IP Library Granted Patent US 10,494,347
Granted Patent B2
US 10,494,347 · App. 15/833,513 · Granted Dec 3, 2019

Processes for the preparation of uracil derivatives

Inventors: Donald J. Gallagher (Hopkinton, MA); Laszlo R. Treiber (San Diego, CA); Robert Michael Hughes (San Diego, CA); Onorato Campopiano (Hayward, CA); Peng Wang (Carlsbad, CA); Yuxin Zhao (San Diego, CA); Shine K. Chou (Wildwood, MO); Michael Allen Ouellette (San Diego, CA); Donald Nicholas Hettinger (Broomfield, CO)
Assignee: Neurocrine Biosciences, Inc.
C07D239/54A61P15/00C07D239/553A61K9/146A61K9/1688
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Quick Facts
Patent No.
US 10,494,347
App. No.
15/833,513
Granted
Dec 3, 2019
Kind
B2
Abstract

The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.

Claims (14)

1. A compound of structure (VII)

wherein:

R 2a and R 2b are the same or different and independently halogen, trifluoromethyl, cyano or —SO 2 CH 3 ; and

R 3 is hydrogen or methyl.

2. The compound of claim 1 wherein R 2a is F and R 2b is —CF 3 .

3. The compound of claim 2 wherein R 3 is hydrogen.

4. A compound of structure (VII)

wherein:

R 2a and R 2b are different and independently hydrogen, halogen, trifluoromethyl, cyano or —SO 2 CH 3 ; and

R 3 is hydrogen or methyl.

5. The compound of claim 4 wherein R 2a is F.

6. The compound of claim 5 wherein R 3 is methyl.

7. The compound of claim 4 wherein R 2b is −CF 3.

8. The compound of claim 7 wherein R 3 is methyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 6, 2019
From: GALLAGHER, DONALD J.; TREIBER, LASZLO R.; HUGHES, ROBERT MICHAEL; CAMPOPIANO, ONORATO; WANG, PENG; ZHAO, YUXIN; CHOU, HELEN; OUELLETTE, MICHAEL ALLEN; HETTINGER, DONALD NICHOLAS
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 048254/0383 →
Continuity (6)
Continuation 15406476 · Jan 13, 2017
Continuation 15174774 · Jun 6, 2016
Continuation 14309732 · Jun 19, 2014
Division 12741819
Provisional Application 60986227 · Nov 7, 2007
Related Publication 20180346428A1 · Dec 6, 2018