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1. 发明授权

US4326054A Cleomycins and process for producing same 失效
标题翻译：克莱霉素及其生产方法
公开(公告)号：US4326054A
公开(公告)日：1982-04-20
申请号：US167439
申请日：1980-07-09
申请人： Hamao Umezawa , Tomohisa Takita , Akio Fujii , Yasuhiko Muraoka , Mamoru Kunishima
发明人： Hamao Umezawa , Tomohisa Takita , Akio Fujii , Yasuhiko Muraoka , Mamoru Kunishima
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。

2. 发明授权

US4195018A 3-[(S)-1'-Phenylethylamino]propylaminobleomycin, non-toxic salt thereof, and method for producing same 失效
标题翻译： 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。

3. 发明授权

US3953594A Process for preparing bleomycin group antibiotics 失效
标题翻译：博莱霉素组抗生素的制备方法
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
IPC分类号： C07H15/26 , C07K9/00
CPC分类号： C07H15/26 , C07K9/003
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：

4. 发明授权

US4267102A Bleomycin group antibiotics 失效
标题翻译：博来霉素组抗生素
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。

5. 发明授权

US4238391A 3-[(S)-1'-phenylethylamino]propylaminobleomycin, non-toxic salt thereof, and method for producing same 失效
标题翻译： 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。

6. 发明授权

US3984390A Novel process for producing phleomycin group antibiotics 失效
标题翻译：生产腐草霉素抗生素的新方法
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。

7. 再颁专利

USRE30451E Novel process for producing antibiotics bleomycin 失效
标题翻译：生产抗生素博莱霉素的新方法
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
IPC分类号： C07H15/26 , C07K9/00
CPC分类号： C07K9/003 , C07H15/26
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.

8. 发明授权

US3960834A Method for preparing 3-(methylmercaptol) propylaminobleomycin 失效
标题翻译：制备3-（甲基巯基丙基）丙基氨基高杆菌素的方法
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
IPC分类号： C07K9/00 , C07H7/06
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。

9. 发明授权

US4808703A Novel 3-(4'-aminobutylamino) propylaminobleomycin derivatives 失效
标题翻译：新型3-（4'-氨基丁基氨基）丙基氨基倍半霉素衍生物
公开(公告)号：US4808703A
公开(公告)日：1989-02-28
申请号：US622884
申请日：1984-06-21
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P31/04 , A61P35/00 , C07K9/00 , C07C103/52
CPC分类号： C07K9/003
摘要： Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.sub.4 each represents (i) a hydrogen atom, (ii) an alkyl group having 5 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms and a benzyloxy group, with the proviso that at least one of R.sub.3 and R.sub.4 is a group other than a hydrogen atom, and salt thereof.
摘要翻译：公开了具有低肺毒性的3-（4'-氨基丁基氨基）丙基氨基巴豆霉素，其由以下通式[BX] -NH-（CH 2）3 -A-（CH 2）4 -B表示，其中[BX]表示残基在从博来霉素酸的羧基中除去羟基后残留，A代表式为“IMAGE”的基团，其中R1表示（i）氢原子，（ii）具有1-10个碳原子的烷基或（ iii）可以被苯基和具有5至13个碳原子的环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个选自下列的取代基中的一个或多个取代基取代：卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基; 并且R 2表示具有1至4个碳原子的低级烷基或苄基，B表示下式的基团：其中R 3和R 4各自表示（i）氢原子，（ii）具有5个至少10个碳原子，或（iii）可以被苯基和环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个取代基取代，所述取代基选自：卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基，条件是R3和R4中的至少一个为氢原子以外的基团，及其盐。

10. 发明授权

US4568490A Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
标题翻译：氨丙基氨基甜菜碱素衍生物及其制备方法
公开(公告)号：US4568490A
公开(公告)日：1986-02-04
申请号：US743738
申请日：1985-06-12
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07K9/00
CPC分类号： C07K9/003 , Y10S930/19 , Y10S930/27
摘要： An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.
摘要翻译：由下式表示的氨基丙基氨基伯合珠霉素或其盐，其在副作用如肺毒性中最小化：[BX] -NH-（CH2）3-A-）CH2）3-B其中[BX]表示酰基通过从所述酸的羧基除去羟基，其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团，R 2为低级烷基或苄基，R为低级亚烷基，n为0或1; 并且B代表下式的基团：其中（i）R3是氢，R4是（a）被一个或多个卤素原子取代的苄基，条件是当R 1是低级烷基时，苄基被两个卤原子取代，（（c）由氰基，两个或多个烷氧基或两个或更多个苄氧基取代的苄基，（c）被环烷基或蒽基取代的低级烷基，（d）被一个或多个卤素原子取代的苯基乙基，或（e）二苯基乙基; 或（ii）R 3和R 4均为可被一个或多个（a）苄氧基取代的苄基，（b）环取代的苄氧基，其中环取代基可以是一个或多个卤素原子，低级烷氧基或苄氧基，或（c）环烷基甲氧基; 及其制备方法。

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