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公开(公告)号:US20180273488A1
公开(公告)日:2018-09-27
申请号:US15540893
申请日:2015-12-29
Applicant: VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania , THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HE
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , A61K45/06 , C07D417/04 , A61K31/427 , C07D471/04 , A61K31/437 , A61K31/5355 , C07D417/14 , C07D495/04 , A61K31/519 , C07D403/04 , A61K31/4178 , C07D409/04 , A61K31/4155 , A61K31/4439 , A61K31/415 , A61K31/496 , C07D495/14 , A61K31/501 , C07D231/38 , C07D403/06 , C07D401/04 , C07D413/04 , A61K31/422 , A61K31/506 , A61K31/454
CPC classification number: C07D231/20 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14
Abstract: Provided is a compound of formula (I) [Formula (I) should be inserted here], in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US20230052528A1
公开(公告)日:2023-02-16
申请号:US17777971
申请日:2020-11-20
Applicant: The Regents of the University of California , WASHINGTON UNIVERSITY IN ST. LOUIS , VANDERBILT UNIVERSITY , SRI INTERNATIONAL , The United States of America, as represented by the Secretary, Department of Health and Human Servic
Inventor: Michelle R. Arkin , R. Jeffrey Neitz , Adam R. Renslo , James Hsieh , Shubhankar Dutta , Clifford Bryant , William J. Moore , Alex G. Waterson , Lidia Sambucetti , Somnath Jana , lan M. Romaine , Alexander P. Lamers , Yassir Younis Adam , Claire Repellin
IPC: C07D241/04 , A61P35/00 , A61P11/00 , C07C311/11 , C07D295/26 , C07D403/12 , C07C323/41 , C12N9/64
Abstract: Disclosed herein, inter alia, are compounds and methods for inhibiting Taspase1 and the treatment of cancer.
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3.
公开(公告)号:US10954228B2
公开(公告)日:2021-03-23
申请号:US16313727
申请日:2017-06-29
Applicant: NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPARTMENT OF HEALTH AND HUMAN SERVICES , Vanderbilt University , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesha Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor M. Darley-Usmar , Matthew Hall , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D417/04 , C07D417/14 , A61P11/00 , A61P35/00
Abstract: The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.
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公开(公告)号:US10351532B2
公开(公告)日:2019-07-16
申请号:US15540893
申请日:2015-12-29
Applicant: THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HE , VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K31/415 , A61K45/06
Abstract: Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US11897845B2
公开(公告)日:2024-02-13
申请号:US17572359
申请日:2022-01-10
Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14 , A61K31/415 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , A61K31/4178
CPC classification number: C07D231/20 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14
Abstract: Provided is a compound of formula (I)
in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.-
公开(公告)号:US20220144794A1
公开(公告)日:2022-05-12
申请号:US17602133
申请日:2020-04-09
Applicant: Vanderbilt University
Inventor: Gary A. Sulikowski , Christopher Fullenkamp , Kwangho Kim , Somnath Jana
IPC: C07D321/00 , A61P31/04
Abstract: Provided are 9-dechlorochrysophaentin analog compounds and the synthesis process thereof. The disclosed compound have remarkable antimicrobial activities that are comparable to, or even more potent than, the natural product chrysophaentin A. Also provided are method of inhibiting bacterial growth or treating bacterial infection by administering an effective amount of the disclosed compounds.
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公开(公告)号:US11247971B2
公开(公告)日:2022-02-15
申请号:US17160868
申请日:2021-01-28
Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K31/4439 , A61K45/06
Abstract: Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US10961200B2
公开(公告)日:2021-03-30
申请号:US16455848
申请日:2019-06-28
Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH , VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14
Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US20200002285A1
公开(公告)日:2020-01-02
申请号:US16455848
申请日:2019-06-28
Applicant: The United States of America, as represented by the Secretary, Department of Health , Vanderbilt University , The UAB Research Foundation , The Trustees of the University of Pennsylvania
Inventor: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC: C07D231/20 , C07D403/04 , C07D417/04 , C07D417/14 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , C07D231/38 , C07D401/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D471/04 , C07D495/04 , C07D495/14
Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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