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79 条记录 (耗时 0.04 秒)

    Combinatorial synthesis of PEG oligomer libraries
    31.
    发明申请
    Combinatorial synthesis of PEG oligomer libraries 有权
    PEG寡聚体文库的组合合成

    公开(公告)号：US20060008850A1

    公开(公告)日：2006-01-12

    申请号：US11174938

    申请日：2005-07-05

    申请人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    发明人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    IPC分类号： C07C41/03 ,  G01N33/53

    CPC分类号： C07C43/11 ,  C07C69/28

    摘要： A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.

    摘要翻译： 建立了一种简单的扩链方法，用于单保护单分散PEG二醇材料的放大。 THP-（OCH 2 CH 2 CH 2）n -OMs（n = 4,8,12）与大量可商购的反应 在碱性条件下，H（OCH 2 CH 2 CH 2）n -OH（n = 1-4）导致THP-（OCH 2 H 2 -OH（n = 5-15）。 类似地，Me-（OCH 2 CH 2 CH 2）n -OH（n = 4-11,13）由Me-（OCH （n = 3，7，11）n -OMs（n = 3,7,11）。 对于链延伸步骤，通过萃取纯化获得40-80％的产率。 通过烷基化或酰化THP-（OCH 2 CH 2 CH 2）n H 2生成PEG低聚物文库I和II，其总产率为50-95％ -OH（n = 1-15），随后脱保护。 使用X-（CH

    Immunoregulatory compounds and derivatives and methods of treating diseases therewith
    32.
    发明申请
    Immunoregulatory compounds and derivatives and methods of treating diseases therewith 有权
    免疫调节化合物及其治疗疾病的衍生物和方法

    公开(公告)号：US20050228051A1

    公开(公告)日：2005-10-13

    申请号：US11144093

    申请日：2005-06-03

    申请人： Nnochiri Ekwuribe ,  Jennifer Riggs-Sauthier

    发明人： Nnochiri Ekwuribe ,  Jennifer Riggs-Sauthier

    IPC分类号： A61P1/04 ,  A61K31/194 ,  A61K31/195 ,  A61K31/196 ,  A61K31/215 ,  A61K31/606 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07C245/08

    CPC分类号： A61K31/195 ,  A61K31/196 ,  A61K31/215 ,  A61K31/24 ,  C07C229/42 ,  C07C245/08 ,  Y02A50/475 ,  Y02A50/481 ,  A61K2300/00

    摘要： Compounds are disclosed having the structure of Formula I: where R1 , R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and -C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

    摘要翻译： 公开了具有式I结构的化合物：其中R 1，R 3和R 4独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C C 1至C 4烷基，或其中R 6，R 7和R 8是 独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。 这些化合物可用于预防或治疗各种疾病，特别是GI道的炎性病症。 还公开了使用具有下式的化合物治疗胃肠道炎症性疾病如炎症性肠病的方法：其中R 9，R 10和R 11 独立地选自氢和C 1至C 4烷基，R 12选自基团 由氢和-C（O）R 13组成，其中R 13是C 1至C 6 - 烷基或芳基。

    N-Optionally Substituted Aryl-2-Oligomer-3-Alkoxypropionamides
    34.
    发明申请
    N-Optionally Substituted Aryl-2-Oligomer-3-Alkoxypropionamides 有权
    N-任选取代的芳基-2-低聚物-3-烷氧基丙酰胺

    公开(公告)号：US20140296334A1

    公开(公告)日：2014-10-02

    申请号：US13879603

    申请日：2011-10-14

    申请人： Jennifer Riggs-Sauthier ,  Wen Zhang

    发明人： Jennifer Riggs-Sauthier ,  Wen Zhang

    IPC分类号： A61K47/48

    CPC分类号： A61K47/60 ,  A61K31/165 ,  C07D235/22

    摘要： The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.

    摘要翻译： 本发明涉及（尤其是）N-任选取代的芳基-2-低聚物-3-烷氧基丙酰胺及其组合物。 当通过任何多种施用途径给药时，本发明的化合物相对于缺乏寡聚体的相应化合物显示出一个或多个优点。

    Oligomer-diarylpiperazine conjugates
    36.
    发明授权
    Oligomer-diarylpiperazine conjugates 有权
    低聚 - 二芳基哌嗪共轭物

    公开(公告)号：US08685979B2

    公开(公告)日：2014-04-01

    申请号：US12864481

    申请日：2009-01-22

    申请人： Zhongxu Ren ,  Jennifer Riggs-Sauthier

    发明人： Zhongxu Ren ,  Jennifer Riggs-Sauthier

    IPC分类号： A61K31/495 ,  C07D241/04

    CPC分类号： A61K31/495 ,  A61K47/48215 ,  A61K47/60 ,  C07D241/04

    摘要： The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.

    摘要翻译： 本发明涉及（尤其是）低聚物 - 二芳基哌嗪共轭物和相关化合物。 本发明的缀合物当通过任何多种施用途径施用时，显示出优于先前施用的未共轭二芳基哌嗪化合物的优点。