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    Novel oxofuryl ester derivatives of penicillin and cephalosporin
    1.
    发明授权
    Novel oxofuryl ester derivatives of penicillin and cephalosporin 失效
    新型青霉素和头孢菌素的氧氟草醚衍生物

    公开(公告)号：US3951954A

    公开(公告)日：1976-04-20

    申请号：US550457

    申请日：1975-02-18

    申请人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi ,  Hidefumi Matsui ,  Kohzi Nakano ,  Kozo Takahashi ,  Hiroshi Horiguchi ,  Akio Koda

    发明人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi ,  Hidefumi Matsui ,  Kohzi Nakano ,  Kozo Takahashi ,  Hiroshi Horiguchi ,  Akio Koda

    IPC分类号： C07D499/00 ,  C07D499/32 ,  C07D499/68 ,  C07D501/20 ,  C07D501/22 ,  C07D501/32

    CPC分类号： C07D499/00

    摘要： The oxofuryl ester derivatives of 6-(.alpha.-amino-phenylacetamido)penicillanic acid, 7-(.alpha.-aminophenylacetamido)-cephalosporanic acid, or 7-(.alpha. -aminophenylacetamide)desacetoxycephalosporanic acid represented by the general formula ##SPC1##Wherein A represents ##SPC2##Wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, said R.sup.1 and R.sup.2 may form together a 1,3-butadienylene group, R.sup.3 represents a hydrogen atom or an acetoxy group, andMeans a single bond or a double bond, and acid addition salts of them. When those compounds are orally administered, they are readily absorbed by the intestines and show antibacterial activity by splitting their ester bonds. The rate of absorption of the compounds by the intestines are higher and the toxic property of them is less than those of known compounds similar to the above compounds.

    摘要翻译： 6-（α-氨基 - 苯乙酰氨基）青霉烷酸，7-（α-氨基苯基乙酰氨基） - 头孢烷酸或由通式为WHEREIN A表示的7-（α-氨基苯基乙酰胺）脱乙酰氧基头孢烷酸的氧代氟代酯衍生物代表其中R1和R2 可以相同或不同，各自表示氢原子或低级烷基，所述R 1和R 2可以一起形成1,3-丁二烯基，R 3表示氢原子或乙酰氧基，和单个键 或双重债券及其酸加法销售。 当口服这些化合物时，它们容易被肠子吸收，并通过分裂其酯键显示抗菌活性。 肠中化合物的吸收速率较高，其毒性低于与上述化合物相似的已知化合物。

    Ampicillin derivatives substituted by heterocyclic acyl group
    2.
    发明授权
    Ampicillin derivatives substituted by heterocyclic acyl group 失效
    由杂环酰基取代的氨苄青霉素衍生物

    公开(公告)号：US3953428A

    公开(公告)日：1976-04-27

    申请号：US356120

    申请日：1973-05-01

    申请人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

    发明人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

    IPC分类号： A61K31/43 ,  C07D20060101 ,  C07D499/12 ,  C07D499/44 ,  C07D499/68 ,  C07D499/70 ,  C07D499/72

    CPC分类号： C07D499/68

    摘要： The ampicillin derivatives represented by the general formula ##SPC1##Wherein R represents ##SPC2##Wherein R' represents a hydrogen atom, a methyl group, or an ethyl group and A and B each represents a hydrogen atom, a hydroxyl group, a methyl group, a methoxy group, a nitro group, or a halogen atom and further said B may combine with A on the carbon atom at the position to form ##SPC3##Group (where in Z represents --CH=N-- or --CH=CH-- and an R.sup.2 represents a hydrogen atom, a hydroxyl group, a phenyl group, a methyl group, an ethyl group, a methoxy group, an ethoxyl group, a methylthio group, a trifluoromethyl group, a halogen atom, a nitro group, an acetyl group, an acetamido group, a ethoxycarbonyloxy group, or a methylsulfonyl group and further R.sub.2 and ##SPC4##May form a thiazole, isothiazolo, pyrrolo, furo, or benzo fused ring which may be substituted by an oxo group, a methyl group, or an acetyl group) and the dotted line means an arbitrary double bond, ##SPC5##Wherein R.sup.3 and R.sup.4 each represents a hydrogen atom or a methyl group, ##SPC6##Wherein R.sup.5 represents a halogen atom, a methoxy group, a nitro group, or a hydroxyl group and R.sup.6 represents a hydrogen atom, a methoxy group, a halogen atom, a nitro group, or a hydroxyl group, or ##SPC7##Wherein R.sup.7 represents a hydrogen atom or a hydroxyl group, Y represents O or S, and the dotted line means an arbitrary double bond, said substituent group, being bonded to the ampicillin molecule through --CO-- at the 2-position, 3-position, 5-position or 6-position when the oxo group (+0) is at the 4-portion and being bonded to the ampicillin molecule through the --CO-- group at the 2-position, 4-position, or 5-position when the oxy group is at the 6-position, and salts of the ampicillin derivatives.Those compounds are valuable as antibacterial agents.

