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121. 发明授权

US4453003A Process for producing threo-3-amino-2-hydroxy-butanoyl-aminoacetic acids as well as novel intermediates therefor and process for producing them 失效
公开(公告)号：US4453003A
公开(公告)日：1984-06-05
申请号：US336492
申请日：1981-12-31
申请人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
IPC分类号： A47L13/40 , A61K20060101 , A61K31/16 , A61K31/195 , C07C20060101 , C07C51/347 , C07C233/31 , C07C233/47 , C07C233/76 , C07C233/87 , C07C271/22 , C07C271/34 , C07C271/54 , C07D209/48 , C07K1/06 , C07K5/02 , C07K5/06 , C07C101/30
CPC分类号： C07C237/20 , A61K38/00 , Y02P20/55
摘要： A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: ##STR1## wherein R.sub.1 represents a naphthyl or a group of the formula: ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R.sub.2 represents a protected amino, with a starting compound represented by the general formula: ##STR3## wherein R.sub.3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: ##STR5## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: ##STR6## wherein R.sub.2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: ##STR7## wherein R.sub.4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: ##STR8## wherein R.sub.1 and R.sub.4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.

122. 发明授权

US4439603A Anthracycline derivatives of .beta.-rhodomycinone glycosides 失效
标题翻译： β-红霉素酮苷的蒽环霉素衍生物
公开(公告)号：US4439603A
公开(公告)日：1984-03-27
申请号：US436630
申请日：1982-10-25
申请人： Hamao Umezawa , Tomio Takeuchi , Tomoyuki Ishikura , Akihiro Yoshimoto , Yasue Matsuzawa , Yukio Takatsuki
发明人： Hamao Umezawa , Tomio Takeuchi , Tomoyuki Ishikura , Akihiro Yoshimoto , Yasue Matsuzawa , Yukio Takatsuki
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： New anthracycline derivatives, .beta.-rhodomycinone-RDA, .beta.-rhodomycinone-RDRs and .beta.-rhodomycinone-RD having potent anticancer activities and lower toxicities and a process for the production thereof by reduction or hydrolysis of .beta.-rhodomycinone-RDC are disclosed.
摘要翻译：公开了新的蒽环类衍生物，β-近红霉素酮-RDA，β-霉菌酮-RDR和具有较强抗癌活性和较低毒性的β-二酮霉素-RR及其通过还原或水解β-维生素D-RDC生产的方法。

123. 发明授权

US4415657A Process for preparation of an optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid 失效
标题翻译：制备β-（S） - 氨基戊二酸的光学活性单烷基酯的方法
公开(公告)号：US4415657A
公开(公告)日：1983-11-15
申请号：US328696
申请日：1981-12-08
申请人： Hamao Umezawa , Masaji Ohno , Junzo Hasegawa , Shigeki Hamaguchi , Masahiro Ogura , Hajime Kawaharada , Kiyoshi Watanabe
发明人： Hamao Umezawa , Masaji Ohno , Junzo Hasegawa , Shigeki Hamaguchi , Masahiro Ogura , Hajime Kawaharada , Kiyoshi Watanabe
IPC分类号： C12P13/04 , C07B19/02 , C12P7/62
CPC分类号： C12P13/04 , Y10S435/83 , Y10S435/832 , Y10S435/84 , Y10S435/843 , Y10S435/859 , Y10S435/872 , Y10S435/874 , Y10S435/882 , Y10S435/885 , Y10S435/911 , Y10S435/912 , Y10S435/913 , Y10S435/921 , Y10S435/929 , Y10S435/931 , Y10S435/932 , Y10S435/933 , Y10S435/938 , Y10S435/939
摘要： A process is disclosed in which an optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is prepared by subjecting a dialkyl ester of .beta.-protected aminoglutaric acid to the action of a culture broth, cells, or treated cells of a microorganism capable of stereoselectively hydrolyzing only one of the ester groups in the above-mentioned dialkyl ester to produce an optically active monoalkyl ester of .beta.-protected (S)-aminoglutaric acid, and then removing the amino-protecting group from the product. An optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is useful as a starting material for synthesizing .beta.-lactam antibiotics of carbapenem type such as thienamycin.
摘要翻译：公开了一种方法，其中β-（S） - 氨基戊二酸的光学活性单烷基酯通过使β-受保护的氨基戊二酸的二烷基酯经受培养液，细胞或能够处理的微生物的处理细胞的作用立体选择性地水解上述二烷基酯中的一个酯基，得到β-保护（S） - 氨基戊二酸的光学活性单烷基酯，然后从产物中除去氨基保护基。 β-（S） - 氨基戊二酸的光学活性单烷基酯可用作合成碳青霉烯类的β-内酰胺抗生素如噻吩霉素的起始原料。

