公开(公告)号：US20250064945A1

公开(公告)日：2025-02-27

申请号：US18709947

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Huifen Chen ,  Peter Scott Dragovich ,  Leanna Renee Staben ,  Jing Wang

IPC: A61K47/55 ,  A61K31/519 ,  A61K47/54 ,  C07D487/04 ,  C07D519/00

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20250059198A1

公开(公告)日：2025-02-20

申请号：US18710130

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Fabio Broccatelli ,  Huifen Chen ,  Peter Scott Dragovich ,  Jing Wang

IPC: C07D487/08 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20250034096A1

公开(公告)日：2025-01-30

申请号：US18772066

申请日：2024-07-12

Applicant: Arvinas Operations, Inc.

Inventor： Michael BERLIN ,  Andrew P. CREW ,  Craig M. CREWS ,  Hanqing DONG ,  Keith R. HORNBERGER ,  Lawrence B. SNYDER ,  Jing WANG ,  Kurt ZIMMERMANN

IPC: C07D233/42 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04 ,  C07D401/14

Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20250009737A1

公开(公告)日：2025-01-09

申请号：US18759774

申请日：2024-06-28

Applicant: Arvinas Operations, Inc.

Inventor： Jingang George ZHANG ,  Lawrence B. SNYDER ,  Yongqing HUANG

IPC: A61K31/496 ,  A61K45/06

Abstract: This disclosure pertains to methods of treating prostate cancer in a subject in need thereof, including, for example, metastatic prostate cancer, castrate-resistant prostate cancer, and metastatic castrate-resistant prostate cancer, wherein the method comprises administering to the subject a therapeutically effective amount of Compound A, or a pharmaceutically acceptable salt thereof, and further comprises a step of discontinuing or reducing the administration of a CYP3A inhibitor or inducer, an efflux transporter substrate or inhibitor, or an uptake transporter substrate or inhibitor, to the subject prior to initiating administration of Compound A or the pharmaceutically acceptable salt thereof.

公开(公告)号：US20240336566A1

公开(公告)日：2024-10-10

申请号：US18622152

申请日：2024-03-29

Applicant: Arvinas Operations, Inc.

Inventor： Chungpin Herman Chen ,  Maxwell Marco Reeve ,  Nitinchandra Dahyabhai Patel ,  Royal J. Haskell, III

IPC: C07D211/88

CPC classification number: C07D211/88

Abstract: The present disclosure relates to novel solid forms, including salts and solid forms thereof, of Compound A:




and to processes for their preparation. The disclosure is also directed to pharmaceutical compositions containing at least one salt or salt form and to the therapeutic and/or prophylactic use of such salts, salt forms, and compositions thereof.

公开(公告)号：US20240335444A1

公开(公告)日：2024-10-10

申请号：US18407150

申请日：2024-01-08

Applicant: Arvinas Operations, Inc.

Inventor： Dan SHERMAN ,  Sheryl Maxine GOUGH

IPC: A61K31/506 ,  A61P35/00

CPC classification number: A61K31/506 ,  A61P35/00

Abstract: This application pertains to the use of compounds, e.g., Compound A:




or a pharmaceutically acceptable salt thereof, for the treatment of various diseases or disorders, including, for example, diffuse large B-cell lymphoma (DLBCL) and angioimmunoblastic T-cell lymphoma.

公开(公告)号：US12053469B2

公开(公告)日：2024-08-06

申请号：US17207325

申请日：2021-03-19

Applicant: Arvinas Operations, Inc.

Inventor： Erika Araujo ,  Michael M. Berlin ,  Steven M. Sparks ,  Jing Wang ,  Wei Zhang

IPC: A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61P25/16 ,  C07D401/14 ,  C07D413/14 ,  C07D487/10

CPC classification number: A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61P25/16 ,  C07D401/14 ,  C07D413/14 ,  C07D487/10

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240180900A1

公开(公告)日：2024-06-06

申请号：US18493773

申请日：2023-10-24

Applicant: Arvinas Operations, Inc.

Inventor： Ronald PECK ,  Sarah Deborah CHIRNOMAS ,  Edward CHAN ,  Richard Walter GEDRICH ,  Elmer J. BERGHORN, Jr. ,  Jeanette Toni ALICEA ,  Lawrence B. SNYDER ,  SangHyun LEE ,  Taavi NEKLESA

IPC: A61K31/496 ,  A61K31/573 ,  A61K31/58 ,  A61P35/00

CPC classification number: A61K31/496 ,  A61K31/573 ,  A61K31/58 ,  A61P35/00

Abstract: This disclosure pertains to methods of treating prostate cancer in a subject, including prostate cancer comprising at least one somatic AR tumor mutation, such as metastatic prostate cancer, castrate-resistant prostate cancer, metastatic castrate-resistant prostate cancer, progressive metastatic castrate-resistant prostate cancer, castrate-sensitive prostate cancer, metastatic castrate-sensitive prostate cancer, prostate cancer naïve to novel hormonal agents (NHAs), metastatic prostate cancer naïve NHAs, castrate-resistant prostate cancer naïve to NHAs, castrate-sensitive prostate cancer naïve to NHAs, metastatic castrate-resistant prostate cancer naïve to NHAs, and metastatic castrate-sensitive prostate cancer naïve to NHAs, wherein the method comprises administering to a subject in need thereof a therapeutically effective amount of Compound A, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11981683B2

公开(公告)日：2024-05-14

申请号：US17699082

申请日：2022-03-19

Applicant: Arvinas Operations, Inc.

Inventor： Erika Marina Vieira Araujo ,  Michael Berlin ,  Hanqing Dong ,  Steven M. Sparks ,  Jing Wang ,  Wei Zhang

IPC: C07D401/14 ,  A61K45/06 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/10

CPC classification number: C07D498/10 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240131023A1

公开(公告)日：2024-04-25

申请号：US18460063

申请日：2023-09-01

Applicant: Arvinas Operations, Inc.

Inventor： LAWRENCE B. Snyder ,  Andrew P. Crew ,  Jing Wang ,  Hanqing Dong

IPC: A61K31/496 ,  A61K31/167 ,  A61K31/277 ,  A61K31/337 ,  A61K31/417 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/57 ,  A61K31/661 ,  A61K31/663 ,  A61K31/675 ,  A61K38/09 ,  A61K47/54 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/10

CPC classification number: A61K31/496 ,  A61K31/167 ,  A61K31/277 ,  A61K31/337 ,  A61K31/417 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/57 ,  A61K31/661 ,  A61K31/663 ,  A61K31/675 ,  A61K38/09 ,  A61K47/545 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/10

Abstract: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.