IP Library Granted Patent US 10,975,061
Granted Patent B2
US 10,975,061 · App. 16/276,887 · Granted Apr 13, 2021

Modulators of ATP-binding cassette transporters

Inventors: Sara S. Hadida Ruah (La Jolla, CA); Peter D. J. Grootenhuis (Del Mar, 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
C07D405/12A61K31/445A61K31/496A61K31/5377C07B59/002C07D403/12C07D405/14C07D471/04C07D487/04G01N33/5008G01N33/6872C07B2200/05G01N2333/705G01N2500/02G01N2500/10
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Quick Facts
Patent No.
US 10,975,061
App. No.
16/276,887
Granted
Apr 13, 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 (30)

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 one of the following:

—H, —CH 3 , —CH 2 CH 3 , —C(O)CH 3 , —C(O)OCH 3 ,

and

each R 3 is independently selected from —H, —CH 3 , —CH 2 CH 3 , —CH 2 CH 2 CH 3 , —NH 2 , halo, —OCH 3 , —CN, —CF 3 , —C(O)OCH 2 CH 3 , —S(O) 2 CH 3 , —CH 2 NH 2 , —C(O)NH 2 ,

2. 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 one of the following:

—H, —CH 3 , —CH 2 CH 3 , —C(O)CH 3 , —C(O)OCH 3 ,

and

each R 3 is independently selected from —H, —CH 3 , —CH 2 CH 3 , —CH 2 CH 2 CH 3 , —NH 2 , halo, —OCH 3 , —CN, —CF 3 , —C(O)OCH 2 CH 3 , —S(O) 2 CH 3 , —CH 2 NH 2 , —C(O)NH 2 ,

3. 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 one of the following:

—H, —CH 3 , —CH 2 CH 3 , —C(O)CH 3 , —C(O)OCH 3 ,

and

each R 3 is independently selected from —H, —CH 3 , —CH 2 CH 3 , —CH 2 CH 2 CH 3 , —NH 2 , halo, —OCH 3 , —CN, —CF 3 , —C(O)OCH 2 CH 3 , —S(O) 2 CH 3 , —CH 2 NH 2 , —C(O)NH 2 ,

4. 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.

5. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof as described in claim 2 , and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

6. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof as described in claim 3 , and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

7. The pharmaceutical composition of claim 4 , wherein the pharmaceutical composition further comprises one or more additional therapeutic agents.

8. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition further comprises one or more additional therapeutic agents.

9. The pharmaceutical composition of claim 6 , wherein the pharmaceutical composition further comprises one or more additional therapeutic agents.

10. 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 .

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 2 .

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 3 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 15, 2020
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 051518/0172 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 15, 2020
From: YANG, XIAOQING
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 051518/0205 →
CHANGE OF ADDRESS Recorded Jan 15, 2020
From: VERTEX PHARMACEUTICALS INCORPORATED
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 051596/0922 →
Continuity (8)
Continuation 15659926 · Jul 26, 2017
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 20200115366A1 · Apr 16, 2020
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