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    PHARMACOKINETICALLY IMPROVED COMPOUNDS
    1.
    发明申请
    PHARMACOKINETICALLY IMPROVED COMPOUNDS 审中-公开
    药物动力学改进的化合物

    公开(公告)号：US20100093719A1

    公开(公告)日：2010-04-15

    申请号：US12570153

    申请日：2009-09-30

    申请人： Stewart CAMPBELL ,  David DUFFY ,  Michael GROGAN ,  Steven KATES ,  Emanuele OSTUNI ,  Olivier SCHUELLER ,  Paul SWEETNAM

    发明人： Stewart CAMPBELL ,  David DUFFY ,  Michael GROGAN ,  Steven KATES ,  Emanuele OSTUNI ,  Olivier SCHUELLER ,  Paul SWEETNAM

    IPC分类号： A61K31/53 ,  C07D487/04 ,  A61P15/00 ,  A61K31/5377

    CPC分类号： C07D487/04

    摘要： A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5 together form a 5- or 6-membered ring, or R6 and R7 together form a 3 to 6 membered ring; R9 is independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; alternatively R8 and R9 together with the nitrogen to which they are attached form a 5- or 6-membered ring; n is 1 to 4; and m is 1 to 6.

    摘要翻译： 提供了具有改善的非特异性结合特征和药代动力学性质的式A化合物：或其药学上可接受的盐，立体异构体或水合物，其中R 1是低级烷基，R 2和R 3独立地选自低级烷基和低级烯基，低级 炔基，其中低级烷基，低级烯基和低级炔基可以任选被一个或多个卤素，低级烷氧基，羟基，CN，NO 2，氨基，酰氨基，酰氨基，羰基和烷硫基取代，A是N或C-H ，B是N，C-H，C-（SO2-R4）或C-CO-R4，D是N，C-H，C-（SO2-R4）或C-CO-R4，E是N或 C-H，其中A，B或E中只有一个可以是N，B或D中的一个是C-（SO 2 -R 4）或C-CO-R 4，R 4是下式的基团：其中每个R 5 ，R6，R7和R8独立地选自H和低级烷基，其中低级烷基可以任选地被一个或多个卤素，低级烷氧基，羟基，CN，NO 2，氨基，酰氨基，酰氨基，羰基和烷基 io 另外或可选地，R6和R5一起形成5-或6-元环，或者R6和R7一起形成3至6元环; R 9独立地选自H和低级烷基，其中低级烷基可以任选被一个或多个卤素，低级烷氧基，羟基，CN，NO 2，氨基，酰氨基，酰氨基，羰基和烷硫基取代; 或者R8和R9与它们所连接的氮一起形成5-或6-元环; n为1〜4; m为1〜6。