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    Antagonists of the kappa opioid receptor
    21.
    发明授权
    Antagonists of the kappa opioid receptor 有权

    公开(公告)号：US10118896B2

    公开(公告)日：2018-11-06

    申请号：US15529290

    申请日：2015-11-25

    Applicant: University of Kansas

    Inventor： Jeffrey Aube ,  Kevin Frankowski ,  Thomas Prisinzano ,  Laura Bohn

    IPC: C07D217/08 ,  C07D209/44 ,  C07D223/16

    Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like kappa opioid receptor (KOR) antagonists. The technology is suited to treat addiction, diuresis, depression, post traumatic stress disorder, an eating disorder, panic disorder, social anxiety disorder, general anxiety disorder, obsessive compulsive disorders, excessive or unreasonable specific phobias, and/or other conditions related to anxiety or aversion-reward responses.

    SYNTHESIS OF FUNCTIONALIZED OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXYLIC ESTERS AND ANALOGS, AND THERAPEUTIC METHODS
    26.
    发明申请
    SYNTHESIS OF FUNCTIONALIZED OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXYLIC ESTERS AND ANALOGS, AND THERAPEUTIC METHODS 审中-公开
    官能化OCTAHYDRO-异喹啉-1-酮-8-羧酸酯和类似物的合成及其治疗方法

    公开(公告)号：US20140243333A1

    公开(公告)日：2014-08-28

    申请号：US14276195

    申请日：2014-05-13

    Applicant: University of Kansas ,  University of North Carolina

    Inventor： Jeffrey Aube ,  Bryan L. Roth ,  Partha Ghosh ,  Kevin J. Frankowski

    IPC: C07D217/24 ,  C07D401/06 ,  C07D417/12 ,  C07D413/06

    CPC classification number: C07D217/24 ,  A61K31/472 ,  C07D217/22 ,  C07D401/06 ,  C07D413/06 ,  C07D417/12

    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.

    Abstract translation: 官能化的多环化合物可以具有式1或其盐，前药，类似物或衍生物的结构，该化合物可以通过提供二烯制备; 使二烯与亲二烯体在足够的条件下进行组合的狄尔斯 - 阿尔德/酰化反应，以提供具有羧酸的多环化合物; 并将羧酸与含胺化合物或含羟基化合物偶联以形成酰胺或酯，并制备具有式1结构的化合物。该化合物可用于调节阿片受体，其可以 通过向阿片样受体施用如本文所述的官能化多环化合物以有效量来调节阿片受体的功能性来进行。 这种阿片样物质调节可以为受试者提供生物学益处。

    Modulators of GTPase and Use In Relevant Treatment
    29.
    发明申请
    Modulators of GTPase and Use In Relevant Treatment 有权
    GTPase调节剂和相关治疗用途

    公开(公告)号：US20130345277A1

    公开(公告)日：2013-12-26

    申请号：US13867658

    申请日：2013-04-22

    Applicant: STC.UNM ,  Kansas University Center for Technology Commercialization, Inc.

    Inventor： Angela Wandinger-Ness ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea ,  Laurie Hudson ,  Jeffrey Aube ,  Jennifer E. Golden ,  Chad E. Schroeder ,  Denise S. Simpson ,  Julica J. Noth

    IPC: A61K31/415 ,  A61K45/06 ,  C07D231/06

    CPC classification number: A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/573 ,  Y02A50/473 ,  Y02A50/486 ,  A61K2300/00

    Abstract: The present invention relates to molecules which function as selective modulators of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role, such as neurodegenerative diseases, rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney disease, cystic kidney disease, precystic kidney disease, microbial infections, including Chlamydia infections, E. coli infections, H. pylori infections and its secondary effects including gastric ulcers, Coxiella Brunetti (Q-fever) infections and Streptococcus pneumonia infections, fungal infections including Paracoccidiodes brasiliensis and Candida albicans and their secondary effects including lung edema. Additionally, compounds according to the present invention may be used to inhibit rejection in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others.

    Abstract translation: 本发明涉及用作小GTP酶的Ras同源（Rho）家族，特别是Cdc42GTP酶的选择性调节剂的分子及其用于治疗疾病的用途，例如癌症，包括转移性癌症，遗传和获得性疾病，其中激活 的Cdc42 GTPase起着关键的作用，如神经退行性疾病，类风湿关节炎，动脉粥样硬化，I型糖尿病，常染色体多囊肾病，囊性肾病，前期肾脏疾病，微生物感染，包括衣原体感染，大肠杆菌感染，幽门螺杆菌 感染及其次要作用包括胃溃疡，布氏梭菌（Qex fever）感染和肺炎链球菌感染，包括巴西隐孢子虫和白色念珠菌在内的真菌感染及其副作用，包括肺水肿。 此外，根据本发明的化合物可以用于抑制移植患者的排斥（根据移植），以促进免疫抑制，抗炎反应和在需要的患者中调动干细胞（迁移）等。

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