IP Library Granted Patent US 10,941,159
Granted Patent B2
US 10,941,159 · App. 16/460,781 · Granted Mar 9, 2021

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

Inventors: Graham Beaton (Poway, CA); Mi Chen (San Diego, CA); Timothy Richard Coon (Carlsbad, CA); Todd Ewing (San Diego, CA); Wanlong Jiang (San Diego, CA); Willy Moree (San Diego, CA); Martin Rowbottom (San Diego, CA); Warren Wade (San Diego, CA); Liren Zhao (San Diego, CA); Richard Lowe (Oakland, CA); Nicole Smith (San Diego, CA); Neil Ashweek (San Diego, CA); Yun-Fei Zhu (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
C07D495/04C07C233/88C07C235/42C07C255/57C07D213/56C07D213/58C07D213/61C07D213/64C07D213/70C07D213/81C07D213/84C07D213/89C07D215/14C07D215/54C07D239/36C07D401/04C07D401/12C07D413/12C07D417/12
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Quick Facts
Patent No.
US 10,941,159
App. No.
16/460,781
Granted
Mar 9, 2021
Kind
B2
Abstract

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R 1a , R 1b , R 1c , R 1d , R 2 , R 2a , and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Claims (4)

1. The compound that is 3-(2-{[4-chloro-3-(4-cyano-6-trifluoromethyl-pyridin-3-yl)-benzoyl]-methyl-amino}-phenoxy)-propionic acid, or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

3. The compound that is 4-(2-{[4-chloro-3-(4-cyano-6-trifluoromethyl-pyridin-3-yl)-benzoyl]-methyl-amino}-3-methyl-phenoxy)-butyric acid, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising the compound of claim 3 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

Assignments (2)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2021
From: BEATON, GRAHAM; CHEN, MI; COON, TIMOTHY RICHARD; EWING, TODD; JIANG, WANLONG; LOWE, RICHARD; MOREE, WILLY; SMITH, NICOLE; WADE, WARREN; ZHAO, LIREN; ZHU, YUN-FEI; ROWBOTTOM, MARTIN; ASHWEEK, NEIL
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 057109/0098 →
Continuity (8)
Continuation 15445673 · Feb 28, 2017
Continuation 15210470 · Jul 14, 2016
Continuation 14592690 · Jan 8, 2015
Continuation 13910961 · Jun 5, 2013
Continuation 13293943 · Nov 10, 2011
Division 12594809
Provisional Application 60910621 · Apr 6, 2007
Related Publication 20200095259A1 · Mar 26, 2020