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公开(公告)号：US20190075798A1
公开(公告)日：2019-03-14
申请号：US16186106
申请日：2018-11-09
Applicant: Vanderbilt University
Inventor： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC: A01N43/653 , C07D491/048 , C07D491/056 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04 , C07D491/052 , A01N43/82 , A01N43/90 , A01N43/78 , A01N25/34 , A01N27/00 , A01N29/02 , A01N33/18 , A01N33/22 , A01N47/08 , A01N47/14 , A01N57/12 , A01N57/14 , A01N57/16
Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitoes. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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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：US20170174689A1
公开(公告)日：2017-06-22
申请号：US15129042
申请日：2015-03-26
Applicant: Vanderbilt University
Inventor： Taekyu Lee , Zhiguo Bian , Johannes Belmar , Plamen P. Christov , Nicholas F. Pelz , Subrata Shaw , Kwangho Kim , James C. Tarr , Edward T. Olejniczak , Bin Zhao , Stephen W. Fesik
IPC: C07D487/04 , A61K31/404 , A61K45/06 , C07D401/12 , A61K31/4439 , C07D403/04 , A61K31/4155 , A61K31/4985 , A61K31/551 , C07D403/14 , C07D401/04 , C07D403/12 , A61K31/496 , A61K31/5377 , A61K31/454 , C07D405/12 , C07D405/14 , C07D401/14 , A61K31/4725 , C07D209/42
CPC classification number: C07D487/04 , A61K31/381 , A61K31/404 , A61K31/4045 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D209/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D471/04
Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
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公开(公告)号：US20230136150A1
公开(公告)日：2023-05-04
申请号：US17954279
申请日：2022-09-27
Applicant: Vanderbilt University
Inventor： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC: A01N43/653 , A01N43/82 , A01N43/78 , A01N43/90 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D513/04
Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US11484032B2
公开(公告)日：2022-11-01
申请号：US16945369
申请日：2020-07-31
Applicant: Vanderbilt University
Inventor： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC: A01N43/653 , A01N43/82 , A01N43/78 , A01N43/90 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D513/04
Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Patent Agency Ranking
公开(公告)号：US20210283138A1
公开(公告)日：2021-09-16
申请号：US16081709
申请日：2017-03-03
Applicant: Vanderbilt University
Inventor： Taekyu Lee , James C. Tarr , KyuOk Jeon , James M. Salovich , Subrata Shaw , Nagarathanam Veerasamy , Kwangho Kim , Plamen P. Christov , Edward T. Olejniczak , Bin Zhao , Stephen W. Fesik , Zhiguo Bian
IPC: A61K31/551 , A61K45/06 , C07D487/04 , A61K31/4985 , A61K31/5377 , A61K31/538 , A61K31/506 , C07D519/00 , C07D403/04 , C07D403/14 , C07D401/14 , A61P35/00
Abstract: The present disclosure provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
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27.发明授权公开(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：US10076578B2
公开(公告)日：2018-09-18
申请号：US14871866
申请日：2015-09-30
Applicant: Vanderbilt University
Inventor： Ashwath Jayagopal , Kwangho Kim , Gary Sulikowski , Stephanie Evans
IPC: A61B5/00 , A61B8/00 , A61B10/00 , A61K49/00 , C07D493/10 , G01N33/58 , G01N33/533
CPC classification number: A61K49/0052 , A61K49/0041 , A61K49/0043 , C07D493/10 , G01N33/533 , G01N33/582 , G01N2800/52 , G01N2800/7038
Abstract: Exemplary probes for detecting hypoxic cells and tissue have the structure of
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公开(公告)号：US20170208809A1
公开(公告)日：2017-07-27
申请号：US15443340
申请日：2017-02-27
Applicant: Vanderbilt University
Inventor： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC: A01N43/653 , C07D401/04 , A01N53/00 , C07D471/04 , A01N43/90 , C07D405/14 , C07D401/14 , C07D491/056 , C07D491/052 , A01N47/18 , C07D491/048 , C07D409/04 , A01N47/16 , C07D409/14 , C07D405/04 , C07D249/12 , C07D405/06 , C07D403/04 , C07D413/14 , C07D513/04 , A01N25/08
CPC classification number: A01N43/653 , A01N25/08 , A01N43/78 , A01N43/82 , A01N43/90 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D513/04 , A01N25/34 , A01N27/00 , A01N29/02 , A01N33/18 , A01N33/22 , A01N47/08 , A01N47/14 , A01N57/12 , A01N57/14 , A01N57/16
Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitoes. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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