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    Cephem compounds
    1.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4550102A

    公开(公告)日：1985-10-29

    申请号：US415910

    申请日：1982-09-08

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/38 ,  C07D501/46

    CPC classification number: C07D501/46

    Abstract: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or lower alkanoylamino,R.sup.2 is lower alkyl, lower alkynyl, carboxy (lower) alkyl or esterified carboxy (lower) alkyl,R.sup.3 is amino or lower alkanoylamino, andX is hydrogen or halogen; and pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及具有下式的高抗微生物活性的新型头孢烯化合物：其中R1是氨基或低级烷酰氨基，R2是低级烷基，低级炔基，羧基（低级）烷基或酯化的羧基（低级）烷基，R3是氨基 或低级烷酰氨基，X为氢或卤素; 和其药学上可接受的盐。

    Cephem compounds
    2.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4495182A

    公开(公告)日：1985-01-22

    申请号：US382763

    申请日：1982-05-27

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07D213/61 ,  C07D213/70 ,  C07D213/73 ,  C07D285/08 ,  C07D501/36 ,  A61K31/545

    CPC classification number: C07D213/70 ,  C07D213/61 ,  C07D213/73 ,  C07D285/08

    Abstract: This invention relates to cephem compounds of high antimicrobial activity of the formula ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group selected from lower alkyl, alkenyl and alkynyl which may be substituted with carboxy, protected carboxy, lower alkylthio or phenyl, cyclo(lower)alkyl, or cyclo(lower)alkenyl;R.sup.3 is lower alkyl which may be substituted with carboxy, carbamoyl, hydroxy, amino or protected amino;R.sup.3a is hydrogen, lower alkyl or amino; andR.sup.3b is hydrogen or lower alkyl; andpharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及具有下式的高抗微生物活性的头孢烯化合物：其中R1是氨基或被保护的氨基; R2是氢，可以被羧基取代的低级烷基，烯基和炔基的低级脂族烃基，保护的羧基，低级烷硫基或苯基，环（低级）烷基或环（低级）烯基; R3是可被羧基，氨基甲酰基，羟基，氨基或被保护的氨基取代的低级烷基; R3a是氢，低级烷基或氨基; 和R3b是氢或低级烷基; 及其药学上可接受的盐。

    Cephem compounds
    4.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4457928A

    公开(公告)日：1984-07-03

    申请号：US330465

    申请日：1981-12-14

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07C17/26 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21 ,  C07D501/46 ,  A61K31/545

    CPC classification number: C07D257/04 ,  C07C17/26 ,  C07D285/08 ,  C07D295/21

    Abstract: This invention relates to novel cephem compounds of high antimicrobial activity, to processes for preparation of said compounds, and to pharmaceutical compositions comprising said compounds, the novel cephem compounds being of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group which may be substituted with a substituent selected from the group consisting of carboxy and protected carboxy, cyclo (lower) alkyl or cyclo (lower) alkenyl; andR.sup.3 is a thiazolio group which may be substituted with a substituent selected from the group consisting of lower alkyl and hydroxy (lower) alkyl, or a pyridinio group substituted with a substituent selected from the group consisting of halogen, cyano, hydroxy, amino, acylamino, lower alkanoyl, hydroxycarbamoyl, alkylcarbamoyl, carboxy, protected carboxy, lower alkyl, hydroxy (lower) alkyl, sulfo (lower) alkyl, protected amino (lower) alkyl, amino (lower) alkyl, carboxy (lower) alkyl and hydroxyimino (lower) alkyl;and pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及高抗微生物活性的新型头孢烯化合物，所述化合物的制备方法以及包含所述化合物的药物组合物，所述新型头孢烯化合物具有下式：其中R 1为氨基或被保护的氨基; R2是氢，可以被选自羧基和保护的羧基，环（低级）烷基或环（低级）烯基的取代基取代的低级脂族烃基; 或者可以被选自低级烷基和羟基（低级）烷基的取代基取代的噻唑基，或被选自卤素，氰基，羟基，氨基， 酰基氨基，低级烷酰基，羟基氨基甲酰基，烷基氨基甲酰基，羧基，保护的羧基，低级烷基，羟基（低级）烷基，磺基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基和羟基亚氨基 低级）烷基; 及其药学上可接受的盐。

