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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9321746 B1

PDFFull Text
Date of Patent:
Apr. 26, 2016

Filed:

Feb. 12, 2014

Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

Applicant:

Novartis Ag, Basel, CH;

Inventors:

Heather Elizabeth Burks, Cambridge, MA (US);

Michael A. Dechantsreiter, Cambridge, MA (US);

Guo He, Cambridge, MA (US);

Jill Nunez, Cambridge, MA (US);

Stefan Peukert, Cambridge, MA (US);

Clayton Springer, Cambridge, MA (US);

Yingchuan Sun, Cambridge, MA (US);

Noel Marie-France Thomsen, Cambridge, MA (US);

George Scott Tria, Cambridge, MA (US);

Bing Yu, Cambridge, MA (US);

Assignee:

NOVARTIS AG, Basel, CH;

Attorney:

Scott W. Reid

Primary Examiner:

Craig Ricci

Int. Cl.
CPC ...
A61K 31/00 (2006.01); C07D 333/64 (2006.01); A61K 31/381 (2006.01); A61K 31/4196 (2006.01); A61K 31/422 (2006.01); A61K 31/4245 (2006.01); A61K 31/4436 (2006.01); A61K 31/506 (2006.01); A61K 45/06 (2006.01); C07D 333/66 (2006.01); C07D 409/12 (2006.01); C07D 413/04 (2006.01); C07D 413/12 (2006.01); C07D 409/04 (2006.01); C07D 409/10 (2006.01); C07D 417/12 (2006.01); A61K 31/397 (2006.01); A61K 31/4025 (2006.01); A61K 31/404 (2006.01); A61K 31/41 (2006.01); A61K 31/428 (2006.01); A61K 31/5377 (2006.01);
U.S. Cl.
CPC ...
C07D 333/64 (2013.01); A61K 31/381 (2013.01); A61K 31/397 (2013.01); A61K 31/404 (2013.01); A61K 31/4025 (2013.01); A61K 31/41 (2013.01); A61K 31/4196 (2013.01); A61K 31/422 (2013.01); A61K 31/428 (2013.01); A61K 31/4245 (2013.01); A61K 31/4436 (2013.01); A61K 31/506 (2013.01); A61K 31/5377 (2013.01); A61K 45/06 (2013.01); C07D 333/66 (2013.01); C07D 409/04 (2013.01); C07D 409/10 (2013.01); C07D 409/12 (2013.01); C07D 413/04 (2013.01); C07D 413/12 (2013.01); C07D 417/12 (2013.01);
Abstract

The present invention relates to compounds of formula I: in which n, m, X, Y, R, R, R, Rand Rare 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.

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