IP Library › Granted Patent US 10,987,348
Granted Patent B2
US 10,987,348 · App. 15/949,404 · Granted Apr 27, 2021

Modulators of ATP-binding cassette transporters

Inventors: Sara Sabina Hadida Ruah (La Jolla, CA); Peter Diederik Jan Grootenhuis (San Diego, CA); Fredrick F. Van Goor (San Diego, CA); Jinglan Zhou (San Diego, CA); Brian Richard Bear (Carlsbad, CA); Mark Thomas Miller (San Diego, CA); Jason McCartney (Cardiff by the Sea, CA); Mehdi Michel Djamel Numa (San Diego, CA)
Assignee: Vertex Pharmaceuticals Incorporated
A61K31/47A61K31/404A61K31/405A61K31/407A61K31/4045A61K31/41A61K31/4184A61K31/4192A61K31/454A61K31/5377A61K45/06C07D209/08C07D233/64C07D403/12C07D405/12C07D405/14C07D471/04C07D487/04G01N33/5035G01N2333/705G01N2500/10
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Quick Facts
Patent No.
US 10,987,348
App. No.
15/949,404
Granted
Apr 27, 2021
Kind
B2
Abstract

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Claims (15)

1. A process of preparing a compound of the formula:

comprising the steps of:

a) reacting a compound of the formula:

with cesium carbonate and a compound of the formula:

to form a mixture of compounds of the formulae:

b) reducing the mixture of compounds of the formulae:

with lithium aluminum hydride to form a compound of the formula:

and

c) reducing the compound of the formula:

with palladium on carbon and H 2 to form a compound of the formula:

2. A compound selected from:

3. The compound of claim 2 , wherein the compound is of the formula:

4. The compound of claim 2 , wherein the compound is of the formula:

5. The compound of claim 2 , wherein the compound is of the formula:

6. The compound of claim 2 , wherein the compound is of the formula:

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2018
From: HADIDA RUAH, SARA S.; GROOTENHUIS, PETER D.J.; VAN GOOR, FREDERICK; ZHOU, JINGLAN; BEAR, BRIAN; MILLER, MARK T.; MCCARTNEY, JASON; NUMA, MEHDI MICHEL JAMEL
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045532/0406 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2018
From: YANG, XIAOQING
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045532/0415 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2018
From: HADIDA RUAH, SARA S.; GROOTENHUIS, PETER D.J.; VAN GOOR, FREDRICK F.; ZHOU, JINGLAN; BEAR, BRIAN; MILLER, MARK T.; MCCARTNEY, JASON; NUMA, MEHDI MICHEL DJAMEL
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045532/0521 →
CHANGE OF ADDRESS Recorded Apr 13, 2018
From: VERTEX PHARMACEUTICALS INCORPORATED
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045937/0673 →
Continuity (9)
Continuation 15234877 · Aug 11, 2016
Continuation 14579098 · Dec 22, 2014
Continuation 14036286 · Sep 25, 2013
Division 12948162 · Nov 17, 2010
Continuation 12619412 · Nov 16, 2009
Division 11975297 · Oct 18, 2007
Continuation In Part 11786001 · Apr 9, 2007
Provisional Application 60790459 · Apr 7, 2006
Related Publication 20190076419A1 · Mar 14, 2019
Cited By (6)
US 50,453 US 12,214,083 US 12,269,831 US 12,324,802 US 12,458,635 US 12,508,231