    摘要翻译： 由通式WHEREIN R表示的氨苄青霉素衍生物代表WHEREIN R'表示氢原子，甲基或乙基，A和B各自表示氢原子，羟基，甲基，甲氧基， 硝基或卤素原子，并且所述B可以与碳原子上的A结合形成基团（其中Z表示-CH = N-或-CH = CH-，R2表示氢原子， 羟基，苯基，甲基，乙基，甲氧基，乙氧基，甲硫基，三氟甲基，卤素原子，硝基，乙酰基，乙酰氨基，乙氧基羰基氧基 或甲基磺酰基，并且还可以是OXO基团，甲基或乙酰基团可以取代的噻唑，异噻唑，吡咯，呋喃，或苯并呋喃环），并且被引导的线表示仲胺双 BOND，其中R 3和R 4各自表示氢原子或甲基 其中，R5表示卤素原子，甲氧基，硝基或羟基，R6表示氢原子，甲氧基，卤素原子，硝基或羟基，或者WHEREIN R7表示 氢原子或羟基，Y表示O或S，虚线表示任意双键，所述取代基通过2-位，3-位，5-位上的-CO-键合到氨苄青霉素分子上 当氧基团（+0）为4-部分时，或6-位，当氧基团为氧基团时，2-位，4-位或5-位通过-CO-基团连接于氨苄青霉素分子 在6位，和氨苄青霉素衍生物的盐。

    Cephalosporin compounds
    4.
    发明授权
    Cephalosporin compounds 失效
    头孢菌素化合物

    公开(公告)号：US4311842A

    公开(公告)日：1982-01-19

    申请号：US53852

    申请日：1979-07-02

    申请人： Akio Koda ,  Ichiro Isaka ,  Yukiyasu Murakami

    发明人： Akio Koda ,  Ichiro Isaka ,  Yukiyasu Murakami

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/57 ,  C07D501/56

    CPC分类号： C07D501/20 ,  A61K31/545 ,  C07D501/24

    摘要： Cephalosporin compounds shown by the general formula ##STR1## wherein R.sub.1 represents hydrogen atom or an amino group; R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen atom, a hydroxy group, an oxo group, a lower alkyl group, or a lower alkoxy group; R.sub.4 represents a hydrogen atom or a lower alkoxy group; R.sub.5 represents an acetoxy group or --S--R.sub.6 (wherein R.sub.6 represents a 5- or 6-membered nitrogen-containing heterocyclic group which can be substituted by a lower alkyl group or lower alkoxy group); and A represents a monocyclic or bicyclic heterocyclic ring containing one or two atoms selected from the group consisting of nitrogen, oxygen and a sulfur atom; and pharmaceutically acceptable nontoxic salts thereof.These compounds have excellent antimicrobial activity against various microorganisms including resistant bacteria and are used for the treatment of bacterial infections of animals including human beings.

    摘要翻译： 由通式表示的头孢菌素化合物，其中R1表示氢原子或氨基; R 2和R 3可以相同或不同，各自表示氢原子，羟基，氧代基，低级烷基或低级烷氧基; R4代表氢原子或低级烷氧基; R5表示乙酰氧基或-S-R6（其中R6表示可被低级烷基或低级烷氧基取代的5-或6-元含氮杂环基）。 A表示含有一个或两个选自氮，氧和硫原子的原子的单环或双环杂环; 及其药学上可接受的无毒盐。 这些化合物对包括抗性细菌在内的各种微生物具有优异的抗微生物活性，并用于治疗包括人在内的动物的细菌感染。

    Cephalosporin derivative and pharmaceutical composition
    5.
    发明授权
    Cephalosporin derivative and pharmaceutical composition 失效
    头孢菌素衍生物和药物组合物

    公开(公告)号：US4581353A

    公开(公告)日：1986-04-08

    申请号：US628971

    申请日：1984-07-11

    申请人： Masaru Iwanami ,  Akio Koda ,  Yukiyasu Murakami

    发明人： Masaru Iwanami ,  Akio Koda ,  Yukiyasu Murakami

    IPC分类号： C07D277/20 ,  C07D501/20 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D277/587 ,  Y02P20/55

    摘要： A cephalosporin derivative of the formula ##STR1## wherein R is a hydrogen atom, a lower alkyl group which may have been substituted or a carbamoyl group which may have been substituted; R.sub.1 is hydrogen atom or a methoxy group; R.sub.2 is a hydrogen atom, an acyloxy group, or a nitrogen-containing 5-membered heterocyclic thio group which may have been substituted; R.sub.3 is a free amino group or an amino group having a protective group; and R.sub.4 is a free carboxy group or a carboxy group having a protective group or the salts thereof.The compound of this invention has an excellent antibacterial activity against gram negative bacteria and gram positive bacteria.

    摘要翻译： 其中R为氢原子，可被取代的低级烷基或可被取代的氨基甲酰基的式IMAMA的头孢菌素衍生物; R1是氢原子或甲氧基; R2是氢原子，酰氧基或可以被取代的含氮5元杂环硫基; R3是游离氨基或具有保护基的氨基; R4为游离羧基或具有保护基的羧基或其盐。 本发明化合物对革兰氏阴性细菌和革兰氏阳性细菌具有优异的抗菌活性。