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：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.

公开(公告)号：US11634404B2

公开(公告)日：2023-04-25

申请号：US16093365

申请日：2017-04-14

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services ,  The University of Kansas ,  The University of North Carolina at Chapel Hill

Inventor： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC: C07D401/12 ,  A61P25/28 ,  C07D295/185 ,  C07D209/42 ,  C07D213/65 ,  C07D213/81 ,  C07D235/24 ,  C07D307/85 ,  C07D317/64 ,  C07D333/70 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

Abstract: The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

公开(公告)号：US20230312511A1

公开(公告)日：2023-10-05

申请号：US18111241

申请日：2023-02-17

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ,  The University of Kansas ,  The University of North Carolina at Chapel Hill

Inventor： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC: C07D401/12 ,  A61P25/28 ,  C07D209/42 ,  C07D213/65 ,  C07D213/81 ,  C07D235/24 ,  C07D295/185 ,  C07D307/85 ,  C07D317/64 ,  C07D333/70 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

CPC classification number: C07D401/12 ,  A61P25/28 ,  C07D209/42 ,  C07D213/65 ,  C07D213/81 ,  C07D235/24 ,  C07D295/185 ,  C07D307/85 ,  C07D317/64 ,  C07D333/70 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

Abstract: The disclosure of a compound of Formula I or a pharmaceutically acceptable salt thereof




The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula I together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula I is administered to the patient together with one or more additional active agents.

公开(公告)号：US12145922B2

公开(公告)日：2024-11-19

申请号：US18111241

申请日：2023-02-17

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services ,  The University of Kansas ,  The University of North Carolina at Chapel Hill

Inventor： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC: C07D401/12 ,  A61P25/28 ,  C07D209/42 ,  C07D213/65 ,  C07D213/81 ,  C07D235/24 ,  C07D295/185 ,  C07D307/85 ,  C07D317/64 ,  C07D333/70 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

Abstract: The disclosure of a compound of Formula I or a pharmaceutically acceptable salt thereof The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula I together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula I is administered to the patient together with one or more additional active agents.

公开(公告)号：US20210323941A1

公开(公告)日：2021-10-21

申请号：US16093365

申请日：2017-04-14

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ,  The University of Kansas

Inventor： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC: C07D401/12 ,  C07D209/42 ,  C07D471/04 ,  C07D409/12 ,  C07D235/24 ,  C07D405/12 ,  C07D295/185 ,  C07D213/65 ,  C07D213/81 ,  C07D317/64 ,  C07D307/85 ,  C07D333/70 ,  A61P25/28

Abstract: The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

公开(公告)号：US09745261B2

公开(公告)日：2017-08-29

申请号：US14897445

申请日：2014-06-10

Applicant: THE GENERAL HOSPITAL CORPORATION ,  THE BROAD INSTITUTE, INC. ,  UNIVERSITY OF KANSAS

Inventor： Patrick Faloon ,  Warren S. Weiner ,  Robert A. Smith ,  Frank John Schoenen ,  David E. Fisher ,  Rizwan Haq

IPC: C07C311/16 ,  A61K31/18 ,  C07C311/17 ,  C07D333/34 ,  C07D409/12 ,  C07D209/48 ,  C07D307/91 ,  C07D307/68 ,  A61K31/4184

CPC classification number: C07C311/17 ,  A61K31/4184 ,  C07D209/48 ,  C07D307/68 ,  C07D307/91 ,  C07D333/34 ,  C07D409/12

Abstract: Provided herein are compounds of the formula (IV) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful as MITF inhibitors, MITF pathway inhibitors and for the treatment of cancer.