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    Method for isomerising the 10-methyl radical of erythromycin derivatives
    1.
    发明授权
    Method for isomerising the 10-methyl radical of erythromycin derivatives 有权
    红霉素衍生物的10-甲基异构化方法

    公开(公告)号：US6022965A

    公开(公告)日：2000-02-08

    申请号：US180641

    申请日：1998-11-11

    申请人： Yannick Benedetti ,  Jacques Lagouardat ,  Jacques Scholl

    发明人： Yannick Benedetti ,  Jacques Lagouardat ,  Jacques Scholl

    IPC分类号： A61K31/70 ,  C07H17/08 ,  C07H1/00

    CPC分类号： C07H17/08

    摘要： An isomerization method wherein a compound of formula ##STR1## wherein X and y together form a 3-oxo radical, or X is a hydrogen atom and Y is either a radical a ##STR2## where R.sub.2 is OH or O-acyl, or an O-alkyl or NH.sub.2 radical; R.sub.1 is a hydrogen atom or a methyl radical; Z is hydrogen or an acyl radical; and R is a hydrogen atom, an NH.sub.2 radical or a (CH.sub.2).sub.n Ar, NH(CH.sub.2).sub.n Ar or N.dbd.CH(CH.sub.2).sub.n Ar radical, in the form of a 10.alpha. isomer or a mixture of 10.alpha. and 10.beta. isomers, is exposed to a basic agent to give the corresponding compound of formula I in which the 10-methyl radical is in the .beta. position.

    摘要翻译： PCT No.PCT / FR97 / 00840 Sec。 371日期：1998年11月11日 102（e）1998年11月11日PCT PCT 1997年5月13日PCT公布。 出版物WO97 / 43297 日期：1997年11月20日一种异构化方法，其中其中X和Y一起形成3-氧代基，或X是氢原子，Y是其中R2是OH或O-酰基的基团，或O - 烷基或NH 2基; R1是氢原子或甲基; Z是氢或酰基; 和R是氢原子，NH 2基团或（CH 2）n Ar，NH（CH 2）n Ar或N = CH（CH 2）n Ar基，其为10α异构体或10α和10β异构体的混合物 暴露于碱性试剂中，得到相应的10-甲基在β位的式I化合物。

    Erythromycin derivatives
    4.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号：US5656607A

    公开(公告)日：1997-08-12

    申请号：US414503

    申请日：1995-03-31

    申请人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    IPC分类号： C07H17/08 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/00 ,  A61P31/04 ,  C07H17/00

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form ##STR2## and R'.sub.1 and R'.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

    摘要翻译： 选自下式的化合物的化合物其中R 1和R 2分别选自氢和至多24个碳原子的任选不饱和烃，任选地被至少一个选自以下的杂原子间隔的杂原子 由氧，硫和氮组成并且任选地具有至少一个官能团或一起形成的基团组成，并且R'1和R'2分别选自氢和任选不饱和的烃，最多达23个 碳原子任选地被至少一个选自氮，氧和硫并且任选具有至少一个官能团的杂原子中断，Z是氢或具有1至18个碳原子的有机羧酸的酰基，波浪线表示 该10-甲基可具有R或S构型或R + S与其无毒的药学上可接受的具有抗生素的酸加成盐的混合物 tic属性。

    Erythromycin compounds
    6.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5444051A

    公开(公告)日：1995-08-22

    申请号：US83636

    申请日：1993-06-28

    申请人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  C07H20060101 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted,or X is ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', B is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

    摘要翻译： 式I的化合物其中X和X'形成C = O或C = NOR，R选自氢，杂环，烷基，烯基，炔基，全部被取代，或X是< R a和R b是氢或烃基或与氮一起形成杂环或与A一起形成9-N，11-O环，X'是氢，-Y和Y'具有与X相同的定义， X'，B是氢或OR 4，R 4是氢或与A一起形成碳酸酯或氨基甲酸酯，A形式与C是双键或A是OR'4，R'4是氢或与B一起形成碳酸酯或 R 2是烷基或-CONH 2，-CONHCOR 11或-CONHSO 2 R 11，R 11是至多18个碳原子的烃，R 3是氢，Z是氢或羧酸残基，它们是无毒的，药学上可接受的 酸加成盐，它们的制备和中间体可用作抗生素。

    Erythromycin compounds
    8.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5770579A

    公开(公告)日：1998-06-23

    申请号：US378186

    申请日：1995-01-25

    申请人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  C07H20060101 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', b is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

    摘要翻译： 式I的化合物其中X和X'形成C = O或C = NOR，R选自氢，杂环，烷基，烯基，炔基，全部被取代，R a和R b 是氢或烃基或与氮杂环的形式，或与A一起形成9-N，11-O环，X'为氢，-Y和Y'具有与X和X'相同的定义， b是氢或OR 4，R 4是氢或与A一起形成碳酸酯或氨基甲酸酯，A形式与C是双键或A是OR'4，R'4是氢或与B一起形成碳酸酯或 R 2是烷基或-CONH 2，-CONHCOR 11或-CONHSO 2 R 11，R 11是至多18个碳原子的烃，R 3是氢，Z是氢或羧酸残基及其无毒的药学上可接受的酸加成盐 ，它们的制备和中间体可用作抗生素。

    Erythromycin compounds
    9.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5561118A

    公开(公告)日：1996-10-01

    申请号：US220484

    申请日：1994-03-31

    申请人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Francois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  C07H20060101 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, or X is ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-0 ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', B is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or A is ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

    摘要翻译： 式I的化合物其中X和X'形成C = O或C = NOR，R选自氢，杂环，烷基，烯基，炔基，全部被取代，或X是< R a和R b是氢或烃基或与氮一起形成杂环或与A一起形成9-N，11-0环，X'是氢，-Y和Y'具有与X相同的定义， X'，B是氢或OR 4，R 4是氢或与A一起形成碳酸酯或氨基甲酸酯，A形式与C是双键或A是OR'4，R'4是氢或与B一起形成碳酸酯或 A是R 2是烷基或-CONH 2，-CONHCOR 11或-CONHSO 2 R 11，R 11是至多18个碳原子的烃，R 3是氢，Z是氢或羧酸残基，它们是无毒的， 药学上可接受的酸加成盐，它们的制剂和用作抗生素的中间体。