating and aerobically culturing in a nutrient source-containing medium a bleomycin-producing strain belonging to the actinomyces, wherein the culture is effected in the presence of an amino compound having at least one ##STR1## group and at least one basic group selected from amino, imino, guanidino, amidino and sulfonium groups and nitrogen-containing cyclic compounds, or in the presence of a compound convertible in the culture liquor to such amino compound as mentioned above, thereby selectively producing a known or novel bleomycin component corresponding to the said amino compound or to an amino compound derived from the above-mentioned compound, and then the known or novel bleomycin is recovered by known means from the culture medium.
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公开(公告)号：US3960834A
公开(公告)日：1976-06-01
申请号：US412128
申请日：1973-11-02
申请人： Hamao Umezawa , Tomohisa Takita , Akio Fujii , Hiroko Ito
发明人： Hamao Umezawa , Tomohisa Takita , Akio Fujii , Hiroko Ito
CPC分类号： C07K9/003
摘要： By thermal decomposition of 3-(S,S-dimethylmercapto)propylaminobleomycin, there is easily obtained 3-(methylmercapto)propylaminobleomycin which is a useful antibiotic substance having an extremely high antimicrobial activity and a carcinostartic activity with low toxicity.
摘要翻译： 通过3-（S，S-二甲基巯基）丙基氨基巴豆霉素的热分解，可容易地获得3-（甲基巯基）丙基氨基高双酚，其是具有极高的抗微生物活性和低毒性的致癌活性的有用的抗生素物质。
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公开(公告)号：US4240975A
公开(公告)日：1980-12-23
申请号：US79777
申请日：1979-09-26
IPC分类号： C07K5/02 , C07C69/96 , C07C101/72
CPC分类号： C07K5/02
摘要： Bestatin, which is [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, and related compounds which inhibit aminopeptidase B, leucino aminopeptidase and Bleomycin hydrolase, enhance the anti-tumor effect of Bleomycin and exhibit an antifertility effect were synthesized and tested.
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公开(公告)号：US4716221A
公开(公告)日：1987-12-29
申请号：US842286
申请日：1986-03-21
申请人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Wataru Tanaka , Tomohisa Takita , Yoshio Nishimura , Hiroshi Yoshikawa
发明人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Wataru Tanaka , Tomohisa Takita , Yoshio Nishimura , Hiroshi Yoshikawa
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P35/00 , C07H17/04 , C07H15/24
CPC分类号： C07H17/04
摘要： This invention relates to a novel 4'-demethyl-4-epipodophylltoxin derivative of the formula: ##STR1## (wherein R.sub.1 is a lower alkyl group; X.sub.1 and X.sub.2 are each a hydroxyl group or an amino group substituted by one or two lower alkyls, provided that either one of X.sub.1 and X.sub.2 is an amino group substituted by one or two lower alkyls and the other is a hydroxyl group) and salts thereof.
摘要翻译： 本发明涉及下式的新型4'-去甲基-4-表鬼臼毒素衍生物：其中R1是低级烷基; X1和X2分别是羟基或被一个或两个低级烷基取代的氨基 ，条件是X1和X2中的任一个是被一个或两个低级烷基取代的氨基，另一个是羟基）及其盐。
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