公开(公告)号：US20230128132A1

公开(公告)日：2023-04-27

申请号：US18085869

申请日：2022-12-21

申请人： Arvinas Operations, Inc.

发明人： Andrew P. CREW ,  Lawrence B. SNYDER ,  Jing WANG ,  Royal J. HASKELL, III ,  Marcia Dougan MOORE

IPC分类号： A61K31/501 ,  A61P35/00 ,  A61K9/00

摘要： The present application relates to treating and/or preventing prostate cancer, including metastatic and/or castrate-resistant prostate 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, X1, X2, X3, X4, and n are defined herein.

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：US20230012321A1

公开(公告)日：2023-01-12

申请号：US17313679

申请日：2021-05-06

申请人： Arvinas Operations, Inc.

发明人： Laura E.N. ALLAN ,  Chungpin Herman CHEN ,  Hanqing DONG ,  Robert J. DUGUID ,  John A. GROSSO ,  Royal J. HASKELL, III ,  Casey Keith JAGER ,  Venkata A. KATTUBOINA ,  Aditya Mohan KAUSHAL ,  Samuel Elliott KENNEDY ,  Rhys LLOYD ,  Miranda Annell NEESER ,  Yuping QIU ,  Hayley REECE ,  Maxwell Marco REEVE ,  Joseph P. REO ,  Jerod ROBERTSON ,  Mohammad Mehdi ZAHEDI

IPC分类号： C07D401/14 ,  A61K9/00 ,  A61K9/20 ,  A61K45/06

摘要： The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A: The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

公开(公告)号：US20210113557A1

公开(公告)日：2021-04-22

申请号：US17075808

申请日：2020-10-21

申请人： Arvinas Operations, Inc.

发明人： Andrew P. CREW ,  Lawrence B. SNYDER ,  Jing WANG ,  Royal J. HASKELL, III ,  Marcia Dougan MOORE

IPC分类号： A61K31/501 ,  A61P35/00 ,  A61K9/00

摘要： The present application relates to treating and/or preventing prostate cancer, including metastatic and/or castrate-resistant prostate 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, X1, X2, X3, X4 and n are defined herein.

公开(公告)号：US20220081416A1

公开(公告)日：2022-03-17

申请号：US17472847

申请日：2021-09-13

申请人： Arvinas Operations, Inc.

发明人： Katharine Victoria BOULTON ,  Chungpin Herman CHEN ,  Royal J. HASKELL, III ,  Hayley REECE

IPC分类号： C07D401/14

摘要： The present disclosure relates to polymorphic forms of (S)-3-(5-(4-((1-(4-((1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, methods of making these polymorphic forms, and compositions comprising these polymorphic forms. These polymorphic forms are useful in the treatment of various diseases, including, for example, breast cancer.

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.