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    N-acylamino-.alpha.-arylacetamido cephalosporins
    5.
    发明授权
    N-acylamino-.alpha.-arylacetamido cephalosporins 失效
    N-酰氨基 - {60-芳基乙酰氨基头孢菌素

    公开(公告)号：US4160087A

    公开(公告)日：1979-07-03

    申请号：US795596

    申请日：1977-05-10

    申请人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

    发明人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

    IPC分类号： A61K31/545 ,  C07D501/34

    CPC分类号： C07D501/34 ,  C07D501/24

    摘要： A cephalosporin derivative of the formula (I), ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be substituted with one or more substituents; R is a phenyl group substituted with at least one substituent selected from the group consisting of an amino group, a hydroxy group, a ureido group and a hydroxymethyl group; and X is an --OCOCH.sub.3 group or an --S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial and prepared by the reaction of a compound of the formula (II),ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III), ##STR2## wherein R and X are as defined above, or a derivative thereof.

    摘要翻译： 式（I）的头孢菌素衍生物，其中A是单环或多环杂芳环，其含有至少一个氮原子作为杂原子并且可以被一个或多个取代基取代; R是被至少一个选自氨基，羟基，脲基和羟甲基的取代基取代的苯基; 并且X是-OCOCH 3基团或-S-Het基团，其中Het是含有1至4个选自氮，氧和硫原子的杂原子的5或6元杂环，其可以被 一种或多种取代基及其无毒的药学上可接受的盐，其可用作抗微生物剂并通过式（II）化合物，其中A如上定义的HO-A-COOH（II） 或其活性衍生物与式（III）化合物，其中R和X如上所定义的其中，或其衍生物。

    Penicillins
    6.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号：US4008220A

    公开(公告)日：1977-02-15

    申请号：US495914

    申请日：1974-08-08

    申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    IPC分类号： C07D499/00 ,  C07D499/68 ,  C07D499/48

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.

    摘要翻译： 一种下式的青霉素：其中是含有1或2个氮原子作为杂原子的六元杂芳环，Y是氢，低级烷酰基或低级烷氧基羰基，R 1和R 2各自是氢，低级烷基 ，低级烷酰基，苯甲酰基，低级烷基巯基，羟基，巯基，羟基（低级）烷基，卤素或氰基，或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链，Z是苯基， 低级烷基，环己二烯基，噻吩基或异噻唑基，其通过使下式化合物：其中Z如上所定义或其衍生物与下式的羧酸反应制备：其中和R2 各自如上所定义，或其反应性衍生物，如果需要，随后水解或酰化所得产物和/或消除任何保护基团，并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂，包括 uding假单胞菌

    Penicillins substituted with heterocyclic and substituted phenyl groups
    7.
    发明授权
    Penicillins substituted with heterocyclic and substituted phenyl groups 失效
    用杂环和取代的苯基取代的青霉素

    公开(公告)号：US3992371A

    公开(公告)日：1976-11-16

    申请号：US536181

    申请日：1974-12-24

    申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    IPC分类号： C07D499/10 ,  C07D471/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/64 ,  C07D499/68 ,  C07D519/06 ,  C07D499/70

    CPC分类号： C07D471/04 ,  C07D499/00

    摘要： Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: ##EQU3## wherein ##EQU4## X and Y are each as defined above or its reactive derivative with a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.

