IP Library Granted Patent US 8,399,467
Granted Patent B2
US 8,399,467 · App. 13/174,662 · Granted Mar 19, 2013

Substituted triazolo-pyridazine derivatives

Inventor: Scott L. Harbeson (Lexington, MA)
Assignee: Concert Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,399,467
App. No.
13/174,662
Granted
Mar 19, 2013
Kind
B2
Abstract

This invention relates to novel substituted triazolo-pyridazines, their derivatives, 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 an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist.

Claims (23)

1. A method of:

a. inhibiting the α-1 subtype of the GABA-A receptor in a cell; or

b. activating one or more of the α2, α3 and α5 subtypes of the GABA-A receptor in a cell,

the method comprising contacting the cell with a compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is CH 3 or CD 3 ;

R 2 is —C(CD 3 ) 3 ; and

each of Y 1a , Y 1b , and Y 2 is independently hydrogen or deuterium.

2. A method of treating a patient suffering from, a disease or condition selected from neuropathic pain, inflammatory pain, and migraine pain, comprising the step of administering to the patient in need thereof a composition comprising a compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is CH 3 or CD 3 ;

R 2 is —C(CD 3 ) 3 ; and

each of Y 1a Y 1b , and Y 2 is independently hydrogen or deuterium;

and an acceptable carrier.

3. The method of claim 2 , wherein Y 1a and Y 1b are the same.

4. The method of claim 3 , wherein the compound of formula I is selected from any one of the following compounds:

or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

6. The method of claim 2 , wherein in the compound of formula I any atom not designated as deuterium is present at its natural isotopic abundance.

7. The method of claim 2 , wherein the composition is formulated for pharmaceutical administration, wherein the carrier is a pharmaceutically acceptable carrier.

8. The method of claim 7 , wherein the composition is formulated for oral administration.

9. The method of claim 2 , wherein the disease or condition is inflammatory pain.

Assignments (1)
MERGER Recorded Aug 2, 2023
From: CONCERT PHARMACEUTICALS, INC.
To: SUN PHARMACEUTICAL INDUSTRIES, INC.
Reel/Frame 064465/0383 →
Continuity (3)
Continuation 12550346 · Aug 28, 2009
Provisional Application 61093293 · Aug 29, 2008
Related Publication 20120004236A1 · Jan 5, 2012