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1. 发明授权

US4795743A 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives of low toxicity 失效
标题翻译： 2'-脱氨基-2'-羟基马斯汀Bo衍生物低毒
公开(公告)号：US4795743A
公开(公告)日：1989-01-03
申请号：US21781
申请日：1987-03-04
申请人： Yoshiro Okami , Shinichi Kondo , Daishiro Ikeda , Hamao Umezawa, deceased
发明人： Yoshiro Okami , Shinichi Kondo , Daishiro Ikeda , Hamao Umezawa, deceased
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/222 , C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.
摘要翻译：作为新的2'-脱氨基-2'-羟基毛霉素Bo衍生物，提供四种化合物，即2'-脱氨基-2'-羟基毛霉素B; 2'-脱氨基-2'-羟基-3-O-脱甲基霉素B; 4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基毛霉素Bo; 和4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基-3-O-脱甲基丝杆霉素B B，其组合表现出高的抗菌活性和低的急性毒性。这些新化合物可用作抗菌剂。

2. 发明授权

US4499083A 3-O-Demethyl derivatives of the istamycin B series of compounds 失效
标题翻译：伊曲霉素B系列化合物的3-O-去甲基衍生物
公开(公告)号：US4499083A
公开(公告)日：1985-02-12
申请号：US298844
申请日：1981-09-03
申请人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
发明人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
IPC分类号： C12P19/48 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/00 , C07H15/224 , C12R1/465 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224 , Y02P20/55
摘要： New derivatives of the istamycin B series of compounds are provided, which are 3-O-demethylistamycin B.sub.O, 3-O-demethylistamycin B and 3-O-demethyl-2"-N-formimidoylistamycin B represented generally by Formula I or specifically by Formulae Ia, Ib and Ic, respectively. Compound Ia is useful as an intermediate for the preparation of Compounds Ib and Ic and the latter two compounds exhibit a high antibacterial activity against a wide variety of Gram-positive and Gram-negative bacteria and are useful antibiotics. Also provided are processes for the preparation of the new derivatives starting from istamycin B.sub.O.
摘要翻译：提供了伊曲霉素B系列化合物的新衍生物，它们是通常由式I表示的3-O-脱甲基霉素B B，3-O-脱甲基霉素B和3-O-脱甲基-2'-N-甲亚氨基硫杆菌素B. 式Ia，Ib和Ic。化合物Ia可用作制备化合物Ib和Ic的中间体，后两种化合物对各种革兰氏阳性和革兰氏阴性细菌表现出高抗菌活性，并且是有用的抗生素。还提供了从伊曲霉素BO开始制备新衍生物的方法。

3. 发明授权

US4296106A Istamycins and production thereof 失效
标题翻译：伊曲霉素及其生产
公开(公告)号：US4296106A
公开(公告)日：1981-10-20
申请号：US141492
申请日：1980-04-18
申请人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
发明人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
IPC分类号： C07H15/224 , C12P19/48 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224 , C12P19/48 , C12R1/465
摘要： Four new antibiotics which are denominated istamycin A, istamycin B, istamycin A.sub.o and istamycin B.sub.o, and which are useful as antibacterial agents, are produced by fermentation of a new microorganism, Streptomyces tenjimariensis.
摘要翻译：以新霉素Streptomyces tenjimariensis的发酵产生的四种新型抗生素，其为Isim霉素A，伊曲霉素B，伊曲霉素Ao和伊曲霉素Bb，可用作抗菌剂。

4. 发明授权

US4382926A Formimidoyl A and B useful as semi-synthetic aminoglycosidic antibiotics 失效
标题翻译：亚胺酰基A和B可用作半合成氨基糖苷类抗生素
公开(公告)号：US4382926A
公开(公告)日：1983-05-10
申请号：US244232
申请日：1981-03-16
申请人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
发明人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： New, useful derivatives of istamycins A and B are provided, which are formimidoylistamycins A and B of formula (I) having a toxicity significantly lower than those of istamycins A and B with an antibacterial activity higher than that of fortimicin A and of the same level as those of istamycins A and B. These compounds may be prepared by reacting 1,2',6'-tri-N-protected istamycins A and B of formula (V) with an iminoether.
摘要翻译：提供了伊曲霉素A和B的新的有用的衍生物，其是式（I）的甲酰氨基丝氨酸霉素A和B，其毒性显着低于伊曲霉素A和B的抗菌活性高于苦味霉素A和相同水平这些化合物可以通过使式（V）的1,2'，6'-三-N-保护的伊曲霉素A和B与亚氨基醚反应来制备。

5. 发明授权

US4380581A Istamycins and streptomyces culture for the production thereof 失效
标题翻译：伊曲霉素和链霉菌培养物用于生产
公开(公告)号：US4380581A
公开(公告)日：1983-04-19
申请号：US231640
申请日：1981-02-05
申请人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
发明人： Hamao Umezawa , Yoshiro Okami , Shinichi Kondo
IPC分类号： C07H15/224 , C12P19/48 , C12N1/20 , C12R1/465
CPC分类号： C07H15/224 , C12P19/48 , C12R1/465 , Y10S435/886
摘要： Four new antibiotics which are denominated istamycin A, istamycin B, istamycin A.sub.o and istamycin B.sub.o, and which are useful as antibacterial agents, are produced by fermentation of a new microorganism, Streptomyces tenjimariensis.
摘要翻译：以新霉素Streptomyces tenjimariensis的发酵产生的四种新型抗生素，其为伊曲霉素A，伊曲霉素B，伊曲霉素Ao和伊曲霉素Bo，其可用作抗菌剂。

6. 发明授权

US4052449A Biologically active substance, bestatin, and production thereof 失效
标题翻译：生物活性物质，贝沙坦及其生产
公开(公告)号：US4052449A
公开(公告)日：1977-10-04
申请号：US690457
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 , C07C101/72
CPC分类号： C12P13/04 , C12P21/02
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).

