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21. 发明授权

US4781977A Cyclodextrin adsorbing-material 失效
标题翻译：环糊精吸附材料
公开(公告)号：US4781977A
公开(公告)日：1988-11-01
申请号：US925264
申请日：1986-10-31
申请人： Yoshiaki Yagi , Kenichi Yamamoto , Yukio Tsuchiyama , Michikatsu Sato , Kouki Fujii , Tomoyuki Ishikura
发明人： Yoshiaki Yagi , Kenichi Yamamoto , Yukio Tsuchiyama , Michikatsu Sato , Kouki Fujii , Tomoyuki Ishikura
IPC分类号： B01J20/26 , B01D15/00 , B01J20/24 , B01J20/281 , B01J20/32 , C08B37/16 , G01N30/88
CPC分类号： C08B37/0012 , B01J20/261 , B01J20/262 , B01J20/267 , B01J20/28016 , B01J20/289 , B01J20/3092 , B01J20/321 , B01J20/3212 , B01J20/3217 , B01J20/3219 , B01J20/3221 , B01J20/3248 , B01J20/3251 , B01J20/3253 , B01J20/3255 , B01J2220/54 , B01J2220/58 , Y10T428/26 , Y10T428/2991 , Y10T428/31971
摘要： A cyclodextrin adsorbing material composed of a water-insoluble resin substrate to which a ligand having such a size as to be included by cyclodextrin is chemically bonded via a spacer radical; a method of separating and purifying cyclodextrin from an aqueous solution containing it, which comprises bringing said aqueous solution into contact with the above adsorbing material to adsorb cyclodextrin on the adsorbing material, and subjecting the adsorbing material to a desorption treatment to recover cyclodextrin; and a method of increasing the amount of cyclodextrin yielded, which comprises carrying out a cyclodextrin-forming reaction by an enzymatic method in the presence of the above adsorbent material.
摘要翻译：由水不溶性树脂基材构成的环糊精吸附材料，其中具有由环糊精包含的尺寸的配体通过间隔基团化学键合; 从含有它的水溶液中分离和纯化环糊精的方法，其包括使所述水溶液与上述吸附材料接触以将环糊精吸附在吸附材料上，并对吸附材料进行解吸处理以回收环糊精; 以及增加产生的环糊精的量的方法，其包括在上述吸附材料的存在下通过酶法进行环糊精形成反应。

22. 发明授权

US4778883A 3-(CHFCH.sub.3)-azetidinone intermediates 失效
标题翻译： 3-（CHFCH 3） - 氮杂环丁酮中间体
公开(公告)号：US4778883A
公开(公告)日：1988-10-18
申请号：US16106
申请日：1987-02-18
申请人： Takeo Yoshioka , Noritaka Chida , Azuma Watanabe , Yasuo Fukagawa , Tomoyuki Ishikura
发明人： Takeo Yoshioka , Noritaka Chida , Azuma Watanabe , Yasuo Fukagawa , Tomoyuki Ishikura
IPC分类号： C07D205/08 , C07B39/00 , C07D405/04 , C07F7/10
CPC分类号： C07D205/08 , Y02P20/55
摘要： An azetidinone derivative of the formula ##STR1## wherein R.sub.1 represents a formyl group, a carboxyl group, an acetyloxy group or a group of the formula ##STR2## in which R.sub.2 and R.sub.3 each represent a lower alkyl group or together represent a lower alkylene group, and Z represents a hydrogen atom or an amino-protecting group.
摘要翻译：式（I）的氮杂环丁酮衍生物，其中R 1表示甲酰基，羧基，乙酰氧基或式“IMAGE”的基团，其中R 2和R 3各自表示低级烷基或一起表示低级亚烷基，Z表示氢原子或氨基保护基。

23. 发明授权

US4528397A Aminocarboxylic acid derivatives 失效
标题翻译：氨基羧酸衍生物
公开(公告)号：US4528397A
公开(公告)日：1985-07-09
申请号：US479982
申请日：1983-03-29
申请人： Norio Shibamoto , Takeo Yoshioka , Yasuo Fukagawa , Tomoyuki Ishikura
发明人： Norio Shibamoto , Takeo Yoshioka , Yasuo Fukagawa , Tomoyuki Ishikura
IPC分类号： C12N9/99 , A61K31/19 , A61K31/195 , A61K31/40 , A61P43/00 , C07C67/00 , C07C229/16 , C07C313/00 , C07C323/51 , C07C323/52 , C07D209/48 , C07C101/24
CPC分类号： C07D209/48 , A61K31/40 , C07C323/51
摘要： An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.
摘要翻译：由式（Ia）表示的氨基羧酸衍生物，其中R1和R2彼此独立地表示氢原子或可具有取代基的烷基，Y表示-NH-或-S-，提供当Y表示-NH-时，R 1和R 2中的至少一个表示可以具有取代基的烷基。这些化合物对动物中的二肽酶具有优异的抑制活性，并且可用于与碳青霉烯类抗生素组合施用。

