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    Erythromycin compounds
    6.
    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
    7.
    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。

    Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
    9.
    发明申请
    Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors 审中-公开
    细菌性肝细胞合成的化学抑制剂，其制备方法和所述抑制剂的生物应用

    公开(公告)号：US20100022541A1

    公开(公告)日：2010-01-28

    申请号：US12311278

    申请日：2007-09-25

    申请人： Sonia Escaich ,  Alexis Denis ,  Francois Moreau ,  Vincent Gerusz ,  Nicolas Desroy

    发明人： Sonia Escaich ,  Alexis Denis ,  Francois Moreau ,  Vincent Gerusz ,  Nicolas Desroy

    IPC分类号： A61K31/5377 ,  C12Q1/66 ,  C07D413/12 ,  A61K31/437

    CPC分类号： C07D417/14 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

    摘要： The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C═NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.

    摘要翻译： 本发明涉及具有式（I）的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药，其中A是芳基或杂环，任选被一个或多个相同或不同的R如H，C1 C 1 -C 10烷基-OR 1，C 1 -C 10烷基-NR 1 R 1，烷氧基，羟基，硫代烷基，芳基，杂环，卤素，硝基，氰基，CO 2 R 1，NR 1 R 1，NR 1 C（O）R 1，C（O）NR 1 R 1， NR 1 C（S）R 1，C（S）NR 1 R 1，SO 2 NR 1 R 1，SO 2 R 1，NR 1 SO 2 R 1，NR 1 C（O）NR 1 R 1，NR 1 C（O）OR 1，NR 1 C R1，芳氧基，硫代芳基，烯基，炔基R1相同或不同，是H或C1-C10烷基B1，B2，B3相同或不表示C，N，O，S，形成五元芳环，其中一至三碳 原子被选自S，O，N的杂原子替代，任选地被一个或多个相同或不同的R取代，如上定义。B4是C或NY是H，C1-C10烷基，烷氧基，硫代烷基，任选被一个 或几个iden 如W所定义的不同的R是C，O或N，被一个或多个C 1 -C 10烷基取代或不被取代，D是任选被一个或多个相同或不同的R如上所定义的R取代的杂环。