Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

US9321746B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Heather Elizabeth Burks · Cambridge, US
• Michael Dechantsreiter · Cambridge, US
• Guo He · Lexington, US
• Jill Nunez · Boston, US
• Stefan Peukert · Frankfurt am Main, DE
• Clayton Springer · Cambridge, US
• Yingchuan Sun · Cambridge, US
• Noel Marie-France Thomsen · Cambridge, US
• George Scott Tria · Cambridge, US
• Bing Yu · Stow, US

Key dates

• Filing date: Feb 12, 2014
• Grant date: Apr 26, 2016
• Expiry date: Feb 12, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.