24. 发明授权

US4474945A Anthracycline antibiotics 失效
标题翻译：蒽环类抗生素
公开(公告)号：US4474945A
公开(公告)日：1984-10-02
申请号：US405917
申请日：1982-08-06
申请人： Akihiro Yoshimoto , Hiroyasu Tobe , Tomoyuki Ishikura , Hamao Umezawa , Tomio Takeuchi
发明人： Akihiro Yoshimoto , Hiroyasu Tobe , Tomoyuki Ishikura , Hamao Umezawa , Tomio Takeuchi
IPC分类号： C07H15/252 , C12P19/56 , C07H17/08 , C12N1/00 , C12P19/62
CPC分类号： C07H15/252 , C12P19/56 , C12R1/465 , Y10S514/908
摘要： New anthracycline compounds, 2-hydroxyaclacinomycin B having potent antitumor activity and lower toxicity, and a process for producing 2-hydroxyaclacinomycins A, B, and N by fermentation.
摘要翻译：新的蒽环类化合物，具有有效抗肿瘤活性和较低毒性的2-羟基阿拉伯霉素B，以及通过发酵生产2-羟基卡曲霉素A，B和N的方法。

25. 发明授权

US4368203A Antibiotics and derivatives thereof having .beta.-lactamase inhibitory activity and production thereof 失效
标题翻译：具有β-内酰胺酶抑制活性的抗生素及其衍生物及其生产
公开(公告)号：US4368203A
公开(公告)日：1983-01-11
申请号：US949854
申请日：1978-10-10
申请人： Kazuhiko Okamura , Shoji Hirata , Yasushi Okumura , Yasuo Fukagawa , Yasutaka Shimauchi , Tomoyuki Ishikura , Kageaki Kouno , Joseph Lein
发明人： Kazuhiko Okamura , Shoji Hirata , Yasushi Okumura , Yasuo Fukagawa , Yasutaka Shimauchi , Tomoyuki Ishikura , Kageaki Kouno , Joseph Lein
IPC分类号： C12P1/06 , C07D477/20 , C12R1/465 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20
摘要： A novel antibiotic substance of the formula ##STR1## wherein R.sub.1 is CH.sub.3 and R.sub.2 is --CH.sub.2 --CH.sub.2 -- or R.sub.1 is H and R.sub.2 is --CH.dbd.CH--; and R.sub.3 represents hydrogen, lower alkyl or triphenylmethyl,and including the salts of the compound of formula (I) wherein R.sub.3 is hydrogen, said antibiotic substance having strong antibiotic activity and .beta.-lactamase inhibiting effect, and a method for producing the same by aerobic cultivation of Streptomyces A271.
摘要翻译：式（Ⅰ）的新型抗生素物质，其中R 1为CH 3且R 2为-CH 2 -CH 2 - 或R 1为H且R 2为-CH = CH-; 并且R 3表示氢，低级烷基或三苯基甲基，并且包括其中R 3是氢的式（I）化合物的盐，所述抗生素具有很强的抗生素活性和β-内酰胺酶抑制作用的方法及其生产方法培养链霉菌A271。

26. 发明授权

US4337199A Antibiotic .beta.-lactam compounds, production thereof, and their use as antimicrobial agent 失效
标题翻译：抗生素β-内酰胺化合物，其制备及其作为抗微生物剂的用途
公开(公告)号：US4337199A
公开(公告)日：1982-06-29
申请号：US147146
申请日：1980-05-06
申请人： Takeo Yoshioka , Kenichi Yamamoto , Kaoru Yamada , Yasuyuki Kato , Yasutaka Shimauchi , Tomoyuki Ishikura
发明人： Takeo Yoshioka , Kenichi Yamamoto , Kaoru Yamada , Yasuyuki Kato , Yasutaka Shimauchi , Tomoyuki Ishikura
IPC分类号： C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20
摘要： Novel antibiotic .beta.-lactam compounds, i.e. 7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid derivatives of the following formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or a hydroxyl group,R.sub.2 represents a lower alkyl group, a hydroxy lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group, a cyclohexyl group, a phenyl group or a 5- or 6-membered aromatic heterocyclic group containing 1 or 2 nitrogen atoms, andR.sub.3 represents a hydrogen atom, a lower alkyl group, or a substituted or unsubstituted aralkyl group containing 7 to 20 carbon atoms,and the salts thereof; processes for production thereof; use thereof as antimicrobial agents; and novel intermediates for production of the compounds of formula (I).
摘要翻译：新颖的抗生素β-内酰胺化合物，即下式的7-氧代-1-氮杂双环（3.2.0）庚-2-烯-2-羧酸衍生物其中R1代表氢原子，甲基基团或羟基，R2表示低级烷基，羟基低级烷基，低级烷氧基 - 低级烷基，低级烷酰氧基 - 低级烷基，环己基，苯基或5-或6-元含有1或2个氮原子的芳族杂环基，R 3表示氢原子，低级烷基或取代或未取代的含有7〜20个碳原子的芳烷基及其盐; 生产过程; 其用作抗微生物剂; 和用于制备式（I）化合物的新型中间体。