7. 发明授权

US4029547A Biologically active substance, bestatin, and production thereof 失效
标题翻译：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）。

8. 发明授权

US4870172A Bisucaberin 失效
公开(公告)号：US4870172A
公开(公告)日：1989-09-26
申请号：US74369
申请日：1987-07-16
申请人： Yoshiro Okami , Shogo Kurasawa , Toshiyuki Kamayama , Atsushi Takahashi , Masaaki Ishizuka , Hamao Umezawa, deceased
发明人： Yoshiro Okami , Shogo Kurasawa , Toshiyuki Kamayama , Atsushi Takahashi , Masaaki Ishizuka , Hamao Umezawa, deceased
IPC分类号： A61K31/395 , A61P35/00 , C07D257/02 , C12P17/10 , C12R1/01
CPC分类号： C12R1/01 , C07D257/02 , C12P17/10
摘要： A novel compound having anti-tumor activity is disclosed which is 1,12-dihydroxy-1,6,12,17-tetraazacyclodocosan-2,5,13,16-tetrone produced microbiologically by culturing a microorganism belonging to the genus of Alteromonas or, in particular, Alteromonas haloplanktis SB-1123. The characterization data of the compound and the microbiological properties of the microorganism are described. The results of in vitro assays are given for the anti-tumor activity of the compound against L-1210 and IMC carcinoma cells.

9. 发明授权

US4179573A (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid 失效
标题翻译：（2S，3R）-3-氨基-2-羟基-4-苯基丁酸
公开(公告)号：US4179573A
公开(公告)日：1979-12-18
申请号：US825997
申请日：1977-08-19
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 , C07C101/72
CPC分类号： C12P21/02 , C12P13/04
摘要： This invention provides the amino acid (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid which is prepared by hydrolysis of bestatin. Bestatin is a chemical 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, has the following structure ##STR1## and is prepared by 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：本发明提供通过水解苦参碱制备的氨基酸（2S，3R）-3-氨基-2-羟基-4-苯基丁酸。美白汀是抑制氨肽酶B，亮氨酸氨基肽酶和博来霉素水解酶的化学物质，增强了博莱霉素的抗肿瘤作用，具有化学名称[（2S，3R）-3-氨基-2-羟基-4-苯基丁酰] -L-亮氨酸，具有以下结构，并且通过培养在需氧条件下在营养培养基中产生普拉汀的链霉菌菌株制备，直到对所述培养的培养基赋予对氨基肽酶B的抑制作用，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）。

10. 发明授权

US08580544B2 Apparatus for introducing biological material, method of introducing biological material and magnetic support for introducing biological material 失效
标题翻译：用于引入生物材料的装置，引入生物材料的方法和用于引入生物材料的磁性支持物
公开(公告)号：US08580544B2
公开(公告)日：2013-11-12
申请号：US10531520
申请日：2003-10-16
申请人： Hideji Tajima , Yoshiro Okami
发明人： Hideji Tajima , Yoshiro Okami
IPC分类号： C12N13/00 , C12N15/74
CPC分类号： C12N15/64 , C12M35/02 , C12N13/00 , C12N15/87 , C12N15/895 , Y10T428/2982
摘要： The invention relates to an apparatus for introducing a biological material, a method of introducing a biological material, and a magnetic support for introducing a biological material with the object of providing an apparatus for introducing a biological material, a method of introducing a biological material, and a magnetic support for introducing a biological material whereby a biological material can be efficiently introduced into a host.The invention comprises: one or more packing units in which a mixture solution containing a large number of magnetic supports carrying a biological material to be introduced into a host such as cells upon using, together with a large number of the hosts in a liquid is pooled; and an introduction treatment unit in which a magnetic force affecting the inside of the packing unit is controlled so as to move the magnetic supports relatively with respect to the host so that the biological material can be introduced into the host.
摘要翻译：本发明涉及一种用于引入生物材料的装置，引入生物材料的方法和用于引入生物材料的磁性载体，其目的是提供用于引入生物材料的装置，引入生物材料的方法，以及用于引入生物材料的磁性载体，由此可以将生物材料有效地引入主体。本发明包括：一个或多个填充单元，其中将含有大量磁性载体的混合溶液与大量主体在液体中一起被收集，所述混合溶液在使用时携带携带待引入主体如细胞的生物材料的混合溶液 ; 以及引导处理单元，其中控制影响包装单元内部的磁力，以相对于主机移动磁性支架，使得生物材料可以被引入到主机中。

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