公开(公告)号：US20220193072A1

公开(公告)日：2022-06-23

申请号：US17548842

申请日：2021-12-13

申请人： Arvinas Operations, Inc.

发明人： Xin CHEN ,  Andrew P. CREW ,  John FLANAGAN ,  Sheryl Maxine GOUGH ,  Royal J. HASKELL, III ,  Marcia Dougan MOORE ,  Yimin QIAN ,  Ian Charles Anthony TAYLOR ,  Jing WANG

IPC分类号： A61K31/497 ,  A61P35/04 ,  A61K31/519

摘要： The present application relates to treating and/or preventing breast cancer, including locally advanced or metastatic, ER+, HER2− breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, R4, m, and n are defined herein.

公开(公告)号：US20240059686A1

公开(公告)日：2024-02-22

申请号：US18085500

申请日：2022-12-20

申请人： Arvinas Operations, Inc.

发明人： Andrew P. CREW ,  Hanqing DONG ,  Jing WANG ,  Xin CHEN ,  Yimin QIAN ,  Craig M. CREWS ,  Michael BERLIN ,  Meizhong JIN

IPC分类号： C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  C07D401/04 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/078 ,  A61P35/00 ,  A61P25/28

CPC分类号： C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  A61P25/28 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/06165 ,  A61P35/00 ,  C07D401/04

摘要： The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the 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 invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20210060008A1

公开(公告)日：2021-03-04

申请号：US17001519

申请日：2020-08-24

申请人： Arvinas Operations, Inc.

发明人： Xin CHEN ,  Andrew P. CREW ,  John FLANAGAN ,  Sheryl Maxine GOUGH ,  Royal J. HASKELL, III ,  Marcia Dougan MOORE ,  Yimin QIAN ,  Ian Charles Anthony TAYLOR ,  Jing WANG

IPC分类号： A61K31/496 ,  A61K47/38 ,  A61K47/26 ,  A61K47/02 ,  A61K47/22 ,  A61K31/519 ,  A61P35/00

摘要： The present application relates to treating and/or preventing breast cancer, including locally advanced or metastatic, ER+, HER2− breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, R4, m, and n are defined herein.