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

    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。

    Umbrella holder
    2.
    发明授权
    Umbrella holder 失效
    UMBRELLA持有人

    公开(公告)号:US3700149A

    公开(公告)日:1972-10-24

    申请号:US3700149D

    申请日:1971-01-21

    申请人: MICHAEL GROGAN

    发明人: GROGAN MICHAEL

    IPC分类号: A45B11/02 A45F3/02

    CPC分类号: A45B11/02 A45F2003/025

    摘要: This invention is directed primarily to an elongated hollow substantially rigid member adapted to receive the shaft of an umbrella, and having an elongated filament slidably connected with said elongated hollow member and extending the length of said hollow member, said filament having the central portion thereof formed as a loop adapted to surround the wearer by going over one shoulder and under the opposed arm of the wearer, and the terminal ends thereof surrounding the waist of the wearer; and, means for securing said terminal ends. Also included within the invention is means adapting the elongated hollow member to receive umbrella shafts of different diameters, and insertable means releasably securing the umbrella shaft within the elongated hollow member.

    摘要翻译: 本发明主要涉及适于容纳伞的轴的细长的中空基本上刚性的构件,并且具有与所述细长的中空构件可滑动地连接并延伸所述中空构件的长度的细长细丝,所述细丝的中心部分形成 作为适于通过越过穿着者的一个肩部和相对的臂下方并且其围绕穿着者的腰部的终端围绕佩戴者的环路; 以及用于固定所述终端的装置。 本发明还包括适应细长型中空构件以接收不同直径的伞轴的装置,以及将伞杆可释放地固定在细长型中空构件内的可插入装置。

    Pharmacokinetically Improved Compounds
    9.
    发明申请

    公开(公告)号:US20080176844A1

    公开(公告)日:2008-07-24

    申请号:US11884832

    申请日:2006-02-21

    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.