Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

US9561211B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9561211-B2
Application numberUS-201615066425-A
CountryUS
Kind codeB2
Filing dateMar 10, 2016
Priority dateFeb 19, 2013
Publication dateFeb 7, 2017
Grant dateFeb 7, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

The present invention relates to compounds of formula I: in which n, m, X, Y 1 , R 1 , R 2 , R 3 , R 4 and R 5 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.

First claim

Opening claim text (preview).

We claim: 1. A method of treating a cancer selected from breast, ovarian, endometrial, prostate, uterine, cervical and lung, comprising administering to a subject in need of such treatment an effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the structure: 2. The method of claim 1 , further comprising administering to the subject an additional therapeutic agent. 3. The method of claim 2 , wherein the additional therapeutic agent comprises an anticancer drug, a pain medication, an antiemetic, an antidepressant or an anti-inflammatory agent.

Assignees

Inventors

Classifications

  • directly linked by a ring-member-to-ring-member bond · CPC title

  • not condensed and containing further heterocyclic rings · CPC title

  • Nitrogen atoms not forming part of a nitro radical · CPC title

  • linked by a carbon chain containing aromatic rings · CPC title

  • linked by a chain containing hetero atoms as chain links · CPC title

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Frequently asked questions

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What does patent US9561211B2 cover?
The present invention relates to compounds of formula I: in which n, m, X, Y 1 , R 1 , R 2 , R 3 , R 4 and R 5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a pr…
Who is the assignee on this patent?
Burks Heather Elizabeth, Dechantsreiter Michael A, He Guo, and 8 more
What technology area does this patent fall under?
Primary CPC classification A61K31/381. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Feb 07 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).