公开(公告)号：US20230039309A1

公开(公告)日：2023-02-09

申请号：US17518732

申请日：2021-11-04

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 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D209/42 ,  A61K31/551 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/498 ,  C07D409/14 ,  C07D471/04 ,  C07D409/12 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

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.

公开(公告)号：US20180258039A1

公开(公告)日：2018-09-13

申请号：US15975854

申请日：2018-05-10

Applicant: Vanderbilt University

Inventor： Taekyu Lee ,  Kwangho Kim ,  Plamen P. Christov ,  Johannes Belmar ,  Jason P. Burke ,  Edward T. Olejniczak ,  Stephen W. Fesik

IPC: C07D209/26 ,  C07D209/24 ,  C07D413/04 ,  C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/4045 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/4439 ,  A61K45/06

CPC classification number: C07D209/26 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/24 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

Abstract: The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.

公开(公告)号：US10005728B2

公开(公告)日：2018-06-26

申请号：US14914307

申请日：2014-08-28

Applicant: Vanderbilt University

Inventor： Taekyu Lee ,  Kwangho Kim ,  Plamen P. Christov ,  Johannes Belmar ,  Jason P. Burke ,  Edward T. Olejniczak ,  Stephen W. Fesik

IPC: C07D209/26 ,  A61K31/4045 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D209/24 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D209/26 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/24 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

Abstract: The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.

公开(公告)号：US11596639B2

公开(公告)日：2023-03-07

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: A61P35/00 ,  A61K45/06 ,  C07D487/04 ,  A61K31/551 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D519/00

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.

公开(公告)号：US11208415B2

公开(公告)日：2021-12-28

申请号：US16688872

申请日：2019-11-19

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 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D209/42 ,  A61K31/551 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/498 ,  C07D409/14 ,  C07D471/04 ,  C07D409/12 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

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.

公开(公告)号：US20210219551A1

公开(公告)日：2021-07-22

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.

公开(公告)号：US10188105B2

公开(公告)日：2019-01-29

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 ,  A01N43/78 ,  A01N43/90 ,  A01N43/82 ,  A01N53/00 ,  A01N47/16 ,  A01N47/18 ,  C07D491/052 ,  C07D401/14 ,  C07D409/14 ,  C07D405/14 ,  C07D513/04 ,  A01N25/08 ,  C07D249/12 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056

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.

公开(公告)号：US20160151517A1

公开(公告)日：2016-06-02

申请号：US14871866

申请日：2015-09-30

Applicant: Vanderbilt University

Inventor： Ashwath Jayagopal ,  Kwangho Kim ,  Gary Sulikowski ,  Stephanie Evans

IPC: A61K49/00 ,  G01N33/569 ,  G01N33/58 ,  C07D493/10

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

Abstract translation: 用于检测缺氧细胞和组织的示例性探针具有以下结构

公开(公告)号：US12195472B2

公开(公告)日：2025-01-14

申请号：US17518732

申请日：2021-11-04

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 ,  A61K31/381 ,  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.

公开(公告)号：US12144816B2

公开(公告)日：2024-11-19

申请号：US18064206

申请日：2022-12-09

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 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04 ,  C07D519/00

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.