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Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
US2016184265A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2016184265-A1 |
| Application number | US-201615066425-A |
| Country | US |
| Kind code | A1 |
| Filing date | Mar 10, 2016 |
| Priority date | Feb 19, 2013 |
| Publication date | Jun 30, 2016 |
| Grant date | — |
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- Title
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Abstract
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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
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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.
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Classifications
Antineoplastic agents · CPC title
condensed with carbocyclic rings · CPC title
not condensed and containing further heterocyclic rings, e.g. timolol · CPC title
directly linked by a ring-member-to-ring-member bond · CPC title
Oxadiazoles · CPC title
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- What does patent US2016184265A1 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 process for the preparation of compo…
- 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 Thu Jun 30 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (A1). 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).