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    Synthesis of Azo Bonded Immunoregulatory Compounds
    1.
    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。

    Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties
    4.
    发明申请
    Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties 有权
    具有聚乙二醇部分的聚合物的主要单分散混合物

    公开(公告)号：US20050059799A1

    公开(公告)日：2005-03-17

    申请号：US10977973

    申请日：2004-10-29

    申请人： Nnochiri Ekwuribe ,  Christopher Price ,  Aslam Ansari ,  Amy Odenbaugh

    发明人： Nnochiri Ekwuribe ,  Christopher Price ,  Aslam Ansari ,  Amy Odenbaugh

    IPC分类号： C07C41/16 ,  C07C43/13 ,  C08G65/08 ,  C08G65/334 ,  C08L71/02 ,  C12N5/00

    CPC分类号： C08G65/334 ,  C08L71/02 ,  C08L71/00

    摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)b—O−X+  (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMs   (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1   (III). Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.

    摘要翻译： 合成包含聚乙二醇部分的聚合物的基本上单分散的混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：R 1（OC 2 H 4）b O - X +（I） 1>是H或亲脂性部分; n为1至25; 并且X +是具有式II结构的化合物的基本上单分散的混合物：R 2（OC 2 H 4）m-OM（II）其中R 2是H或亲油部分; 并且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本单分散混合物的条件下：R 2（OC 2 H 4）m + n -OR 1（III）。 还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。

    Taxane prodrugs
    6.
    发明授权
    Taxane prodrugs 失效
    紫杉烷前药

    公开(公告)号：US06380405B1

    公开(公告)日：2002-04-30

    申请号：US09476974

    申请日：1999-12-31

    申请人： Nnochiri Ekwuribe ,  Gary S. Bartley ,  Christopher H. Price

    发明人： Nnochiri Ekwuribe ,  Gary S. Bartley ,  Christopher H. Price

    IPC分类号： C07D30514

    CPC分类号： A61K33/24 ,  A61K45/06 ,  A61K47/60 ,  Y02A50/411 ,  A61K2300/00

    摘要： The present invention generally provides taxane prodrugs comprising at least one taxane joined by hydrolyzable bond(s) to one or more polyethylene glycol oligomer(s) selected from the group consisting of a straight or branched polyethylene glycol oligomer having from 1 to 25 polyethylene glycol units and optionally comprising a salt-forming moiety. The polyethylene glycol oligomer preferably comprises a salt-forming moiety, which is preferably selected from the group consisting of ammonium and carboxylate.

    摘要翻译： 本发明通常提供紫杉烷前药，其包含至少一种紫杉烷类，其通过可水解键连接到一种或多种选自具有1至25个聚乙二醇单元的直链或支链聚乙二醇低聚物的聚乙二醇低聚物 并且任选地包含成盐部分。 聚乙二醇低聚物优选包含成盐部分，其优选选自铵和羧酸盐。