公开(公告)号：US07772241B2

公开(公告)日：2010-08-10

申请号：US12349813

申请日：2009-01-07

申请人： Modesto Remuinan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Andres Francesh ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Regan James Anderson ,  Jonathan Charles Morris

发明人： Modesto Remuinan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Andres Francesh ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Regan James Anderson ,  Jonathan Charles Morris

IPC分类号： A61K31/519 ,  C07D473/00

CPC分类号： C07D213/64 ,  C07D213/78 ,  C07D239/38 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/06 ,  C07D471/14

摘要： Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, 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, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

摘要翻译： 提供了式（5）的衍生物，其中由X2，R1，R2，R3，R6，R7和R12定义的取代基各自独立地选自H，OH，OR'，SH，SR' ，SOR'，SO2R'，NO2，NH2，NHR'，N（R'）2，NHCOR'，NHSO2R'，CN，卤素，= O，C（= O）H，C（= O）R' ，CO 2 R'，羧基烷基，C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12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杂芳族; 其中每个R'基团独立地选自H，OH，SH，NO 2，NH 2，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3， C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基，芳基，芳烷基和杂芳族; 其中R 1和R 2，R 2和R 3，R 3和R 12，R 12和R 6，或R 6和R 7的这些基团可以连接成碳环或杂环系。

公开(公告)号：US07495000B2

公开(公告)日：2009-02-24

申请号：US10483525

申请日：2002-07-11

申请人： Modesto Remuiñan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Carmen Cuevas ,  Simon Munt ,  Regan James Anderson ,  Andres Francesh ,  Jonathan Charles Morris ,  Ignacio Manzanares

发明人： Modesto Remuiñan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Carmen Cuevas ,  Simon Munt ,  Regan James Anderson ,  Andres Francesh ,  Jonathan Charles Morris ,  Ignacio Manzanares

IPC分类号： A61K31/506 ,  C07D239/06

CPC分类号： C07D213/64 ,  C07D213/78 ,  C07D239/38 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/06 ,  C07D471/14

摘要： Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7 and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, 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, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

摘要翻译： 提供了式（5）的异喹啉衍生物，其中由X 2，R 1，R 2，R 3，R 6，R 7和R 12定义的取代基各自独立地选自H，OH，OR'，SH，SR' SOR'，SO 2 R'，NO 2，NH 2，NHR'，N（R'）2，NHCOR'，NHSO 2 R'，CN，卤素，-O，C（-O）H，C（-O）R' CO 2 R'，羧基烷基，C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12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杂芳族; 其中每个R'基团独立地选自H，OH，SH，NO 2，NH 2，CN，卤素，-O，C（-O）H，C（-O）CH 3，CO 2 H，CO 2 CH 3， C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基，芳基，芳烷基和杂芳族; 其中基团R 1和R 2，R 2和R 3，R 3和R 12，R 12和R 6，或R 6和R 7的对可以连接成碳环或杂环系。