    摘要翻译： 式+ q，10的新型青霉素其中C | A C表示可被取代的取代或未取代的含有苯或含氮原子的杂芳环，C | C | CB表示吡啶，吡嗪或哒嗪环，X表示 氧或硫原子，Y表示氢原子或低级烷氧基羰基或低级烷酰基，R 1，R 2和R 3各自为氢或卤素原子或硝基，低级烷基氨基，二（低级）烷基氨基，亚氨基，低级烷氧基羰基氨基， 低级烷酰基氨基，氨基（低级）烷基，低级烷基，低级烷氧基，羟基，氨磺酰基，三氟甲基，低级烷硫基或低级烷基磺酰基，不包括R1，R2和R3全部为氢原子，其中R1为羟基， R2和R3各自为氢或卤素原子，以及它们的无毒的药学上可接受的盐，其可以通过使下式的羧酸：XY | C | C-COOH A | CB反应而制备，其中CC | | CA | | C，CB，X和Y为ea ch或其反应性衍生物与下式的化合物：+ q，21，其中R1，R2和R3各自如上所定义，或其反应性衍生物，并且作为抗革兰氏阳性和革兰氏阴性细菌的抗微生物剂 包括假单胞菌。

    Novel penicillins and their preparation
    8.
    发明授权
    Novel penicillins and their preparation 失效
    新青霉素及其制备

    公开(公告)号：US4003887A

    公开(公告)日：1977-01-18

    申请号：US609982

    申请日：1975-09-03

    申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    IPC分类号： C07D499/00 ,  C07D499/68

    CPC分类号： C07D499/00

    摘要： Novel penicillins of the formula: ##STR1## wherein the ring A is a benzene ring or a 5 or 6-membered heteroaromatic ring containing one or two nitrogen atoms as the hetero atom, on which one or more of lower alkyl, lower alkoxy, lower alkylthio, lower haloalkyl, lower alkylenedioxy halogen, hydroxyl, nitro, free or protected amino, lower alkylamino, di(lower)alkylamino and lower alkanoylamino may be present, Z is a nitrogen atom or a methylene group, X is an oxygen atom or a sulfur atom, Y is a hydrogen atom, a lower alkoxycarbonyl group or a lower alkanoyl group, R.sub.1 is a free or protected hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen atom or a halogen atom, and their non-toxic pharmaceutically acceptable salts, and their preparation.

    摘要翻译： 新颖的下列青霉素： 其中环A是苯环或含有一个或两个氮原子作为杂原子的5或6元杂芳环，其中一个或多个低级烷基，低级 烷氧基，低级烷硫基，低级卤代烷基，低级亚烷基二氧基卤素，羟基，硝基，游离或被保护的氨基，低级烷基氨基，二（低级）烷基氨基和低级烷酰基氨基，Z是氮原子或亚甲基，X是氧 原子或硫原子，Y为氢原子，低级烷氧基羰基或低级烷酰基，R1为游离或保护的羟基，R2和R3各自为氢原子或卤素原子，其无毒性 可接受的盐及其制备方法。

    Penicillins and their preparation
    10.
    发明授权
    Penicillins and their preparation 失效
    青霉素及其制备

    公开(公告)号：US4005075A

    公开(公告)日：1977-01-25

    申请号：US610754

    申请日：1975-09-05

    申请人： Hirotada Yamada ,  Hisao Tobiki ,  Iwao Nakatsuka ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome

    发明人： Hirotada Yamada ,  Hisao Tobiki ,  Iwao Nakatsuka ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/68

    CPC分类号： C07D499/00

    摘要： Penicillins of the formula: ##STR1## wherein R is an unsubstituted phenyl group or a substituted phenyl group having one or more hydroxyl groups or a cyclohexadienyl group and A represents a monocyclic or polycyclic nitrogen-containing heterocyclic aromatic ring, which are useful as antimicrobial agents having a broad antimicrobial spectrum against gram-positive and gram-negative bacteria including Pseudomonas and can be produced advantageously from the phenacyl ester of 6-aminopenicillanic acid through a series of steps.

    摘要翻译： 下式的青霉素：其中R为未取代的苯基或具有一个或多个羟基或环己二烯基的取代苯基，A表示单环或多环含氮杂环芳环，其可用作抗微生物剂 具有抗革兰氏阳性菌和革兰氏阴性细菌（包括假单胞菌属）的广谱抗菌谱，并且可以通过一系列步骤有利地从6-氨基青霉烷酸的苯甲酰甲酯生产。