公开(公告)号：US20190270730A1

公开(公告)日：2019-09-05

申请号：US16149009

申请日：2018-10-01

Applicant: University of Kansas ,  University of Louisville Research Foundation, Inc. ,  Southern Research Institute

Inventor： Jennifer Golden ,  Jeffrey Aube ,  Donghoon Chung ,  Chad Schroeder ,  Tuanli Yao ,  E. Lucile White ,  Nichole A. Tower

IPC: C07D409/04 ,  C07D239/95 ,  C07D409/12 ,  C07D403/06 ,  C07D241/06 ,  C07D239/91 ,  C07D239/90 ,  C07D403/12 ,  C07D401/04

Abstract: The present technology relates to compounds and compositions of Formulas I-III and methods using such compounds. The compounds and compositions described herein may be used in the treatment or prophylaxis of diseases associated with an alphavirus, for example, Venezuelan equine encephalitis virus (VEEV).

公开(公告)号：US20170260141A1

公开(公告)日：2017-09-14

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 ,  C07D223/16 ,  C07D209/44

CPC classification number: 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.

公开(公告)号：US09499496B2

公开(公告)日：2016-11-22

申请号：US14405772

申请日：2013-06-05

Applicant: University of Kansas ,  Southern Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Denise S. Simpson ,  Daniel P. Flaherty ,  Daljit S. Matharu ,  William E. Severson ,  Lynn Rasmussen

IPC: C07D239/96 ,  C07D405/12 ,  C12N7/00 ,  A61K31/517

CPC classification number: C07D239/96 ,  A61K31/517 ,  C07D405/12 ,  C12N7/00 ,  C12N2760/18563

Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.

Abstract translation: 本文描述了用于治疗受试者中呼吸道合胞病毒感染或抑制呼吸道合胞病毒复制的化合物，药物组合物和方法。

公开(公告)号：US20160257685A1

公开(公告)日：2016-09-08

申请号：US15156887

申请日：2016-05-17

Applicant: University of Kansas ,  The Scripps Research Institute

Inventor： Jeffrey Aube ,  Laura Bohn ,  Thomas Edward Prisinzano ,  Frank John Schoenen ,  Kevin J. Frankowski

IPC: C07D471/14 ,  C07D401/14 ,  C07D409/14 ,  C07D401/04 ,  C07D471/04 ,  C07D405/14

CPC classification number: C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

Abstract translation: 本发明是可用于治疗乙醇使用障碍戒断，焦虑和/或抑郁，精神分裂症，躁狂症或创伤后应激障碍的选择性κ阿片受体效应物或其药学上可接受的盐。

公开(公告)号：US09376452B2

公开(公告)日：2016-06-28

申请号：US14278468

申请日：2014-05-15

Applicant: STC.UNM ,  UNIVERSITY OF KANSAS

Inventor： Angela Wandinger-Ness ,  Larry Sklar ,  Jacob Agola ,  Zurab Surviladze ,  Jeffrey Aube ,  Jennifer Golden ,  Chad E. Schroeder ,  Denise S. Simpson

IPC: C07D495/04 ,  A61K31/381 ,  A61K45/06

CPC classification number: C07D495/04 ,  A61K31/381 ,  A61K45/06

Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

Abstract translation: 本发明涉及化合物及其作为Rab7 GTPase的抑制剂或活化剂的用途，用于治疗或预防Rab 7 GTP酶相关疾病如神经病变，癌症，骨骼和脂质储存代谢疾病的发生。 本发明也适用于Rab7灭活或其蛋白质 - 蛋白质相互作用被调节以促进病原体的细胞内存活的感染性疾病。 所描述的化合物作为核苷酸结合的竞争性抑制剂，因此也可用作靶向其他小GTP酶的支架。 一方面，本发明的治疗方法用于治疗或预防遗传性感觉神经病发作，例如Charcot-Marie-Tooth 2B型疾病。 还提供了相关的药物组合物，测定和药物筛选。

公开(公告)号：US10829453B2

公开(公告)日：2020-11-10

申请号：US16179637

申请日：2018-11-02

Applicant: University of Kansas ,  THE SCRIPPS RESEARCH INSTITUTE

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.

公开(公告)号：US20190300486A1

公开(公告)日：2019-10-03

申请号：US16179637

申请日：2018-11-02

Applicant: University of Kansas ,  THE SCRIPPS RESEARCH INSTITUTE

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.

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.

公开(公告)号：US09540375B2

公开(公告)日：2017-01-10

申请号：US15156887

申请日：2016-05-17

Applicant: University of Kansas ,  The Scripps Research Institute

Inventor： Jeffrey Aube ,  Laura Bohn ,  Thomas Edward Prisinzano ,  Frank John Schoenen ,  Kevin J. Frankowski

IPC: C07D403/14 ,  C07D249/12 ,  C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

CPC classification number: C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

Abstract translation: 本发明是可用于治疗乙醇使用障碍戒断，焦虑和/或抑郁，精神分裂症，躁狂症或创伤后应激障碍的选择性κ阿片受体效应物或其药学上可接受的盐。

公开(公告)号：US20160031929A1

公开(公告)日：2016-02-04

申请号：US14815686

申请日：2015-07-31

Applicant: University of Kansas

Inventor： Jeffrey Aube ,  Emily E. Scott ,  Charlie Fehl

IPC: C07J1/00 ,  C07D487/04 ,  C07D401/04 ,  C07J43/00 ,  C07J21/00

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07J21/008 ,  C07J31/006 ,  C07J43/003 ,  C07J71/001 ,  C07J73/005

Abstract: Compounds according to formula I or II are provided. Such compounds are useful in treating cancers, such as leukemia, colon cancer, breast cancer, or prostate cancer by beneficially inhibiting CYP17A1. Pharmaceutical compositions and methods including the compounds are also provided.

Abstract translation: 提供了根据式I或II的化合物。 这些化合物通过有益地抑制CYP17A1可用于治疗癌症，如白血病，结肠癌，乳腺癌或前列腺癌。 还提供了包括该化合物的药物组合物和方法。