IP Library Granted Patent US 10,239,867
Granted Patent B2
US 10,239,867 · App. 15/659,926 · Granted Mar 26, 2019

Modulators of ATP-binding cassette transporters

Inventors: Sara S. Hadida Ruah (La Jolla, CA); Peter D. J. Grootenhuis (San Diego, CA); Fredrick Van Goor (San Diego, CA); Jinglan Zhou (San Diego, CA); Brian Bear (Oceanside, CA); Mark T. Miller (San Diego, CA); Jason McCartney (Cardiff by the Sea, CA); Mehdi Michel Jamel Numa (San Diego, CA); Xiaoqing Yang (San Diego, CA)
Assignee: Vertex Pharmaceuticals Incorporated
C07D405/12C07B59/002C07D403/12C07D405/14C07D471/04C07D487/04G01N33/5008G01N33/6872C07B2200/05G01N2333/705G01N2500/02G01N2500/10
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Quick Facts
Patent No.
US 10,239,867
App. No.
15/659,926
Granted
Mar 26, 2019
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 (22)

1. A compound of formula IId:

or a pharmaceutically acceptable salt thereof; wherein

both R 2 groups, together with the atoms to which they are attached, form the group:

R′ 3 is selected from —CH 2 CH 2 and

and

each R 3 is independently selected from

H, and F.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R′ 3 is:

3. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein one occurrence of R 3 is fluoro.

4. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein one occurrence of R 3 is

5. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein one R 3 is fluoro and one R 3 is

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof; wherein

both R 2 groups, together with the atoms to which they are attached, form the group:

R′3 is

and

one R 3 is fluoro and one R 3 is

7. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof as described in claim 1 , and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

8. The pharmaceutical composition of claim 7 or a pharmaceutically acceptable salt thereof, wherein the composition further comprises one or more additional therapeutic agents.

9. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof as described in claim 6 , and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

10. The pharmaceutical composition of claim 9 or a pharmaceutically acceptable salt thereof, wherein the composition further comprises one or more additional therapeutic agents.

11. A method of treating or lessening the severity of cystic fibrosis in a patient, comprising the step of administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof according to claim 1 .

12. A method of treating or lessening the severity of cystic fibrosis in a patient, comprising the step of administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof according to claim 6 .

Assignments (3)
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 →
CHANGE OF ADDRESS Recorded Apr 13, 2018
From: VERTEX PHARMACEUTICALS INCORPORATED
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 045937/0673 →
Continuity (7)
Continuation 15162887 · May 24, 2016
Continuation 14532791 · Nov 4, 2014
Continuation 14058839 · Oct 21, 2013
Continuation 12829879 · Jul 2, 2010
Division 11786001 · Apr 9, 2007
Provisional Application 60790459 · Apr 7, 2006
Related Publication 20180162842A1 · Jun 14, 2018
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