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    Total Synthesis of Myriaporones
    1.
    发明申请
    Total Synthesis of Myriaporones 失效
    全氟化氢的合成

    公开(公告)号：US20080269511A2

    公开(公告)日：2008-10-30

    申请号：US10523172

    申请日：2005-09-01

    申请人： Carlos del Pozo Losada ,  Andres Francesch Solloso ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    发明人： Carlos del Pozo Losada ,  Andres Francesch Solloso ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    IPC分类号： C07D407/02 ,  C07D303/34

    CPC分类号： C07D407/06 ,  A61K31/35 ,  C07D493/08 ,  Y02P20/55

    摘要： Compounds of the general formula (I) or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR′3, SOR′, SO2X, C(═O)R′, C(═O)OR′, C(═O)NR′, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R′ is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R″ is selected from the group consisting of H, OH, OR′, OCOR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, N(COR′)2, NHSO2R′, CN, halogen, C(═O)H, C(═O)R′, CO2H, CO2R′, CH2OR, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of U.S. Pat. No. 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.

    摘要翻译： 提供了通式（I）化合物或其药学上可接受的盐，衍生物，前药或立体异构体：其中由R定义的取代基各自独立地选自H，SiR'3 （O）OR'，C（ - ）NR'，取代或未取代的烷基，取代或未取代的链烯基， 取代或未取代的炔基，芳基，杂芳基或芳烷基; 基团R'选自取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，氨基烷基，芳基，芳烷基和杂环基; 并且基团R“选自H，OH，OR'，OCOR'，SH，SR'，SOR'，SO 2 R'，NO 2， NH 2，NH 2，NH 2，NH 2，NH 2，NH 2，NH 2，NH 3， R 2，R 2，R 2，R 2，R 2，R 2，R 2，R 3， 取代或未取代的烷基，取代或未取代的烷基，取代或未取代的亚烷基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的芳烷基和取代或未取代的芳烷基 杂芳族; 条件是该化合物不是美国专利号4,3,3或4的化合物1,3或4。 第5,514,708号。 该化合物具有抗肿瘤活性。 还提供了合成路线。

    Total Synthesis of Myriaporones
    2.
    发明申请
    Total Synthesis of Myriaporones 失效
    全氟化氢的合成

    公开(公告)号：US20080103320A2

    公开(公告)日：2008-05-01

    申请号：US10523172

    申请日：2005-09-01

    申请人： Carlos del Pozo Losada ,  Andres Francesch Solloso ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    发明人： Carlos del Pozo Losada ,  Andres Francesch Solloso ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    IPC分类号： C07D407/02 ,  C07D303/34

    CPC分类号： C07D407/06 ,  A61K31/35 ,  C07D493/08 ,  Y02P20/55

    摘要： Compounds of the general formula (I) or pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR′3, SOR′, SO2X, C(═O)R′, C(═O)OR′, C(═O)NR′, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R′ is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R″ is selected from the group consisting of H, OH, OR′, OCOR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, N(COR′)2, NHSO2R′, CN, halogen, C(=O)H, C(=O)R′, CO2H, CO2R′, CH2OR, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of U.S. Pat. No. 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.

    Total synthesis of myriaporones
    3.
    发明授权
    Total synthesis of myriaporones 失效
    全氟化氢的合成

    公开(公告)号：US07521478B2

    公开(公告)日：2009-04-21

    申请号：US10523172

    申请日：2003-07-30

    申请人： Carlos del Pozo Losada ,  Andres Francesch ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    发明人： Carlos del Pozo Losada ,  Andres Francesch ,  Carmen Cuevas Marchante ,  Marta Perez Alvarez

    IPC分类号： A61K31/336 ,  C07D301/27 ,  C07D303/12

    CPC分类号： C07D407/06 ,  A61K31/35 ,  C07D493/08 ,  Y02P20/55

    摘要： Compounds of the general formula (I) or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR′3, SOR′, SO2X, C(═O)R′, C(═O)OR′, C(═O)NR′, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R′ is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R″ is selected from the group consisting of H, OH, OR′, OCOR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, N(COR′)2, NHSO2R′, CN, halogen, C(═O)H, C(═O)R′, CO2H, CO2R′, CH2OR, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of U.S. Pat. No. 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.

    摘要翻译： 提供了通式（I）的化合物或其药学上可接受的盐，衍生物，前药或立体异构体：其中由R定义的取代基各自独立地选自H，SiR'3，SOR'，SO2X， C（-O）R'，C（-O）OR'，C（-O）NR'，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，芳基，杂芳基或芳烷基; 基团R'选自取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，氨基烷基，芳基，芳烷基和杂环基; 并且基团R“选自H，OH，OR'，OCOR'，SH，SR'，SOR'，SO 2 R'，NO 2，NH 2，NHR'，N（R'）2，NHCOR' ，N（COR'）2，NHSO 2 R'，CN，卤素，C（-O）H，C（-O）R'，CO 2 H，CO 2 R'，CH 2 OR，取代或未取代的烷基，取代或未取代的卤代烷基，取代或未取代的 取代或未取代的芳基，取代或未取代的芳烷基和取代或未取代的杂芳族; 条件是该化合物不是美国专利号4,3,4或4的化合物1,3或4。 第5,514,708号。 该化合物具有抗肿瘤活性。 还提供了合成路线。

    Antitumoral analogs of lamellarins
    7.
    发明申请
    Antitumoral analogs of lamellarins 失效

    公开(公告)号：US20060173030A1

    公开(公告)日：2006-08-03

    申请号：US10524151

    申请日：2003-08-13

    申请人： Christian Bailly ,  Andres Francesch ,  Maria Mateo Urbano ,  Jose Jimenez Guerrero ,  Alfredo Pastor Del Castillo ,  Carmen Cuevas Marchante

    发明人： Christian Bailly ,  Andres Francesch ,  Maria Mateo Urbano ,  Jose Jimenez Guerrero ,  Alfredo Pastor Del Castillo ,  Carmen Cuevas Marchante

    IPC分类号： A61K31/4745 ,  C07D491/02 ,  C07D498/02 ,  A61K31/675

    CPC分类号： C07D471/14 ,  C07D491/14

    摘要： New lamellarins are provided of the general formula III wherein X is selected from the group consisting of N, O and S; wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SO2R′, NHR′, N(R′)2, N═R′, NHCOR′, N(COR′)2, NHS02R′, N02, PO(R′2, P02R′, C(=0)H, C(=0)R′, C02H, C02R′, OPO(R′)2, OP02R′, OC(=0)H, OC(=0)R′, N═C(R′)2, substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted C1-C12 haloalkyl, substituted or unsubstituted C2-C12 alkenyl, substituted or unsubstituted C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, N02, NH2, SH, CN, halogen, =0, C(=0)H, C(═O)CH3, C02H, C(=0)R′, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-C18 alkoxyl, substituted or unsubstituted C1-C18 aminoalkyl, substituted or unsubstituted C1-C18 aminoacid, substituted or unsubstituted C1-C18 thioalkyl, substituted or unsubstituted C1-C18 alkylsulfinyl, substituted or unsubstituted C1-C18 alkylsulfonyl; wherein the pairs of groups R1 and R2, R2 and R3, R3 and R4, R3 and R9, R4 and R9, R9 and R5, R9 and R6, or R6 and R7, R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and the dotted line represents an single or double bond; or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof.