公开(公告)号：US20100029627A1

公开(公告)日：2010-02-04

申请号：US12373404

申请日：2007-07-12

申请人： Alexandra Papanikos ,  Freyne Eddy Jean Edgard ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Fierre-Henri Storck

发明人： Alexandra Papanikos ,  Freyne Eddy Jean Edgard ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Fierre-Henri Storck

IPC分类号： A61K31/541 ,  C07D271/12 ,  A61K31/519 ,  A61K31/496 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D498/14 ,  C08K5/544

摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O—; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(═O)2—C1-4alkyl-C(═O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(═O)2—C1-4alkyl-.

摘要翻译： 本发明涉及式I化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中Y代表-C3-9烷基 - ， - C1-5烷基-NR6-C1-5烷基 - 或-C1- 5烷基-NR 7 -CO-C 1-5烷基 - ; X1表示-O-; X2表示NR5-C1-2烷基 - ; R1代表氢，卤素或Het3-O-; R2表示氢; R 3表示羟基，被一个或两个独立地选自Het4，羟基，C 1-4烷氧基 - ，C 1-4烷氧基-C 1-4烷氧基和NR 9 R 10的取代基取代的C 1-4烷氧基 - 或C 1-4烷氧基; R5代表氢或C1-4烷基; R6代表氢或C1-4烷基; R7代表氢; R9和R10各自独立地表示氢; C 1-4烷基-S（-O）2 -C 1-4烷基-C（-O） - ; 被羟基取代的C 1-4烷基或C 1-4烷基; Het3表示任选被C 1-4烷基取代的吡啶基; Het4表示吗啉基，哌啶基或哌嗪基，其中所述Het4任选被羟基-C 1-4烷基或C 1-4烷基-S（-O）2 -C 1-4烷基取代。