IP Library Granted Patent US 8,557,815
Granted Patent B2
US 8,557,815 · App. 12/856,360 · Granted Oct 15, 2013

Substituted triazolophthalazine derivatives

Inventor: Scott L. Harbeson (Cambridge, MA)
Assignee: Concert Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,557,815
App. No.
12/856,360
Granted
Oct 15, 2013
Kind
B2
Abstract

This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists.

Claims (53)

1. A compound of Formula Ia,

or a pharmaceutically acceptable salt thereof, wherein:

R 5 is selected from CD 3 and CH 3 ;

R 8 is CD 3 ;

W is —CY 1 Y 2 —, wherein Y 1 and Y 2 are the same and are selected from hydrogen and deuterium; and

Y 3 is hydrogen or deuterium;

wherein there is at least 50.1% incorporation of deuterium at any atom designated as D or deuterium.

2. The compound of claim 1 , wherein Y 3 is hydrogen and W, R 5 , and R 8 are as defined in the table below:

Compound

W

R 5

R 8

102

CD 2

CH 3

CD 3

103

CH 2

CH 3

CD 3

104

CH 2

CD 3

CD 3

105

CD 2

CD 3

CD 3

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein Y 3 is deuterium and W, R 5 , and R 8 are as defined in the table below:

Compound

W

R 5

R 8

112

CD 2

CH 3

CD 3

113

CH 2

CH 3

CD 3

114

CH 2

CD 3

CD 3

115

CD 2

CD 3

CD 3

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein any atom not designated as deuterium in any of the embodiments set forth above is present at its natural isotopic abundance.

5. A pyrogen-free pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt of said compound; and a pharmaceutically acceptable carrier.

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 29, 2011
From: HARBESON, SCOTT L.
To: CONCERT PHARMACEUTICALS, INC.
Reel/Frame 026036/0792 →
Continuity (2)
Provisional Application 61233964 · Aug 14, 2009
Related Publication 20110172235A1 · Jul 14, 2011