IP Library Granted Patent US 7,989,497
Granted Patent B2
US 7,989,497 · App. 12/512,609 · Granted Aug 2, 2011

Squaramide derivatives as CXCR2 antagonist

Assignee: Novartis AG
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 7,989,497
App. No.
12/512,609
Granted
Aug 2, 2011
Kind
B2
Abstract

The present invention relates to compounds of formula (I) wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Claims (19)

1. The compound which is selected from the group consisting of:

Structure

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is 6-chloro-2-hydroxy-N-methoxy-N-methyl-3-{2-[(R)-1-(5-methyl-furan-2-yl)-propylamino]-3,4-dioxo-cyclobut-1-enyl amino}-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound is 6-chloro-3-{3,4-dioxo-2-[(R)-1-(tetrahydro-furan-2-yl)-propylamino]-cyclobut-1-enylamino}-2-hydroxy-N-methoxy-N-methyl-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein the compound is 6 chloro-2-hydroxy-N-methoxy-N-methyl-3-{2-[(R)-1-((2R,5R)-5-methyl-tetrahydro-furan-2-yl)-propylamino]-3,4-dioxo-cyclobut-1-enylamino}-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 , wherein the compound is 6-chloro-3-[3,4-dioxo-2-((R)-1-pyridin-2-yl-propylamino)-cyclobut-1-enylamino]-2-hydroxy-N-methoxy-N-methyl-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein the compound is 6-chloro-3-[2-(1-ethyl-propylamino)-3,4-dioxo-cyclobut-1-enylamino]-2-hydroxy-N-methoxy-N-methyl-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

7. The compound of claim 6 , wherein the compound is the choline salt.

8. The compound of claim 1 , wherein the compound is 6 chloro-3-{3,4-dioxo-2-[(R)-1-(tetrahydro-furan-2-yl)-propylamino]-cyclobut-1-enylamino}-N-ethyl-2-hydroxy-N-methoxy-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , wherein the compound is 6-chloro-N-ethyl-2-hydroxy-3-(2-(isopropylamino)-3,4-dioxocyclobut-1-enylamino)-N-methoxybenzenesulfonamide, or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , wherein the compound is 3-(4-chloro-2-hydroxy-3-((S)-4-hydroxyisoxazolidin-2-ylsulfonyl)phenylamino)-4-((R)-1-((2R,5R)-5-methyltetrahydrofuran-2-yl)propylamino)cyclobut-3-ene-1,2-dione, or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , wherein the compound is 6-chloro-2-hydroxy-3-(2-(isopropylamino)-3,4-dioxocyclobut-1-enylamino)-N-methoxy-N-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , wherein the compound is (R)-6-chloro-N-ethyl-2-hydroxy-N-methoxy-3-(2-(1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzenesulfonamide, or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , wherein the compound is 6-chloro-3-(2-(heptan-4-ylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N-methoxy-N-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof.

14. The compound of claim 1 , wherein the compound is 6-chloro-3-(2-(cyclopentylamino)-3,4-dioxocyclobut-1-enylamino)-2-hydroxy-N-methoxy-N-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof.

15. The compound of claim 1 , wherein the compound is 3-(3,4-dioxo-2-((R)-1-((S)-tetrahydrofuran-2-yl)propylamino)cyclobut-1-enylamino)-N-ethyl-2-hydroxy-N-methoxybenzenesulfonamide, or a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition, comprising:

the compound according to claim 1 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier or excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2011
From: BAETTIG, URS; D'SOUZA, ANNE-MARIE; HUNT, PETER; PRESS, NEIL JOHN; WATSON, SIMON JAMES
To: NOVARTIS AG
Reel/Frame 026454/0960 →
Priority Claims (1)
EP 08161765 · Aug 4, 2008 · regional
Continuity (2)
Provisional Application 61161627 · Mar 19, 2009
Related Publication 20100029670A1 · Feb 4, 2010