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。

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.

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。