124. 发明授权

US4391986A Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediates therefor and process for producing them 失效
标题翻译：产生苏氨酸-3-氨基-2-羟基丁酰氨基乙酸的方法以及其新型中间体及其制备方法
公开(公告)号：US4391986A
公开(公告)日：1983-07-05
申请号：US211035
申请日：1980-11-28
申请人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
IPC分类号： A47L13/40 , A61K20060101 , A61K31/16 , A61K31/195 , C07C20060101 , C07C51/347 , C07C233/31 , C07C233/47 , C07C233/76 , C07C233/87 , C07C271/22 , C07C271/34 , C07C271/54 , C07D209/48 , C07K1/06 , C07K5/02 , C07K5/06 , C07C101/34
CPC分类号： C07C237/20 , A61K38/00 , Y02P20/55
摘要： Threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its esters represented by the formula: ##STR1## wherein R.sub.1 represents naphthyl or a group of the formula ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino, an amino protected with acyl, lower alkyloxycarbonyl or carbamoyl, hydroxy or protected with acyl, lower alkyloxycarbonyl or carbamoyl, lower alkoxy, lower alkyl or phenyl group; R.sub.2 represents an amine protected with acyl, lower alkyloxycarbonyl or carbamoyl; and R.sub.3 represents hydrogen, lower alkyl having 1 to 6 carbon atoms or benzyl.
摘要翻译： Threo-3保护的氨基-2-羟基-4-氧代丁酸或其由下式表示的酯：其中R 1表示萘基或式（VI）的基团，其中R 6和R 7分别表示氢，卤素，氨基，被酰基保护的氨基，低级烷氧基羰基或氨基甲酰基，羟基或用酰基保护，低级烷氧基羰基或氨基甲酰基，低级烷氧基，低级烷基或苯基; R2代表被酰基，低级烷氧基羰基或氨基甲酰基保护的胺; 并且R 3表示氢，具有1至6个碳原子的低级烷基或苄基。

125. 发明授权

US4370318A Bestatin-related compounds as immunopotentiator 失效
标题翻译：美白素相关化合物作为免疫增强剂
公开(公告)号：US4370318A
公开(公告)日：1983-01-25
申请号：US272211
申请日：1981-06-10
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Kenji Kawamura , Shunzo Fukatsu
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Kenji Kawamura , Shunzo Fukatsu
IPC分类号： A61K31/135 , A61K31/16 , A61K31/195 , C07K5/02 , A61K37/00 , A61K31/165
CPC分类号： A61K31/135 , A61K31/16 , A61K31/195 , C07K5/0202
摘要： 3-Amino-2-hydroxy-4-phenylbutanoic acid and esters thereof as well as new derivatives thereof which are related to bestatin in their chemical structure are active to enhance the immune response in living animals.
摘要翻译： 3-氨基-2-羟基-4-苯基丁酸及其酯及其与衍生物在其化学结构中相关的新衍生物是有活性的以增强活体动物的免疫应答。

126. 发明授权

US4357465A 3',4'-Diedeoxykanamycin B derivatives 失效
标题翻译： 3'，4'-脱氧卡那霉素B衍生物
公开(公告)号：US4357465A
公开(公告)日：1982-11-02
申请号：US187014
申请日：1980-09-15
申请人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
发明人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
IPC分类号： C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.
摘要翻译：提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

127. 发明授权

US4335250A Compound with immunopotentiating activity and production and uses thereof 失效
标题翻译：具有免疫增强活性的化合物及其制备及其应用
公开(公告)号：US4335250A
公开(公告)日：1982-06-15
申请号：US57014
申请日：1979-07-12
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Masaaki Ishizuka , Hajime Morishima , Takuzo Yamamoto , Junji Yoshizawa , Masaaki Hosoi , Ikuo Matsumoto
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Masaaki Ishizuka , Hajime Morishima , Takuzo Yamamoto , Junji Yoshizawa , Masaaki Hosoi , Ikuo Matsumoto
IPC分类号： C07C69/88 , A61K31/19 , A61K31/235 , A61P37/04 , C07C51/00 , C07C51/09 , C07C65/01 , C07C65/03 , C07C67/00 , C07C69/84
CPC分类号： C07C65/03 , C07C65/01 , Y10S514/885
摘要： A new compound is produced which has the general formula: ##STR1## wherein R represents hydrogen atom or a lower alkyl group and which exhibits an immunopotentiating activity. This new compound as well as its pharmaceutically acceptable salts and hydrates are useful for immunotherapy and treatment of immune diseases and disorders in living animals including human beings. The new compound can be produced by reduction of a hydroxyterephthalic acid alkyl ester or by esterification of the corresponding 3-hydroxy-4-(hydroxymethyl)-benzoic acid.
摘要翻译：制备了具有以下通式的新化合物：其中R表示氢原子或低级烷基，并表现出免疫增强活性。该新化合物及其药学上可接受的盐和水合物可用于免疫治疗和治疗包括人在内的活动物中的免疫疾病和病症。新化合物可以通过还原羟基对苯二甲酸烷基酯或通过相应的3-羟基-4-（羟甲基） - 苯甲酸的酯化来制备。

