公开(公告)号：US11084811B2

公开(公告)日：2021-08-10

申请号：US16281291

申请日：2019-02-21

Applicant: ONCTERNAL THERAPEUTICS, INC. ,  UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

Inventor： Wei Li ,  Min Xiao ,  James Dalton ,  Sunjoo Ahn ,  Duane D Miller ,  Jin Wang

IPC: A61K31/4178 ,  A61K31/4164 ,  C07D417/14 ,  C07D277/24 ,  C07D213/76 ,  C07D405/06 ,  C07D417/12 ,  A61P35/00 ,  C07D417/04 ,  C07D233/64 ,  C07C49/786 ,  C07D217/04 ,  C07D211/14

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

公开(公告)号：US20190337951A1

公开(公告)日：2019-11-07

申请号：US16430234

申请日：2019-06-03

Applicant: Oncternal Therapeutics, Inc.

Inventor： Stephen E. Webber

IPC: C07D487/04 ,  C07D405/06 ,  C07D209/38 ,  C07D209/40 ,  C07D401/06 ,  C07D209/34 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D403/06

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US09987251B2

公开(公告)日：2018-06-05

申请号：US15357876

申请日：2016-11-21

Applicant: Oncternal Therapeutics, Inc.

Inventor： Jean-Michel Vernier

IPC: C07D209/38 ,  C07D403/10 ,  A61K31/404 ,  C07D401/06 ,  C07D401/10 ,  C07D209/34 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/5377

CPC classification number: A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/5377 ,  C07D209/34 ,  C07D209/38 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10

Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US09822122B2

公开(公告)日：2017-11-21

申请号：US15461327

申请日：2017-03-16

Applicant: Oncternal Therapeutics, Inc.

Inventor： Stephen E. Webber

IPC: C07D487/04 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

CPC classification number: C07D487/04 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US12161626B2

公开(公告)日：2024-12-10

申请号：US17705746

申请日：2022-03-28

Applicant: Oncternal Therapeutics, Inc.

Inventor： Brian Lannutti ,  Katayoun Jessen ,  James Bradley Breitmeyer

IPC: A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K39/395 ,  A61K45/06 ,  C07K16/28

Abstract: Methods and compositions for treating acute myeloid leukemia and diffuse large B cell lymphoma using combinations of venetoclax and indolinone derivatives are provided.

公开(公告)号：US11465987B2

公开(公告)日：2022-10-11

申请号：US15270359

申请日：2016-09-20

Applicant: ONCTERNAL THERAPEUTICS, INC. ,  UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

Inventor： Wei Li ,  Min Xiao ,  James Dalton ,  Sunjoo Ahn ,  Duane D Miller ,  Jin Wang

IPC: C07D403/04 ,  C07D233/64 ,  A61K31/4164 ,  A61K45/06 ,  C07D417/04 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/56 ,  A61K31/4174 ,  A61K31/4178 ,  C07D233/88

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

公开(公告)号：US20220288023A1

公开(公告)日：2022-09-15

申请号：US17830668

申请日：2022-06-02

Applicant: Oncternal Therapeutics, Inc.

Inventor： Jean-Michel Vernier

IPC: A61K31/404 ,  C07D401/10 ,  C07D403/10 ,  C07D209/34 ,  C07D209/38 ,  C07D401/06 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/5377

Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US20210024458A1

公开(公告)日：2021-01-28

申请号：US16776395

申请日：2020-01-29

Applicant: ONCTERNAL THERAPEUTICS, INC ,  University of Tennessee Research Foundation

Inventor： Ramesh NARAYANAN ,  Duane D. MILLER ,  Thamarai PONNUSAMY ,  Dong-Jin HWANG ,  Charles B. DUKE ,  Christopher C. COSS ,  Amanda JONES ,  James T. DALTON

IPC: C07C237/20 ,  A61P35/00 ,  A61P25/00 ,  A61P5/28

Abstract: This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US10711008B2

公开(公告)日：2020-07-14

申请号：US16430234

申请日：2019-06-03

Applicant: Oncternal Therapeutics, Inc.

Inventor： Stephen E. Webber

IPC: C07D487/04 ,  C07D405/06 ,  C07D209/38 ,  C07D209/40 ,  C07D401/06 ,  C07D209/34 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D403/06

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US10351569B2

公开(公告)日：2019-07-16

申请号：US15680905

申请日：2017-08-18

Applicant: Oncternal Therapeutics, Inc.

Inventor： Stephen E. Webber

IPC: C07D487/04 ,  C07D413/06 ,  C07D409/06 ,  C07D403/06 ,  C07D209/34 ,  C07D401/06 ,  C07D209/40 ,  C07D209/38 ,  C07D417/06 ,  C07D405/06

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.