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48 条记录 (耗时 0.043 秒)

    Azetidinone intermediates for cephalosporin analogs
    2.
    发明授权
    Azetidinone intermediates for cephalosporin analogs 失效
    氮杂环丁酮中间体用于头孢菌素类似物

    公开(公告)号：US4592865A

    公开(公告)日：1986-06-03

    申请号：US589670

    申请日：1984-03-13

    申请人： Masayuki Narisada ,  Hiroshi Onoue ,  Teruji Tsuji ,  Yasuhiro Nishitani ,  Mitsuru Yoshioka ,  Yoshio Hamashima ,  Wataru Nagata

    发明人： Masayuki Narisada ,  Hiroshi Onoue ,  Teruji Tsuji ,  Yasuhiro Nishitani ,  Mitsuru Yoshioka ,  Yoshio Hamashima ,  Wataru Nagata

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D505/00 ,  C07F9/568 ,  C07D498/04

    CPC分类号： C07F9/5683 ,  C07D205/085 ,  C07D505/00

    摘要： Intermediates of the following formula are useful for the synthesis of 1-oxacephalosporins. Their preparation from penicillins and the transformation process to make 1-oxacephalosporins are disclosed. The compounds are of the formula: ##STR1## wherein A is amino or a selected acylamino;COB is carboxy or a selected protected-carboxy;X is halogen or the group ORin which R is a group represented by following formulas: ##STR2## wherein Nu is a selected nucleophilic group; R.sup.1 is a group of the following formula: ##STR3## in which Hal is halogen or alkylsulfonyloxy and R.sup.2 is alkyl or aryl; andY is hydrogen or methoxy; with the proviso that when R is propargyl or 2-oxopropyl andR.sup.1 is ##STR4## A is in the 3.alpha.-configuration and Y is 3.beta.-hydrogen or A is in the 3.beta.-configuration and Y is 3.alpha.-methoxy.

    摘要翻译： 下列配方的中间体可用于合成1-氧杂七环素。 公开了它们从青霉素的制备和制备1-氧杂七环素的转化过程。 化合物具有下式：其中A是氨基或选择的酰氨基; COB是羧基或选择的保护羧基; X是卤素或基团OR，其中R是由下式表示的基团：CH2CCH，CH2CCNu，CH2CHCH2，＆lt; IMAGE＆gt;＆gt;其中Nu是选择的亲核基团; R1是下式的基团：其中Hal是卤素或烷基磺酰氧基，R2是烷基或芳基的 Y为氢或甲氧基; 条件是当R为炔丙基或2-氧代丙基且R 1为A 3构型时，Y为3个β-氢，或A为3个β-构型，Y为3个α-甲氧基。

    Vinylthioacetamido oxacephalosporin derivatives
    4.
    发明授权
    Vinylthioacetamido oxacephalosporin derivatives 失效
    乙烯基硫代乙酰氨基氧杂环孢菌素衍生物

    公开(公告)号：US4529721A

    公开(公告)日：1985-07-16

    申请号：US534147

    申请日：1983-09-21

    申请人： Wataru Nagata ,  Mitsuru Yoshioka ,  Yasuhiro Nishitani ,  Tsutomu Aoki ,  Toshiro Konoike ,  Tadatoshi Kubota

    发明人： Wataru Nagata ,  Mitsuru Yoshioka ,  Yasuhiro Nishitani ,  Tsutomu Aoki ,  Toshiro Konoike ,  Tadatoshi Kubota

    IPC分类号： A01N43/90 ,  C07D241/08 ,  C07D339/00 ,  C07D505/00 ,  C07D519/00 ,  C07F9/535 ,  A01N59/06 ,  C07D498/04

    CPC分类号： C07F9/5352 ,  C07C309/00 ,  C07C323/00 ,  C07D241/08 ,  C07D339/00 ,  C07D505/00 ,  Y02P20/55

    摘要： A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.3 CO--; x represents halogen, trifluoromethyl, an alkylthio or an arylthio; y represents hydrogen, a light metal or a carboxylic acid protecting group; and z represents an acyloxy or a heterocycle-thio, each of the above radicals represented by the symbols u, v, w, x, y and z being optionally substituted by halogen or a carbon-, nitrogen-, oxygen- or sulfur-containing functional group, a process for preparing the compound, a pharmaceutical composition containing the compound, and a therapeutical use of the compound.A compound of the formula: ##STR2## wherein u, v, w and x are as defined above, useful as a starting compound for preparing the compound (I) is also provided.

