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    IMMUNOREGULATORY COMPOUNDS AND DERIVATIVES AND METHODS OF TREATING DISEASES THEREWITH
    1.
    发明申请
    IMMUNOREGULATORY COMPOUNDS AND DERIVATIVES AND METHODS OF TREATING DISEASES THEREWITH 有权
    免疫组化化合物及其衍生物及其治疗疾病的方法

    公开(公告)号：US20070004800A1

    公开(公告)日：2007-01-04

    申请号：US11470655

    申请日：2006-09-07

    申请人： Nnochiri Ekwuribe ,  Jennifer Riggs-Sauthier

    发明人： Nnochiri Ekwuribe ,  Jennifer Riggs-Sauthier

    IPC分类号： A61K31/24 ,  A61K31/195

    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。

    Synthesis of Azo Bonded Immunoregulatory Compounds
    2.
    发明申请
    Synthesis of Azo Bonded Immunoregulatory Compounds 有权
    偶氮键合的免疫调节化合物的合成

    公开(公告)号：US20080033153A1

    公开(公告)日：2008-02-07

    申请号：US11631582

    申请日：2005-07-07

    申请人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    发明人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    IPC分类号： C07C245/08

    CPC分类号： C07C245/08

    摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4are 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. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

    摘要翻译： 公开了制备式I化合物的方法：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。 该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。 适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。 所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。 化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。

    Immunoregulatory compounds and derivatives and methods of treating diseases therewith
    3.
    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：US20050054728A1

    公开(公告)日：2005-03-10

    申请号：US10967736

    申请日：2004-10-18

    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至C 4烷基，R 2是：其中R 5选自 由氢和C 1至C 4烷基组成的组，或其中R 6，R 7和R 8独立地为氢或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状况如炎性肠病的方法：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选自氢和-C（O）R 13，其中R 13为C 1至C 6烷基或芳基。

    Combinatorial synthesis of PEG oligomer libraries
    4.
    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
    5.
    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。

    Oligomer modified diaromatic substituted compounds
    7.
    发明授权
    Oligomer modified diaromatic substituted compounds 有权
    低聚物改性的二芳基取代的化合物

    公开(公告)号：US09226970B2

    公开(公告)日：2016-01-05

    申请号：US13580580

    申请日：2011-02-22

    申请人： Jennifer Riggs-Sauthier ,  Bo-Liang Deng

    发明人： Jennifer Riggs-Sauthier ,  Bo-Liang Deng

    IPC分类号： A61K31/497 ,  A61K47/48

    CPC分类号： A61K31/496 ,  A61K47/60

    摘要： Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) (PEG) oligomers. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds.

    摘要翻译： 公开了包含二芳基取代的化合物残基的化合物，即通过连接至水溶性非肽寡聚物，特别是与聚（乙二醇）（PEG）低聚物共价连接的抗病毒（抗HIV）药物地拉夫定。 本发明的化合物当通过任何多种施用途径给药时，显示出优于非低聚物修饰的二芳基取代化合物的优点。