IP Library Granted Patent US 8,546,396
Granted Patent B2
US 8,546,396 · App. 13/132,294 · Granted Oct 1, 2013

N-(hetero)aryl, 2-(hetero)aryl—substituted acetamides for use as Wnt signaling modulators

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Quick Facts
Patent No.
US 8,546,396
App. No.
13/132,294
Granted
Oct 1, 2013
Kind
B2
Abstract

The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A 1 , A 2 , B, Y and Z all represent rings.

Claims (29)

1. A compound having Formula (6):

or a physiologically acceptable salt thereof, wherein:

wherein X 1 , X 2 , X 3 and X 4 is selected from N and CR 7 ;

one of X 5 , X 6 , X 7 and X 8 is N and the others are CH;

X 9 is selected from N and CH;

Z is selected from phenyl, pyrazinyl, pyridinyl, pyridazinyl and piperazinyl; wherein each phenyl, pyrazinyl, pyridinyl, pyridazinyl or piperazinyl of Z is optionally substituted with an R 6 group;

R 1 , R 2 and R 3 are hydrogen;

m is 1;

R 4 is selected from hydrogen, halo, difluoromethyl, trifluoromethyl and methyl;

R 6 is selected from hydrogen, halo and —C(O)R 10 ; wherein R 10 is methyl; and

R 7 is selected from hydrogen, halo, cyano, methyl and trifluoromethyl.

2. The compound of claim 1 , wherein said compound is selected from

or a physiologically acceptable salt thereof.

3. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

4. The compound of claim 1 , wherein said compound is 2-(2′,3-dimethyl-2,4′-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, or a physiologically acceptable salt thereof.

5. The compound of claim 1 , wherein said compound is N-(2,3′-bipyridin-6′-yl)-2-(2′,3-dimethyl-2,4′-bipyridin-5-yl)acetamide, or a physiologically acceptable salt thereof.

6. The compound of claim 1 , wherein said compound is N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2′-methyl-3-(trifluoromethyl)-2,4′-bipyridin-5-yl)acetamide, or a physiologically acceptable salt thereof.

7. The compound of claim 1 , wherein said compound is N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2′-fluoro-3-methyl-2,4′-bipyridin-5-yl)acetamide, or a physiologically acceptable salt thereof.

8. The compound of claim 1 , wherein said compound is 2-(2′-fluoro-3-methyl-2,4′-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide; or a physiologically acceptable salt thereof.

9. The compound of claim 2 , wherein said physiologically acceptable salt is a fumaric acid salt of said compound.

10. The compound of claim 4 , wherein said physiologically acceptable salt is a fumaric acid salt of said compound.

11. The compound of claim 5 , wherein said physiologically acceptable salt is a fumaric acid salt of said compound.

12. The compound of claim 8 , wherein said physiologically acceptable salt is a fumaric acid salt of said compound.

13. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 2 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

14. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 4 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

15. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 5 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

16. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 6 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

17. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 7 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

18. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 8 or a physiologically acceptable salt thereof, and a physiologically acceptable carrier.

Assignments (4)
MERGER Recorded Apr 16, 2015
From: IRM LLC
To: NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.
Reel/Frame 035444/0397 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2015
From: NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.
To: NOVARTIS AG
Reel/Frame 035453/0224 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 26, 2011
From: CHENG, DAI; ZHANG, GUOBAO; HAN, DONG; PAN, SHIFENG
To: IRM LLC
Reel/Frame 027127/0590 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 26, 2011
From: CHENG, DAI; ZHANG, GUOBAO; HAN, DONG; PAN, SHIFENG; GAO, WENQI
To: IRM LLC
Reel/Frame 027127/0923 →