公开(公告)号：US10202367B2

公开(公告)日：2019-02-12

申请号：US15317864

申请日：2015-06-12

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

发明人： Tsanyang Liang ,  Zongyi Hu ,  Juan Jose Marugan ,  Noel Terrence Southall ,  Shanshan He ,  Xin Hu ,  Jingbo Xiao ,  Marc Ferrer ,  Wei Zheng ,  Kevin J. Frankowski ,  Frank J. Schoenen ,  Kelin Li

IPC分类号： C07D413/14 ,  A61K31/4545 ,  C07D417/14 ,  C07D471/08 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/06 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/7056 ,  A61K31/7068 ,  A61K38/07 ,  A61K38/13 ,  A61K38/21

摘要： Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.

公开(公告)号：US11766423B2

公开(公告)日：2023-09-26

申请号：US16977305

申请日：2019-03-01

申请人： THE JOHNS HOPKINS UNIVERSITY ,  THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, OFFICE OF TECHNOLOGY TRANSFER, NATIONAL INSTITUTES OF HEALTH

发明人： Barbara Slusher ,  Camilo Rojas ,  Ajit G. Thomas ,  Norman Haughey ,  Marc Ferrer ,  Xin Hu

IPC分类号： A61K31/4178 ,  A61P25/28

CPC分类号： A61K31/4178 ,  A61P25/28

摘要： Methods for treating one or more diseases associated with neutral sphingomyelinase 2 (nSMase2) in a subject in need of treatment thereof, the method comprising administering to the subject a therapeutically effective amount of 2,6-dimethoxy-4-(5-phenyl-4-thiophen-2-yl-1H-imidazol-2-yl)-phenol (DPTIP) or a pharmaceutically acceptable salt thereof, are disclosed.

公开(公告)号：US11253511B2

公开(公告)日：2022-02-22

申请号：US16068208

申请日：2017-01-04

申请人： THE JOHNS HOPKINS UNIVERSITY ,  THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services

发明人： Ravit Boger ,  Marc Ferrer ,  Juan Marugan ,  Andres Dulcey Garcia ,  Noel Terrence Southall ,  Xin Hu

IPC分类号： A61K31/4745 ,  A61K31/522 ,  A61P31/22 ,  A61K38/05 ,  A61P31/20 ,  A61K45/06 ,  A61K9/00

摘要： The present invention relates to the field of virology. More specifically, the present invention provides methods and compositions useful for prevention and treatment of human cytomegalovirus (CMV). In one embodiment, a pharmaceutical composition comprises (a) emetine or a derivative thereof; (b) a human cytomegalovirus (HCMV) drug; and (c) a pharmaceutically acceptable carrier. In certain embodiments, the pharmaceutical composition further comprises an adjuvant. In a specific embodiment, the HCMV drug is ganciclovir. In such embodiments, emetine is present at about 1/10 to about 1/100 the normal dosage for amebiasis.

公开(公告)号：US20210186972A1

公开(公告)日：2021-06-24

申请号：US17055256

申请日：2019-05-15

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVIC ,  University of Kansas ,  Northwestern University

发明人： Udo Rudloff ,  Serguei Kozlov ,  Juan Jose Marugan ,  Sui Huang ,  Samarjit Patnaik ,  John C. Braisted ,  Noel T. Southall ,  Marc Ferrer ,  Christopher Dextras ,  John Haslam ,  Michael Baltezor

IPC分类号： A61K31/519 ,  A61K47/12 ,  A61K45/06 ,  A61K31/7068 ,  A61P35/04

摘要： Disclosed are pharmaceutical formulations comprising a compound of formula (I): in which R1, R2, R3, and R4 are as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods for treating pancreatic adenocarcinoma comprising administration of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and methods of detecting the change in expression levels of one or both of FoxA1 and FoxO6 in a pancreatic adenocarcinoma tumor sample from a mammal, wherein the mammal has been administered a compound of formula (I), or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170114053A1

公开(公告)日：2017-04-27

申请号：US15317864

申请日：2015-06-12

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

发明人： Tsanyang Liang ,  Zongyi Hu ,  Juan Jose Marugan ,  Noel Terrence Southall ,  Shanshan He ,  Xin Hu ,  Jingbo Xiao ,  Marc Ferrer ,  Wei Zheng ,  Kevin J. Frankowski ,  Frank J. Schoenen ,  Kelin Li

IPC分类号： C07D413/06 ,  A61K31/7056 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/7068 ,  C07D417/14 ,  A61K38/21 ,  A61K38/07 ,  A61K31/4178 ,  A61K38/13 ,  C07D413/14 ,  A61K31/496

CPC分类号： C07D413/06 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  A61K31/7068 ,  A61K38/07 ,  A61K38/13 ,  A61K38/212 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  Y02A50/385

摘要： Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.

公开(公告)号：US20200369649A1

公开(公告)日：2020-11-26

申请号：US16883046

申请日：2020-05-26

申请人： The United States of America,as represented by the Secretary,Department of Health and Human Services

发明人： Melvin L. DePamphilis ,  Gaurav Sharma ,  Juan Jose Marugan ,  Marc Ferrer ,  Ajit Roy

IPC分类号： C07D403/12 ,  C07D251/54 ,  C07D239/50 ,  A61P35/00

摘要： Disclosed is method for treating cancer in a mammal, comprising administering to a mammal in need thereof a compound of the formula: wherein R1, R2, and R3 are as defined herein, wherein the cancer is an autophagy-dependent cancer, in an amount sufficient to induce autophagy in the cell and cause the death of cancer cells. Also disclosed is a method for selectively killing cancer cells in a patient afflicted with cancer, comprising administering to the mammal, wherein the cancer cells are autophagy-dependent cancer cells, in an amount sufficient to induce autophagy in the cells and cause the death of the cancer cells.

公开(公告)号：US20200165257A1

公开(公告)日：2020-05-28

申请号：US16621290

申请日：2018-06-20

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVIC

发明人： Gurmit Grewal ,  Ashish Thakur ,  Gregory James Tawa ,  Marc Ferrer ,  Anton M. Simeonov

IPC分类号： C07D487/04 ,  C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D239/88 ,  A61P35/02

摘要： The present invention is directed to a dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), including a core containing a quinazoline moiety or a quinazolin-4(3H)-one moiety, a kinase hinge binding moiety, and a histone deacetylase pharmacophore, a pharmaceutically acceptable salt thereof, a prodrug thereof, or solvate thereof. The present invention is also directed to a histone deacetylase inhibitor, including a core containing a quinazolin-4(3H)-one moiety and a histone deacetylase pharmacophore.

公开(公告)号：US09550742B2

公开(公告)日：2017-01-24

申请号：US14908271

申请日：2014-07-29

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human

发明人： Juan Jose Marugan ,  Jingbo Xiao ,  Marc Ferrer ,  Noel Terrence Southall ,  R. Benjamin Free ,  David Robert Sibley

IPC分类号： C07D281/16 ,  C07D417/12

CPC分类号： C07D281/16 ,  C07D417/12

摘要： The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.

摘要翻译： 本公开内容包括式（I）的化合物和药学上可接受的盐。 某些化合物和式（I）的盐是多巴胺D2受体的选择性抑制剂。 变量R1-R4，n和L在本文中定义。 本公开还提供了合成式（I）化合物和含有式（I）化合物的药物组合物的方法。 此外，本公开提供方法或治疗患有中枢神经系统疾病的患者，包括图雷特综合征，双相情感障碍，高催乳素血症，迟发性运动障碍，亨廷顿氏舞蹈病，精神病，抑郁症或精神分裂症。