公开(公告)号：US20240316056A1

公开(公告)日：2024-09-26

申请号：US18735506

申请日：2024-06-06

申请人： The United States of America,as represented by the Secretary,Department of Health and Human Services ,  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 ,  A61K31/7068 ,  A61K45/06 ,  A61K47/12 ,  A61P35/04

CPC分类号： A61K31/519 ,  A61K31/7068 ,  A61K45/06 ,  A61K47/12 ,  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：US10301314B2

公开(公告)日：2019-05-28

申请号：US15606740

申请日：2017-05-26

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

发明人： Kevin Frankowski ,  Samarjit Patnaik ,  Sui Huang ,  Juan Jose Marugan ,  John Norton ,  Frank J. Schoenen ,  Noel Terrence Southall ,  Steven Titus ,  Wei Zheng ,  Chen Wang

IPC分类号： A61K31/519 ,  A61P35/04 ,  C07D487/04 ,  C07F7/18 ,  A61K31/695 ,  A61K45/06

摘要： The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.

公开(公告)号：US11241436B2

公开(公告)日：2022-02-08

申请号：US16480885

申请日：2018-01-25

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

发明人： Congcong He ,  Sui Huang ,  Chen Wang ,  Altea Rocchi ,  Juan Jose Marugan ,  Marc Ferrer ,  Samarjit Patnaik ,  Yuchi Chen ,  Kevin Frankowski ,  Frank J. Schoenen

IPC分类号： A61K31/519 ,  A61P25/30 ,  A61K31/704

摘要： The invention provides a compound of formula (I): wherein R1, R2, R3, and R4 are as defined herein, ginsenoside Rg2 of structure (II): or a combination thereof, for use in treating or preventing a condition responsive to the induction of autophagy in a brain of a mammal in need thereof.

公开(公告)号：US09464035B2

公开(公告)日：2016-10-11

申请号：US14388494

申请日：2013-03-15

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

发明人： Juan Jose Marugan ,  Wei Zheng ,  Samarjit Patnaik ,  Noel Southall ,  Ellen Sidransky ,  Ehud Goldin ,  Wendy Westbroek ,  Elma Aflaki ,  Steven Andrew Rogers ,  Frank John Schoenen

IPC分类号： C07C235/64 ,  C07C235/60 ,  C07C237/22

CPC分类号： C07C235/64 ,  C07B2200/07 ,  C07C235/60 ,  C07C237/22

摘要： Compounds of Formula (I) and the pharmaceutically acceptable salts thereof are disclosed. The variables. R1-R13, m, n, o, and p are disclosed herein. The compounds are useful for treating Gaucher disease and inhibiting the onset of Gaucher disease symptoms in a patient having a GBA gene mutation and for treating Parkinson's disease. Pharmaceutical compositions containing compounds of Formula (I) and methods of treatment comprising administering compounds of Formula (I) are also disclosed.

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：US09663521B2

公开(公告)日：2017-05-30

申请号：US14364759

申请日：2012-12-17

申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  UNIVERSITY OF KANSAS ,  NORTH-WESTERN UNIVERSITY

发明人： Kevin Frankowski ,  Samarjit Patnaik ,  Sui Huang ,  Juan Jose Marugan ,  John Norton ,  Frank J. Schoenen ,  Noel Terrence Southall ,  Steven Titus ,  Wei Zheng

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/695 ,  A61K45/06 ,  C07F7/18 ,  A61P35/02 ,  A61P35/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/695 ,  A61K45/06 ,  C07F7/1804

摘要： The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.

公开(公告)号：US11471460B2

公开(公告)日：2022-10-18

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： A61K31/53 ,  A61P35/00 ,  A61K31/506 ,  C07D239/50 ,  C07D251/54 ,  C07D403/12

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：US10239830B2

公开(公告)日：2019-03-26

申请号：US15549743

申请日：2016-02-11

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI ,  The United States of America, as represented by the Secretary, Department of Health and Human Services

发明人： Samarjit Patnaik ,  Mercedes Taylor ,  Raul Rolando Calvo ,  Juan Jose Marugan ,  Noel Southall ,  Wei Zheng ,  Marc Ferrer-Alegre ,  Seameen Dehdasthi ,  Patricia Dranchak ,  Fannie Chen ,  Yiannis Ioannou

IPC分类号： C07C311/21 ,  A61K31/4164 ,  A61K31/44 ,  C07D207/335 ,  C07D213/46 ,  C07D233/64 ,  A61K31/165

摘要： Methods and compositions for treating lysosomal storage disorders are disclosed. The methods involve administering a genus of benzenesulfonamides, particularly N-[3-(aminosulfonyl)phenyl]-benzamides and heteroarylamides. A genus of suitable compounds is shown in formula 1:

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：US09422308B2

公开(公告)日：2016-08-23

申请号：US14387410

申请日：2013-03-15

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

发明人： Hee-Yong Kim ,  Juan Jose Marugan ,  Erika E. Englund ,  Samarjit Patnaik

IPC分类号： C07D495/04 ,  C07D213/40 ,  C07D319/20 ,  C07D205/04 ,  C07C235/28 ,  C07D309/04 ,  C07D333/20 ,  C07D235/14 ,  C07C233/09 ,  C07C233/13 ,  C07C233/20 ,  C07C233/23 ,  C07C233/31 ,  C07C233/38 ,  C07C233/49 ,  C07C255/29 ,  C07D295/13 ,  C07D295/135 ,  C07D295/185 ,  C07D307/52

CPC分类号： C07D495/04 ,  C07C233/09 ,  C07C233/13 ,  C07C233/20 ,  C07C233/23 ,  C07C233/31 ,  C07C233/38 ,  C07C233/49 ,  C07C235/28 ,  C07C255/29 ,  C07C2601/04 ,  C07C2601/14 ,  C07D205/04 ,  C07D213/40 ,  C07D235/14 ,  C07D295/13 ,  C07D295/135 ,  C07D295/185 ,  C07D307/52 ,  C07D309/04 ,  C07D319/20 ,  C07D333/20

摘要： The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis.

摘要翻译： 本发明提供了与DEA相比具有增强的耐药性和耐水解性的DEA衍生物及其组合物，以及使用这些衍生物促进神经发生，神经突生长和/或长度和/或促进突触发生的方法。