27. 发明授权

US4746734A Partially methylated cyclodextrins and process for producing the same 失效
标题翻译：部分甲基化环糊精及其制备方法
公开(公告)号：US4746734A
公开(公告)日：1988-05-24
申请号：US20250
申请日：1987-02-27
申请人： Yukio Tsuchiyama , Michikatsu Sato , Yoshiaki Yagi , Tomoyuki Ishikura
发明人： Yukio Tsuchiyama , Michikatsu Sato , Yoshiaki Yagi , Tomoyuki Ishikura
IPC分类号： C08B37/16 , C08B37/00
CPC分类号： C08B37/0012
摘要： Partially methylated cyclodextrins with enhanced solubility in water have an average degree of methylation of hydroxyl groups at different positions in all the glucose units involved of about 53-64% for the 2-position, about 38-51% for the 3-position and about 70-100% for the 6-position. The partially methylated cyclodextrins are prepared by reacting .beta.-cyclodextrin with more than about 30 equivalent proportions based on the .beta.-cyclodextrin of dimethyl sulfate and more than about 30 equivalent proportions of an alkali metal hydroxide, wherein the concentration of reactants is greater than 10% (wt/wt).
摘要翻译：在水中具有增强的溶解度的部分甲基化的环糊精具有平均甲基化度，所有葡萄糖单位中的不同位置的羟基在2-位上约为53-64％，3-位和约3〜 70％至6％的位置。部分甲基化的环糊精通过使β-环糊精与基于硫酸二甲酯的β-环糊精和超过约30当量比例的碱金属氢氧化物的超过约30当量的比例反应来制备，其中反应物的浓度大于10％（wt / wt）。

28. 发明授权

US4612371A Anthracycline antibiotics 失效
标题翻译：蒽环类抗生素
公开(公告)号：US4612371A
公开(公告)日：1986-09-16
申请号：US756876
申请日：1985-07-18
申请人： Akihiro Yoshimoto , Shizuka Fujii , Katsuro Kubo , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
发明人： Akihiro Yoshimoto , Shizuka Fujii , Katsuro Kubo , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , C07H15/24
CPC分类号： C07H15/252
摘要： Novel anthracycline antibiotics characteristic of Ring A of the anthracycline skeleton are produced by microorganisms belonging to the genus Streptomyces and are useful as anti-cancer agents. The antibiotics designated D-788-6 to -10 are shown by general formula: ##STR1## wherein Y represents a group shown by: ##STR2##
摘要翻译：蒽环霉素骨架A环特征的新型蒽环类抗生素由属于链霉菌属的微生物产生，可用作抗癌剂。称为D-788-6至-10的抗生素由以下通式表示：其中Y代表如下所示的基团：

29. 发明授权

US4463171A Derivatives of macrolide antibiotics 失效
标题翻译：大环内酯类抗生素衍生物
公开(公告)号：US4463171A
公开(公告)日：1984-07-31
申请号：US502480
申请日：1983-06-09
申请人： Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
发明人： Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkanoyl group;R.sup.3 represents a hydrogen atom or the group --COCH.sub.2 R.sup.5 in which R.sup.5 represents a lower alkyl group or an aryl or pyridyl group bonded through a sulfur atom;R.sup.4 represents a methyl group which may be substituted by aryl, pyridyl, pyridylthio, hydroxyl or arylthioamino, an aryl group, a nitrile group, a 5- or 6-membered heterocyclic group having 1 to 4 hetero atoms selected from nitrogen and sulfur atoms, or a tetrahydropyranyl group which may be substituted by methoxy;A represents the group --OCO--, --OSO.sub.2 --, --O-- or --S--, or A and R.sup.4, taken together, represent a halogen atom, a nitrile group or a group of the formula ##STR2## in which R.sup.6 represents two lower alkyl groups, the group ##STR3## or an alkylene group having 4 to 6 carbon atoms which may have in the chain an oxygen atom or a lower alkyl-substituted nitrogen atom; and said aryl group and heterocyclic group may optionally be substituted by a methyl, methoxy or nitro group, and when R.sup.1 represents a lower alkyl group,R.sup.3 does not represent a lower alkyl group,or their salts.These novel derivatives of macrolide antibiotics have excellent antibacterial activity.
摘要翻译：下列通式的化合物：其中R 1和R 2表示氢原子或低级烷酰基; R3表示氢原子或基团-COCH2R5，其中R5表示低级烷基或通过硫原子键合的芳基或吡啶基; R 4表示可以被芳基，吡啶基，吡啶硫基，羟基或芳硫基氨基，芳基，腈基，具有1-4个选自氮和硫原子的杂原子的5或6元杂环基取代的甲基，或可被甲氧基取代的四氢吡喃基; A代表基团-OCO-，-OSO 2 - ， - O-或-S-，或A和R 4一起代表卤素原子，腈基或式（IMAGE）基团，其中R6代表二低级烷基，基团或具有4-6个碳原子的亚烷基，其可以在链中具有氧原子或低级烷基取代的氮原子; 并且所述芳基和杂环基可任选被甲基，甲氧基或硝基取代，并且当R 1表示低级烷基时，R 3不表示低级烷基或其盐。这些大环内酯类抗生素的新型衍生物具有优良的抗菌活性。

30. 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。

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