公开(公告)号：US12043612B2

公开(公告)日：2024-07-23

申请号：US17313679

申请日：2021-05-06

Applicant: Arvinas Operations, Inc.

Inventor： Laura E. N. Allan ,  Chungpin Herman Chen ,  Hanqing Dong ,  John A. Grosso ,  Royal J. Haskell, III ,  Rhys LLoyd ,  Hayley Reece

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

CPC classification number: C07D401/14 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054 ,  A61K45/06 ,  C07B2200/13

Abstract: 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：US12162859B2

公开(公告)日：2024-12-10

申请号：US17472847

申请日：2021-09-13

Applicant: Arvinas Operations, Inc.

Inventor： Katharine Victoria Boulton ,  Chungpin Herman Chen ,  Royal J. Haskell, III ,  Hayley Reece

IPC: C07D401/14

Abstract: 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.