公开(公告)号：US20150322087A1

公开(公告)日：2015-11-12

申请号：US14439373

申请日：2013-11-04

Applicant: UNIVERSITY OF KANSAS ,  CORNELL UNIVERSITY

Inventor： Jeffrey Aube ,  Carl Nathan ,  Robert Smith ,  Ben S. Gold ,  Paul Hanson ,  Chunjing Liu ,  Lester Allen Mitscher ,  Maneesh Pingle ,  Frank John Schoenen

IPC: C07D501/16 ,  A61K31/43 ,  C07D277/06 ,  A61K31/426 ,  A61K45/06 ,  A61K31/427 ,  C07D513/04 ,  A61K31/429 ,  A61K31/545 ,  A61K31/546 ,  C07D499/44 ,  C07D417/12

CPC classification number: C07D501/16 ,  A61K31/426 ,  A61K31/427 ,  A61K31/429 ,  A61K31/43 ,  A61K31/431 ,  A61K31/4725 ,  A61K31/545 ,  A61K31/546 ,  A61K45/06 ,  C07D277/06 ,  C07D417/12 ,  C07D499/44 ,  C07D513/04 ,  Y02A50/401 ,  Y02A50/402 ,  A61K2300/00

Abstract: This invention provides cephalosporin derivatives for killing or inhibiting the spread of microorganisms such as non-replicating Mycobacterium tuberculosis and in the treatment of infectious disease.

Abstract translation: 本发明提供头孢菌素衍生物用于杀死或抑制微生物如非复制型结核分枝杆菌的扩散和用于治疗感染性疾病。

公开(公告)号：US20150197526A1

公开(公告)日：2015-07-16

申请号：US14587925

申请日：2014-12-31

Applicant: STC.UNM ,  UNIVERSITY OF KANSAS

Inventor： Richard Smith Larson ,  Larry A. Sklar ,  Bruce S. Edwards ,  Juan Jacob Strouse ,  Irena Ivnitski-Steele ,  Hydya M. Khawaja ,  Jerec Warren Ricci ,  Jeffrey Aube ,  Jennifer Elizabeth Golden ,  Tuanli Yao ,  Warren S. Weiner ,  Chad E. Schroeder

IPC: C07D487/04 ,  A61K31/4745 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/519 ,  A61K45/06

Abstract: The present invention provides novel compounds which inhibit cancer-associated transporter proteins, methods of treating or preventing the onset of a cancer-associated transporter protein-mediated disease by administering such compounds, and pharmaceutical compositions comprising such compounds. In one embodiment, the invention provides novel pyrazolo[1,5-a]pyrimidine efflux inhibitors that are selective toward ABCG2 over ABCB1.

Abstract translation: 本发明提供抑制癌症相关转运蛋白的新型化合物，通过施用这些化合物治疗或预防癌症相关转运蛋白介导的疾病发作的方法，以及包含这些化合物的药物组合物。 在一个实施方案中，本发明提供了关于ABCB1对ABCG2有选择性的新型吡唑并[1,5-a]嘧啶外排抑制剂。

公开(公告)号：US09056111B1

公开(公告)日：2015-06-16

申请号：US13622651

申请日：2012-09-19

Applicant: STC.UNM ,  UNIVERSITY OF KANSAS

Inventor： Richard Smith Larson ,  Larry A. Sklar ,  Bruce S. Edwards ,  Juan Jacob Strouse ,  Irena Ivnitski-Steele ,  Hadya M. Khawaja ,  Jerec Warren Ricci ,  Jeffrey Aube ,  Jennifer Elizabeth Golden ,  Tuanli Yao ,  Warren S. Weiner ,  Chad E. Schroeder

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  A61K31/437 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/519 ,  A61K45/06

Abstract: The present invention provides pyrazolo[1,5-a]pyrimidine compounds which inhibit cancer-associated transporter proteins, methods of treating or preventing the onset of a cancer-associated transporter protein-mediated disease by administering such compounds, and pharmaceutical compositions comprising such compounds. In one embodiment, the invention provides pyrazolo[1,5-a]pyrimidine efflux inhibitors that are selective toward ABCG2 over ABCB1. Compounds and compositions according to the present invention may be used to treat cancer, including drug resistant (DR) and multiple drug resistant (MDR) cancers.

Abstract translation: 本发明提供了抑制癌症相关转运蛋白的吡唑并[1,5-a]嘧啶化合物，通过施用这些化合物来治疗或预防与癌症相关的转运蛋白介导的疾病发作的方法，以及包含这些化合物的药物组合物 。 在一个实施方案中，本发明提供对ABCB1而言对ABCG2有选择性的吡唑并[1,5-a]嘧啶外排抑制剂。 根据本发明的化合物和组合物可用于治疗癌症，包括耐药性（DR）和多重耐药性（MDR）癌症。

公开(公告)号：US20150119411A1

公开(公告)日：2015-04-30

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 ,  C12N7/00 ,  C07D405/12

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：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。

公开(公告)号：US09611270B2

公开(公告)日：2017-04-04

申请号：US14815686

申请日：2015-07-31

Applicant: University of Kansas

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

IPC: C07D487/04 ,  C07J73/00 ,  C07J71/00 ,  C07J43/00 ,  C07D401/04 ,  C07J31/00 ,  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.

公开(公告)号：US09580393B2

公开(公告)日：2017-02-28

申请号：US14651777

申请日：2013-12-13

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

CPC classification number: C07D409/04 ,  C07D239/90 ,  C07D239/91 ,  C07D239/95 ,  C07D241/06 ,  C07D401/04 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12

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).

Abstract translation: 本技术涉及式I-III的化合物和组合物以及使用这些化合物的方法。 本文所述的化合物和组合物可用于治疗或预防与甲病毒属例如委内瑞兰马脑炎病毒（VEEV）相关的疾病。

公开(公告)号：US20160244457A1

公开(公告)日：2016-08-25

申请号：US15147648

申请日：2016-05-05

Applicant: UNIVERSITY OF KANSAS ,  STC.UNM

Inventor： Richard Smith Larson ,  Larry A. Sklar ,  Bruce S. Edwards ,  Juan Jacob Strouse ,  Irena lvnitski-Steele ,  Hadya M. Khawaja ,  Jerec Warren Ricci ,  Jeffrey Aube ,  Jennifer Elizabeth Golden ,  TuanIi Yao ,  Warren S. Weiner ,  Chad E. Schroeder

IPC: C07D487/04 ,  A61K31/4745 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/519 ,  A61K45/06

Abstract: The present invention provides novel compounds which inhibit cancer-associated transporter proteins, methods of treating or preventing the onset of a cancer-associated transporter protein-mediated disease by administering such compounds, and pharmaceutical compositions comprising such compounds. In one embodiment, the invention provides novel pyrazolo[1,5-a]pyrimidine efflux inhibitors that are selective toward ABCG2 over ABCB1.