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    Antibiotic .beta.-lactam compounds, production thereof, and their use as antimicrobial agent
    2.
    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。

    Tylosin derivatives
    4.
    发明授权
    Tylosin derivatives 失效
    泰乐菌素衍生物

    公开(公告)号：US4612372A

    公开(公告)日：1986-09-16

    申请号：US754568

    申请日：1985-07-12

    申请人： Takeo Yoshioka ,  Miharu Maeda ,  Rokuro Okamoto ,  Yasutaka Shimauchi ,  Tomoyuki Ishikura ,  Tsutomu Sawa ,  Tomio Takeuchi ,  Hamao Umezawa

    发明人： Takeo Yoshioka ,  Miharu Maeda ,  Rokuro Okamoto ,  Yasutaka Shimauchi ,  Tomoyuki Ishikura ,  Tsutomu Sawa ,  Tomio Takeuchi ,  Hamao Umezawa

    IPC分类号： C07H17/08

    CPC分类号： C07H17/08

    摘要： Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.

    摘要翻译： 新型泰乐菌素衍生物由下式表示：其中R代表氢原子，乙酰基或丙酰基; X表示-CO-或-SO 2 - 基团; Y表示在2位或4位与苄基结合的氟原子，乙酰基，甲磺酰基，甲硫基，苯甲酰基或甲氧基; Z代表氢原子或D-霉菌素残留物：作为大环内酯类抗生素的泰乐菌素衍生物提供了改善的抗菌活性和提高体内吸收和排泄的能力。

    Anthracyclinone trisaccharide compounds
    5.
    发明授权
    Anthracyclinone trisaccharide compounds 失效
    蒽环类三糖化合物

    公开(公告)号：US4418192A

    公开(公告)日：1983-11-29

    申请号：US370212

    申请日：1982-04-20

    申请人： Hiroshi Tanaka ,  Takeo Yoshioka ,  Yasutaka Shimauchi ,  Toshikazu Oki ,  Tomoyuki Ishikura ,  Tomio Takeuchi ,  Hamao Umezawa

    发明人： Hiroshi Tanaka ,  Takeo Yoshioka ,  Yasutaka Shimauchi ,  Toshikazu Oki ,  Tomoyuki Ishikura ,  Tomio Takeuchi ,  Hamao Umezawa

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Disclosed are novel anthracyclinone glycosides represented by the chemical formula ##STR1## wherein R.sup.1 is hydrogen or methyl;R.sup.2 is hydrogen or hydroxyl;R.sup.3 is hydrogen or methoxycarbonyl;R.sup.4 is two hydrogen atoms or an oxygen atom;R.sup.5 is hydrogen, hydroxyl or --OCOX (wherein X is lower alkyl or aralkyl);R.sup.6 is amino, monomethylamino or dimethylamino;R.sup.7 is hydrogen or acetyl; andR.sup.8 is hydrogen or L-cinerulose A ##STR2## but, when R.sup.1 and R.sup.3 are hydrogen and methoxycarbonyl respectively, R.sup.2 is hydrogen; R.sup.4 is two hydrogen atoms; R.sup.5 is hydrogen; R.sup.6 is amino, monoethylamino or dimethylamino; R.sup.7 is acetyl; and R.sup.8 is L-cinerulose A,and their acid addition salts and a method for preparation thereof which consists of treating O-alpha-L-cinerulosyl-(1.fwdarw.4)-O-(3-O-acetyl-2-deoxy-alpha-L-fucosyl)-(1.fwdarw.4)-alpha-L-rhodosamine with corresponding aglycones.

    摘要翻译： 公开了由化学式（IMAGE）（I）表示的新型蒽环酸苷，其中R1是氢或甲基; R2是氢或羟基; R3是氢或甲氧基羰基; R4是两个氢原子或氧原子; R5是氢，羟基或-OCOX（其中X是低级烷基或芳烷基）; R6是氨基，单甲基氨基或二甲基氨基; R7是氢或乙酰基; 并且R 8是氢或L-果糖醛酸A，但是当R 1和R 3分别是氢和甲氧基羰基时，R 2是氢; R4是两个氢原子; R5是氢; R6是氨基，单乙基氨基或二甲基氨基; R7是乙酰基; R8为L-丝瓜糖苷A及其酸加成盐及其制备方法，其由O-α-L-脯氨酰基 - （1-> 4）-O-（3-O-乙酰基-2-脱氧 α-L-岩藻糖基） - （1→4）-alpha-L-罗丹明与相应的糖苷配基。