    摘要翻译： 下式的化合物：其中u表示氢，甲酰氨基，N-羟基羧甲酰氨基，羧基，叠氮基，芳基，酰氨基，被保护的羧基或N-烷氧基羧酰胺基，或与v一起可代表 -S-或-CH2S-; v表示氢，卤素，氰基或烷硫基，或与u一起可以表示-S-或-CH 2 S-，或者与w一起可以表示 - （CH 2）3 CO-; w表示氢，氨甲酰基，氰基，羧基，N-烷基氨基甲酰基，烷基，芳基，保护的羧基或杂环，或与v一起可以表示 - （CH 2）3 CO-; x表示卤素，三氟甲基，烷硫基或芳硫基; y表示氢，轻金属或羧酸保护基; 和z表示酰氧基或杂环硫基，由符号u，v，w，x，y和z表示的上述基团中的每一个任选被卤素或含碳，氮，氧或硫的 官能团，制备该化合物的方法，含该化合物的药物组合物和该化合物的治疗用途。 还提供了下式化合物：其中u，v，w和x如上定义，可用作制备化合物（I）的起始化合物。

    Cephalosporin hydroxamic acids
    7.
    发明授权
    Cephalosporin hydroxamic acids 失效
    头孢菌素异羟肟酸

    公开(公告)号：US4614797A

    公开(公告)日：1986-09-30

    申请号：US576404

    申请日：1984-02-02

    申请人： Wataru Nagata ,  Tsutomu Aoki ,  Yasuhiro Nishitani

    发明人： Wataru Nagata ,  Tsutomu Aoki ,  Yasuhiro Nishitani

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/57 ,  C07D505/00

    CPC分类号： C07D505/00 ,  Y02P20/55

    摘要： An antibacterial cephalosporin hydroxamic acid derivative represented by the following formula (I), processes for its preparation, compositions containing the same as an active ingredient, and a method for killing bacteria by contacting with said compound. ##STR1## (wherein, R is acyl; R.sup.1 is hydrogen or methoxy; R.sup.2 is alkylene; R.sup.3 is hydrogen, aliphatic group or a hydroxy-protecting group; R.sup.4 is hydrogen or amino-protecting group; R.sup.5 is hydrogen, light metal atom or carboxy-protecting group; and X is oxygen, sulfur, or sulfinyl).

    摘要翻译： 由下式（I）表示的抗菌头孢菌素异羟肟酸衍生物，其制备方法，含有该活性成分的组合物，以及通过与所述化合物接触来杀死细菌的方法。 （I）（I）（其中R为酰基; R 1为氢或甲氧基; R 2为亚烷基; R 3为氢，脂族基或羟基保护基; R 4为氢或氨基保护基; R 5为氢， 金属原子或羧基保护基; X是氧，硫或亚磺酰基）。

    Cephem Compounds Having Broad Antibacterial Spectrum
    10.
    发明申请
    Cephem Compounds Having Broad Antibacterial Spectrum 失效
    具有广泛抗菌谱的头孢烯化合物

    公开(公告)号：US20090131655A1

    公开(公告)日：2009-05-21

    申请号：US12100307

    申请日：2008-04-09

    申请人： Yasuhiro Nishitani ,  Yoshinori Yamano

    发明人： Yasuhiro Nishitani ,  Yoshinori Yamano

    IPC分类号： C07D501/60

    CPC分类号： C07D501/56 ,  A61K31/546 ,  C07D501/00

    摘要： A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene) Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.

    摘要翻译： 下式的化合物：其中T是S，SO或O; X是卤素，CN，任选被低级烷基，低级烷基，低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基（其中取代基是 任选取代的单低级烷基，任选取代的低级亚烷基或任选取代的低级亚烷基）Z +是任选取代的阳离子和含N原子的杂环基），酯，氨基保护的化合物，其中氨基与噻唑环上的氨基键连接 7-位或其药学上可接受的盐或溶剂化物。