    Cephem and cepham compounds
    5.
    发明授权
    Cephem and cepham compounds 失效
    Cephem和cepham化合物

    公开(公告)号：US4425340A

    公开(公告)日：1984-01-10

    申请号：US314045

    申请日：1981-10-22

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07C17/26 ,  C07D209/48 ,  C07D249/12 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21 ,  C07D501/24 ,  A61K31/545

    CPC classification number: C07D209/48 ,  C07C17/263 ,  C07D249/12 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21

    Abstract: This invention relates to new cephem and cepham compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino,R.sup.2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S or O containing 5-membered heterocyclic group substituted with oxo group(s),R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, acyloxy(lower)alkyl; acylthio(lower) alkyl; pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl;l halogen; hydroxy; thiazolium(lower)alkyl which may be substituted with suitable substituent(s); or lower alkoxy; R.sup.5 is carboxy or a protected carboxy, wherein R.sup.5 is COO.sup.- when R.sup.4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s) or thiazolium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond; and pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及具有下式的高抗微生物活性的新的头孢烯和头孢烯化合物：其中R1是氨基或被保护的氨基，R2是氢，酰基，可被适当的取代基取代的芳基，低级烷基取代的 具有合适的取代基，低级烯基，低级炔基，可被适当的取代基取代的环烷基，环（低级）烯基或含有被氧代基取代的5元杂环基的S或O，R 3 是氢或低级烷基，R 4是氢，酰氧基（低级）烷基; 酰基硫代（低级）烷基; 可用合适的取代基取代的吡啶鎓（低级）烷基; 可被适当的取代基取代的杂环硫基（低级）烷基; 低级烷基; l卤素; 羟基; 可被适当的取代基取代的噻唑鎓（低级）烷基; 或低级烷氧基; R5是羧基或被保护的羧基，其中当R 4是吡啶鎓（低级）烷基时，其中R 5是COO-，其可被合适的取代基取代，或可被适当的取代基取代的噻唑鎓（低级）烷基， 重实线表示单键或双键; 及其药学上可接受的盐。

    7-Amino-thia-diazole oxyimino derivatives of cephem and cephem compounds
    6.
    发明授权
    7-Amino-thia-diazole oxyimino derivatives of cephem and cephem compounds 失效
    头孢烯和头孢烯化合物的7-氨基 - 噻二唑氧基亚氨基衍生物

    公开(公告)号：US4332798A

    公开(公告)日：1982-06-01

    申请号：US116984

    申请日：1980-01-30

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07C17/26 ,  C07D209/48 ,  C07D249/12 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21 ,  C07D501/20 ,  A61K31/545 ,  C07D501/56

    CPC classification number: C07D209/48 ,  C07C17/26 ,  C07C17/263 ,  C07D249/12 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21

    Abstract: 7-Substituted-3-cephem and cepham-4-carboxylic acids of formula (I) ##STR1## wherein R.sup.1 is amino or a protected amino, R.sup.2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S- or O-containing 5-membered heterocyclic group substituted with oxo group(s).R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen; acyloxy(lower)alkyl; acylthio(lower)alkyl pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl; halogen; or hydroxy; andR.sup.5 is carboxy or a protected carboxy wherein R.sup.5 is COO-- when R.sup.4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond, have useful antibiotic properties.