128. 发明授权

US4332794A 6"-Deoxydibekacin, 4",6"-dideoxydibekacin and 1-N-aminoacyl derivatives thereof, and the production of these new compounds 失效
标题翻译： 6“ - 脱氧贝卡辛，4”，6“ - 双脱氧衣壳蛋白及其1-N-氨基酰基衍生物，以及这些新化合物的生产
公开(公告)号：US4332794A
公开(公告)日：1982-06-01
申请号：US174630
申请日：1980-08-01
申请人： Hamao Umezawa , Shinichi Kondo
发明人： Hamao Umezawa , Shinichi Kondo
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： New compounds, 6"-deoxydibekacin, 4", 6"-dideoxydibekacin, 1-N-(L-4-amino-2-hydroxybutyryl)-6"-deoxydibekacin and 1-N-(L-4-amino-2-hydroxybutyryl)-4",6"-dideoxydibekacin are now produced semi-synthetically from dibekacin, i.e. 3',4'-dideoxykanamycin B. These four new compounds are each useful as an antibacterial agent. Production of 6"-deoxydibekacin or 4",6"-dideoxydibekacin is made by removal of the 6"-hydroxyl group or by removal of the 4"- and 6"-hydroxyl groups from an amino-protected and hydroxyl-protected derivative of dibekacin. Production of 1-N-(L-4-amino-2-hydroxybutyryl)-6"-deoxydibekacin or -4",6"-dideoxydibekacin is made by acylating the 1-amino group of 6"-deoxydibekacin or 4",6"-dideoxydibekacin with the L-4-amino-2-hydroxybutyryl group, or alternatively by removal of the 6"-hydroxyl group or the 4"- and 6"-hydroxyl groups from a known compound, 1-N-(L-4-amino-2-hydroxybutyryl)-dibekacin.
摘要翻译：新化合物6“ - 脱氧胆碱，4”，6“ - 脱氧倍半萜烯，1-N-（L-4-氨基-2-羟基丁酰基）-6”脱氧胆球蛋白和1-N-（L-4- 氨基-2-羟基丁酰基）-4“，6” - 双脱氧半乳糖素现在由二卡辛（即3'，4'-双脱氧卡那霉素B）半合成制备。这四种新化合物各自用作抗菌剂。通过除去6“ - 羟基或通过从氨基保护基中除去4”和6“ - 羟基而制备6” - 脱氧双蝎子或4“，6” - 双脱氧贝克辛和二羟脯氨酸的羟基保护衍生物。 1-N-（L-4-氨基-2-羟基丁酰基）-6“ - 脱氧胆球蛋白或-4”，6“ - 脱氧倍半萜烯的制备是通过酰化6” - 脱氧胆碱的1-氨基或 4“，6” - 双脱氧贝克辛与L-4-氨基-2-羟基丁酰基，或者通过从已知的步骤中除去6“ - 羟基或4”和6“ - 羟基化合物，1-N-（L-4-氨基-2-羟基丁酰基） - 二酮。

129. 发明授权

US4303785A Antitumor anthracycline antibiotics 失效
标题翻译：抗蒽环类抗生素
公开(公告)号：US4303785A
公开(公告)日：1981-12-01
申请号：US117163
申请日：1980-01-31
申请人： Hamao Umezawa , Tomio Takeuchi , Hiroshi Naganawa , Kuniaki Tatsuta
发明人： Hamao Umezawa , Tomio Takeuchi , Hiroshi Naganawa , Kuniaki Tatsuta
IPC分类号： C07H15/252 , C07H15/24 , A61K31/71
CPC分类号： C07H15/252
摘要： New anthracycline derivatives of adriamycin and daunomycin prepared by the etherification of the C-4' and/or C-14 hydroxyl groups of the starting material glycosides are found to be useful antimicrobial and antitumor agents.
摘要翻译：发现通过起始物质糖苷的C-4'和/或C-14羟基的醚化制备的阿霉素和道诺霉素的新蒽环类衍生物是有用的抗微生物剂和抗肿瘤剂。

130. 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。

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