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    Methods of preparing substituted tetracyclines with transition metal-based chemistries
    66.
    发明公开
    Methods of preparing substituted tetracyclines with transition metal-based chemistries 审中-公开

    公开(公告)号：EP2327686A2

    公开(公告)日：2011-06-01

    申请号：EP10182808.5

    申请日：2000-09-13

    申请人： TRUSTEES OF TUFTS COLLEGE

    发明人： Nelson, Mark, L. ,  Rennie, Glen ,  Koza, Darrell

    IPC分类号： C07C231/12 ,  C07C237/26 ,  A61K31/65 ,  A61P31/04

    CPC分类号： C07C237/26 ,  C07C231/12 ,  C07C2603/46

    摘要： The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant antibacterial activity. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed. Such compounds may optionally act as intermediates for making other compounds, e.g., hydrogenation of unsaturated groups on the substituent.

    Substituted tetracycline compounds
    68.
    发明公开
    Substituted tetracycline compounds 审中-公开
    取代四环素 - 维生素

    公开(公告)号：EP2298323A3

    公开(公告)日：2011-05-11

    申请号：EP10184671.5

    申请日：2004-06-25

    申请人： Paratek Pharmaceuticals, Inc.

    发明人： Nelson, Mark, L. ,  Amoo, Victor ,  Kim, Oak, K. ,  Abato, Paul ,  Ohemeng, Kwasi ,  Assefa, Haregwein ,  Berniac, Joel ,  Bhatia, Beena ,  Bowser, Todd ,  Chen, Jackson ,  Grier, Mark ,  Honeyman, Laura ,  Ismail, Mohamed, Y. ,  Mechiche, Rachid ,  Mathews, Jude

    IPC分类号： C07C237/26 ,  A61K31/65

    CPC分类号： C07C237/48 ,  A61K31/65 ,  C07C237/26 ,  C07C271/22 ,  C07C271/54 ,  C07C275/28 ,  C07C275/30 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46

    摘要： A compound of formula II:

    wherein:
    X is CHC(R 13 Y'Y), CR 6' R 6 , S, NR 6 , or O;
    R 2 , R 4' , R 4" , R 7' and R 7" are each hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
    R 4 is NR 4' R 4" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
    R 2' , R 3 , R 10 , R 11 and R 12 are each hydrogen or a pro-drug moiety;
    R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy;
    R 6 and R 6' are independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
    R 7 is NR 7' R 7" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
    R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
    R 9 is -CH 2 NR 9a R 9b or linked with R 10 to form a furanyl ring;
    R 9a is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic,or heteroaromatic;
    R 9b is hydrogen or alkyl;
    R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
    R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
    Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt, ester or prodrug thereof.

    摘要翻译： 式I的化合物：其中：X是CHC（R 13 Y'Y），CR 6'R 6，S，NR 6或O; R 2，R 2'，R 4'和R 4“各自独立地为氢，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环，杂芳族或前药部分; R 4 是NR 4'R 4“，烷基，烯基，炔基，羟基，卤素或氢; R 2'，R 3，R 10，R 11和R 12各自为氢或前药部分; 烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，烷基羰基氧基或芳基羰基氧基; R 5是羟基，氢，硫醇，烷酰基，芳酰基， R 6和R 6'各自独立地为氢，亚甲基，不存在，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳烷基。 R 7是乙基，全卤代烯基，取代的吡啶基，吡嗪基，呋喃基或吡唑基; R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 9 -CH 2 NR 9a R 9b; R 9a和R 9b各自独立地为氢，烷基，烯基或连接形成杂环; R 13是氢，羟基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; 其中Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基或其药学上可接受的盐。