    Abstract translation: （I）的7-取代的3-头孢烯和头孢烯-4-羧酸其中R1是氨基或被保护的氨基，R2是氢，酰基，可被适当取代基取代的芳基 ），被合适的取代基取代的低级烷基，低级链烯基，低级炔基，可被适当的取代基取代的环烷基，环（低级）烯基或被S或O取代的5-或 氧代基团。 R3是氢或低级烷基，R4是氢; 酰氧基（低级）烷基; 可以用合适的取代基取代的酰硫基（低级）烷基吡啶鎓（低级）烷基; 可被适当的取代基取代的杂环硫基（低级）烷基; 低级烷基 卤素; 或羟基; 当R 4是可被适当的取代基取代的吡啶鎓（低级）烷基，并且重实线表示单键或双键时，R 5为羧基或被保护的羧基，其中R 5为COO-，具有有用的抗生素性质。

    Cephem compounds
    9.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4463000A

    公开(公告)日：1984-07-31

    申请号：US294291

    申请日：1981-08-19

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07C17/26 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21 ,  C07D501/46 ,  A61K31/545

    CPC classification number: C07D257/04 ,  C07C17/26 ,  C07D285/08 ,  C07D295/21

    Abstract: This invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group which may be substituted with suitable substituents(s), cyclo(lower)alkyl or cyclo(lower)alkenyl; andR.sup.3 is a thiazolio group which may be substituted with suitable substituents(s) or a pyridinio group substituted with substituent(s) selected from the group consisting of halogen, cyano, hydroxy, amino, acylamino, lower alkanoyl, hydroxycarbamoyl, alkylcarbamoyl, carboxy, protected carboxy, lower alkyl, hydroxy(lower)alkyl, sulfo(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl and hydroxyimino(lower)alkyl.

    Abstract translation: 本发明涉及具有下式的高抗微生物活性的新型头孢烯化合物：其中R1是氨基或被保护的氨基; R2是氢，可被适当的取代基，环（低级）烷基或环（低级）烯基取代的低级脂族烃基; 并且R 3是可以被合适的取代基取代的噻唑基或被选自卤素，氰基，羟基，氨基，酰氨基，低级烷酰基，羟基氨基甲酰基，烷基氨基甲酰基，羧基的取代基取代的吡啶基。 被保护的羧基，低级烷基，羟基（低级）烷基，磺基（低级）烷基，保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基和羟基亚氨基（低级）烷基）。

    Cephem compounds
    10.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4431642A

    公开(公告)日：1984-02-14

    申请号：US270029

    申请日：1981-06-03

    Applicant: Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    Inventor： Tsutomu Teraji ,  Kazuo Sakane ,  Jiro Goto

    IPC: C07C17/26 ,  C07D257/04 ,  C07D285/08 ,  C07D295/21 ,  C07D501/46 ,  A61K31/545

    CPC classification number: C07D257/04 ,  C07C17/26 ,  C07D285/08 ,  C07D295/21

    Abstract: This invention relates to new cephem compounds of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group which may be substituted with suitable substituent(s), cyclo(lower)alkyl or cyclo(lower)alkenyl; andR.sup.3 is thiazolio group which may be substituted with suitable substituent(s) or a pyridinio group substituted with substituent(s) selected from the group consisting of halogen, cyano, hydroxy, amino, acylamino, lower alkanoyl, hydroxycarbamoyl, alkylcarbamoyl, carboxy, protected carboxy, lower alkyl, hydroxy(lower)alkyl, sulfo(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl and hydroxyimino(lower)alkyl; and pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及抗微生物活性的新头孢烯化合物，其具有下式：其中R1是氨基或被保护的氨基; R2是氢，可被适当的取代基，环（低级）烷基或环（低级）烯基取代的低级脂族烃基; 氰基，羟基，氨基，酰氨基，低级烷酰基，羟基氨基甲酰基，烷基氨基甲酰基，羧基，氨基甲酰基，氨基甲酰基，氨基甲酰基， 保护的羧基，低级烷基，羟基（低级）烷基，磺基（低级）烷基，保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基和羟基亚氨基（低级） 及其药学上可接受的盐。

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