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    Erythromycin compounds
    1.
    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
    2.
    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。

    Erythromycin compounds
    3.
    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
    4.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5543400A

    公开(公告)日：1996-08-06

    申请号：US146695

    申请日：1993-11-01

    申请人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/706 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    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 is ##STR2## m and n are individually integers from 0 to 6, A and B are individually a member selected from the group consisting of hydrogen, halogen and alkyl of 1 to 8 carbon atoms, the double bond geometry being E or Z or E+Z or A and B form a third bond between the carbon atoms to which they are attached, Ar is selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms optionally substituted with at least one member of the group consisting of free carboxy, alkoxycarbonyl, carboxy salified with a non-toxic, pharmaceutically acceptable base, amidified carboxy, --OH, halogen, --NO.sub.2, --CN, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio and alkynylthio of up to 12 carbon atoms, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms and cycloalkyl of 3 to 12 carbon atoms, all optionally substituted with at least one halogen and ##STR3## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms, carbocyclic aryl, aryloxy, arylthio, heterocyclic aryl and aryloxy and arylthio containing at least one heteroatom, all optionally substituted as above and b) heterocyclic aryl having at least one heteroatom optionally substituted with at least one of the above substituents, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

    摘要翻译： 选自下列化合物的化合物其中R为M的化合物，其中R为0至6的整数，A和B分别为选自氢，卤素 1至8个碳原子的烷基，双键几何为E或Z或E + Z或A和B在它们所连接的碳原子之间形成第三键，Ar选自a）碳环 任选被至少一个由游离羧基，烷氧基羰基，无毒的药学上可接受的碱盐化的羧基，酰胺化的羧基，-OH，卤素，-NO 2，-CN， 烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，烯硫基和炔硫基，最多12个碳原子的N-烷基，N-烯基和N-炔基和3-12个碳原子的环烷基， 全部任选被至少一个卤素取代， nd R2各自独立地选自氢，1至12个碳原子的烷基，碳环芳基，芳氧基，芳硫基，杂环芳基和含有至少一个杂原子的芳氧基和芳硫基，全部如上所述被取代，和b）杂环芳基，其具有 至少一个任选被至少一个上述取代基取代的杂原子Z是氢或具有1至18个碳原子的有机羧酸的酰基及其无毒的药学上可接受的具有抗生素性质的酸加成盐。

    Erythromycin derivatives
    5.
    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。

    Propanal derivatives
    6.
    发明授权
    Propanal derivatives 失效
    丙醛衍生物

    公开(公告)号：US5760233A

    公开(公告)日：1998-06-02

    申请号：US805439

    申请日：1997-02-25

    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 ,  C07D215/00 ,  C07C13/00 ,  C07D271/00 ,  C07D277/04

    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 derivatives
    9.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号：US5527780A

    公开(公告)日：1996-06-18

    申请号：US146697

    申请日：1993-11-01

    申请人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    IPC分类号： C07C211/27 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  C07C217/62 ,  C07D239/20 ,  C07D333/10 ,  C07H17/00 ,  C07H17/08

    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 is --(CH.sub.2).sub.n --Ar.sub.1 or --XAr.sub.2, n is an integer from 1 to 6, Ar.sub.1 and Ar.sub.2 are individually selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms substituted by at least one member of the group consisting of free carboxy, alkoxy carbonyl and carboxyl salified with a pharmaceutically acceptable base, --OH, halogen, --NO.sub.2, --CN, ##STR2## and alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms optionally substituted with at least one halogen, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 12 carbon atoms, b) ##STR3## wherein R.sub.3 is selected from the group consisting of alkyl of 1 to 12 carbon atoms, optionally substituted carbocyclic aryl, aryloxy and arylthio, optionally substituted heterocyclic aryl, aryloxy and arylthio containing at least one heteroatom with the optional substituents being those of carbocyclic aryl above, X is an alkyl of 1 to 6 carbon atoms interrupted by a member of the group consisting of --O--, --S--, --SO--, --SO.sub.2, --CO--, ##STR4## Z is hydrogen or acyl of an organic carboxylic acid of up to 18 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity against gram positive and gram negative bacteria.

    摘要翻译： 选自下式的化合物的化合物其中R为 - （CH 2）n -Ar 1或-XAr 2，n为1至6的整数，Ar 1和Ar 2分别选自 a）由至少一个由游离羧基，烷氧基羰基和与药学上可接受的碱成盐的羧基取代的至多18个碳原子的碳环芳基，-OH，卤素，-NO 2，-CN， 烷基，环烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，烯硫基，炔硫基，任选被至少一个卤素取代的具有12个碳原子的N-烷基，N-烯基和N-炔基R1和R2 单独的氢或1至12个碳原子的烷基，b）其中R 3选自1至12个碳原子的烷基，任选取代的碳环芳基，芳氧基和芳硫基，任选取代的杂环芳基，芳氧基和芳硫基 含有至少一个杂原子 任选的取代基是上述碳环芳基的取代基，X是被-O - ， - S - ， - SO - ， - SO 2，-CO-， - CO-的成员间隔的1至6个碳原子的烷基， Z是具有至多18个碳原子的有机羧酸的氢或酰基，以及它们对革兰氏阳性和革兰氏阴性菌具有抗生素活性的无毒的药学上可接受的酸加成盐。