公开(公告)号：US20170283420A1

公开(公告)日：2017-10-05

申请号：US15461327

申请日：2017-03-16

Applicant: Oncternal Therapeutics, Inc.

Inventor： Stephen E. Webber

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

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：US20230041951A1

公开(公告)日：2023-02-09

申请号：US17694183

申请日：2022-03-14

Applicant: University of Tennessee Research Foundation ,  Oncternal Therapeutics, Inc.

Inventor： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He ,  Jayaprakash Pagadala ,  Christopher C. Coss ,  James T. Dalton ,  Charles B. Duke

IPC: A61K31/404 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/47 ,  A61P35/00 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/472

Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US11285132B2

公开(公告)日：2022-03-29

申请号：US16847516

申请日：2020-04-13

Applicant: Oncternal Therapeutics, Inc.

Inventor： Brian Lannutti ,  Katayoun Jessen ,  James Bradley Breitmeyer

IPC: A61K31/40 ,  A61K31/55 ,  A61K31/501 ,  A61K38/00 ,  A61K31/404 ,  A61K39/395 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/4155 ,  A61K31/496 ,  A61K31/551 ,  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：US20200253927A1

公开(公告)日：2020-08-13

申请号：US16847516

申请日：2020-04-13

Applicant: Oncternal Therapeutics, Inc.

Inventor： Brian Lannutti ,  Katayoun Jessen ,  James Bradley Breitmeyer

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

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：US10646470B2

公开(公告)日：2020-05-12

申请号：US16114076

申请日：2018-08-27

Applicant: Oncternal Therapeutics, Inc.

Inventor： Brian Lannutti ,  Katayoun Jessen ,  James Bradley Breitmeyer

IPC: A61K31/415 ,  A61K31/445 ,  A61K31/404 ,  A61K39/395 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/4155 ,  A61K31/496 ,  A61K31/551 ,  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：US20180256546A1

公开(公告)日：2018-09-13

申请号：US15973110

申请日：2018-05-07

Applicant: Oncternal Therapeutics, Inc.

Inventor： Jean-Michel Vernier

IPC: A61K31/404 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10 ,  C07D209/34 ,  C07D209/38 ,  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：US20170349600A1

公开(公告)日：2017-12-07

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

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：US20170065559A1

公开(公告)日：2017-03-09

申请号：US15357933

申请日：2016-11-21

Applicant: Oncternal Therapeutics, Inc.

Inventor： Jean-Michel Vernier

IPC: A61K31/404 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/4155

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.

Abstract translation: 提供了作为EWS-FLI1转录因子抑制剂的吲哚啉酮衍生物化合物。 还提供了吲哚啉酮衍生物的药物组合物，其合成方法，使用其的治疗方法以及用于鉴定EWS-FLI1癌蛋白抑制剂的测定法。