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    Pharmacokinetically Improved Compounds
    3.
    发明申请
    Pharmacokinetically Improved Compounds 审中-公开

    公开(公告)号：US20080176844A1

    公开(公告)日：2008-07-24

    申请号：US11884832

    申请日：2006-02-21

    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： A61K31/5355 ,  C07D487/02 ,  A61P15/10 ,  A61K31/53

    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.