IP Library Granted Patent US 9,856,248
Granted Patent B2
US 9,856,248 · App. 15/136,159 · Granted Jan 2, 2018

Modulators of cystic fibrosis transmembrane conductance regulator

Inventors: Sara Hadida-Ruah (La Jolla, CA); Fredrick Van Goor (San Diego, CA); Mark Miller (San Diego, CA); Jason McCartney (Cardiff by the Sea, CA); Jinglan Zhou (San Diego, CA); Vijayalaksmi Arumugam (San Marcos, CA)
Assignee: Vertex Pharmaceuticals Incorporated
C07D417/14A61K31/427
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Quick Facts
Patent No.
US 9,856,248
App. No.
15/136,159
Granted
Jan 2, 2018
Kind
B2
Abstract

The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.

Claims (13)

1. A compound having formula I′ or formula II′:

wherein:

R X

is independently hydrogen, halo, CF 3 , C 1 -C 4 alkyl, or —OC 1 -C 4 alkyl; provided that both R X are not simultaneously hydrogen: or

the two R X , taken together form ring (a):

X is CH 2 , CF 2 CH 2 —CH 2 , or CF 2 —CF 2 ;

ring A is 3-7 membered monocyclic cycloalkyl ring;

Z is an electron withdrawing substituent;

q is 0- 3;

R is hydrogen or C 1 -C 6 aliphatic;

L is a linker selected from C(O) or SO 2 ;

p is 0 or 1; and

CA is a chiral auxiliary.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 6, 2017
From: HADIDA RUAH, SARA S.; VAN GOOR, FREDRICK F.; MILLER, MARK T.; MCCARTNEY, JASON; ZHOU, JINGLAN; ARUMUGAM, VIJAYALAKSMI
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 042613/0149 →
Continuity (8)
Continuation 14598560 · Jan 16, 2015
Division 14055247 · Oct 16, 2013
Division 13178677 · Jul 8, 2011
Division 11503449 · Aug 11, 2006
Provisional Application 60732476 · Nov 2, 2005
Provisional Application 60707380 · Aug 11, 2005
Related Publication 20160237079A1 · Aug 18, 2016
Related Publication 20170174675A9 · Jun 22, 2017