IP Library Granted Patent US 9,328,113
Granted Patent B2
US 9,328,113 · App. 14/391,443 · Granted May 3, 2016

Substituted xanthine derivatives

Inventors: Roger D. Tung (Lexington, MA); Bhaumik Pandya (Arlington, MA); Scott L. Harbeson (Cambridge, MA)
Assignee: Concert Pharmaceuticals, Inc.
C07D473/10C07D487/04C07B2200/05
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Quick Facts
Patent No.
US 9,328,113
App. No.
14/391,443
Granted
May 3, 2016
Kind
B2
Abstract

This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentifylline and related compounds are beneficial.

Claims (71)

1. A compound of Formula A:

or pharmaceutically acceptable salts thereof, wherein

each of X 1a , X 1b , X 2a , and X 2b is deuterium;

each of X 3a , X 3b , X 4a , X 4b , X 5a , X 5b and X 6 is hydrogen;

R 1 is —CD 3 ; and

each of R 2 and R 3 is independently CH 3 or CD 3 .

2. The compound of claim 1 , wherein R 3 and R 2 are each —CD 3 .

3. The compound of claim 1 , wherein R 3 and R 2 are each —CH 3 .

4. The compound of claim 1 , wherein R 3 is —CH 3 and R 2 is —CD 3 .

5. The compound of claim 1 , wherein R 2 is —CH 3 and R 3 is —CD 3 .

6. The compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.

7. The compound of claim 1 , wherein the compound is a compound selected from the group consisting of the compounds of Table 1 and wherein any atom not designated as deuterium is present at its natural isotopic abundance:

TABLE 1

X 1a =

X 2a =

X 3a =

X 4a =

X 5a =

Cmpd

X 1b

X 2b

X 3b

X 4b

X 5b

X 6

R 1

R 2

R 3

102

D

D

H

H

H

H

CD 3

CH 3

CH 3

103

D

D

H

H

H

H

CD 3

CD 3

CD 3

110

D

D

H

H

H

H

CD 3

CH 3

CD 3

111

D

D

H

H

H

H

CD 3

CD 3

CH 3

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

9. A method of therapeutic or prophylactic treatment of intermittent claudication in a patient in need thereof, comprising administering to the patient an effective amount of a compound of claim 1 .

Assignments (2)
MERGER Recorded Aug 2, 2023
From: CONCERT PHARMACEUTICALS, INC.
To: SUN PHARMACEUTICAL INDUSTRIES, INC.
Reel/Frame 064465/0383 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 8, 2016
From: TUNG, ROGER D.; PANDYA, BHAUMIK; HARBESON, SCOTT L.
To: CONCERT PHARMACEUTICALS, INC.
Reel/Frame 037915/0913 →
Continuity (2)
Provisional Application 61623858 · Apr 13, 2012
Related Publication 20150119407A1 · Apr 30, 2015