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32 条记录 (耗时 0.025 秒)

    Partially methylated cyclodextrins and process for producing the same
    2.
    发明授权
    Partially methylated cyclodextrins and process for producing the same 失效
    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）。

    Antibiotic .beta.-lactam compounds, production thereof, and their use as antimicrobial agent
    4.
    发明授权
    Antibiotic .beta.-lactam compounds, production thereof, and their use as antimicrobial agent 失效
    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。

    Anthracycline antibiotics
    5.
    发明授权
    Anthracycline antibiotics 失效
    蒽环类抗生素

    公开(公告)号：US4918172A

    公开(公告)日：1990-04-17

    申请号：US252636

    申请日：1988-10-03

    申请人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

    发明人： Akihiro Yoshimoto ,  Osamu Jodo ,  Yoshio Watanabe ,  Rokuro Okamoto ,  Tomoyuki Ishikura ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Tomio Takeuchi

    IPC分类号： C07H15/252

    CPC分类号： C07H15/252

    摘要： Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is 1-hydroxyethyl group, R.sup.4 is hydrogen atom and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1, R.sup.2 and R.sup.4 are hydroxyl groups, R.sup.3 is ethyl group and X represents daunosamine-rhodenose, daunosamine-deoxyfucose, rhodosamine-rhodenose, N-monomethyldaunosamine-rhodenose or N-monomethyldaunosamine-deoxyfucose; orR.sup.1 is methoxy group, R.sup.2 is hydroxyl group, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.4 are hydroxy groups, R.sup.2 is hydrogen atom, R.sup.3 is ethyl group and X represents daunosamine-deoxyfucose, as well as pharmaceutically acceptable acid addition salts thereof. The antibiotics (I) have a carcinostatic activity and are useful as a carcinostatic for murine leukemia L1210 cells in culture.

    Optically active azetidinones
    8.
    发明授权
    Optically active azetidinones 失效
    光学活性氮杂环丁酮

    公开(公告)号：US4939248A

    公开(公告)日：1990-07-03

    申请号：US246826

    申请日：1988-08-18

    申请人： Takeo Yoshioka ,  Machiko Watanabe ,  Yasuo Fukagawa ,  Tomoyuki Ishikura

    发明人： Takeo Yoshioka ,  Machiko Watanabe ,  Yasuo Fukagawa ,  Tomoyuki Ishikura

    IPC分类号： C07D405/06 ,  C07D205/08 ,  C07D405/04 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D205/08 ,  C07D233/56 ,  C07D249/08 ,  C07D405/04 ,  Y02P20/55

    摘要： This invention provides compounds of the formula ##STR1## wherein Y represents an acetyl, 1-hydroxyethyl or 1-fluoroethyl group, R.sub.1 represents a hydrogen atom or an easily splittable amino-protecting group, and R.sub.2 and R.sub.3 are identical or different and each represents a hydrogen atom, a lower alkyl group, a phenyl group, a benzyl group or a diphenylmethyl group, or R.sub.2 and R.sub.3 together represent a lower alkylene group; and processes for production thereof. These compounds are useful as synthesis intermediates for production of various medicines, particulary carbapenam or carbapenem antibiotics, such as a carbapenem antibiotic of the following formula which has excellent antimicrobial activity and relatively good stability to kidney dehydropeptidase. ##STR2##

    摘要翻译： PCT No.PCT / JP87 / 00991 Sec。 371日期1988年8月18日 102（e）日期1988年8月18日PCT Filted 1987年12月18日PCT公布。 出版物WO88 / 04656 日本6月30日，1988年。本发明提供式（I）的化合物，其中Y表示乙酰基，1-羟乙基或1-氟乙基，R 1表示氢原子或易裂解的氨基保护基， R2和R3相同或不同，各自表示氢原子，低级烷基，苯基，苄基或二苯基甲基，或R2和R3一起表示低级亚烷基; 及其生产方法。 这些化合物可用作生产各种药物，特别是碳青霉烯或碳青霉烯类抗生素的合成中间体，如下式的碳青霉烯类抗生素，其具有优异的抗微生物活性，对肾脱水肽酶具有较好的稳定性。 （A）