IP Library Granted Patent US 11,072,611
Granted Patent B2
US 11,072,611 · App. 16/682,553 · Granted Jul 27, 2021

Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Inventors: Nicolas Desroy (Romainville, FR); Bertrand Heckmann (Romainville, FR); Reginald Christophe Xavier Brys (Mechelen, BE); Agnès Marie Joncour (Romainville, FR); Christophe Peixoto (Romainville, FR); Xavier Marie Bock (Romainville, FR)
Assignee: GALAPAGOS NV
C07D471/04A61K31/437A61K31/444A61K31/4545A61K31/496A61K31/506A61K31/5377A61K31/541A61K45/06
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Quick Facts
Patent No.
US 11,072,611
App. No.
16/682,553
Granted
Jul 27, 2021
Kind
B2
Abstract

The present invention discloses compounds according to Formula I: Wherein R 1a , R 1b , R 2 , R 4 , R 5 , R 6a , R 6b , R 8 , W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

Claims (18)

1. A compound of the formula:

or a pharmaceutically acceptable salt, or a solvate, or a pharmaceutically acceptable salt of a solvate thereof.

2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 .

4. A pharmaceutical composition comprising the compound according to claim 1 , or a pharmaceutically acceptable salt, or a solvate, or a pharmaceutically acceptable salt of a solvate thereof, and a pharmaceutically acceptable carrier.

5. The pharmaceutical composition according to claim 4 , comprising a further therapeutic agent.

6. The pharmaceutical composition according to claim 5 , wherein the further therapeutic agent is an agent for the treatment of idiopathic pulmonary fibrosis.

7. The pharmaceutical composition according to claim 4 , comprising the compound of the formula:

or a pharmaceutically acceptable salt thereof.

8. The pharmaceutical composition according to claim 7 , comprising a further therapeutic agent.

9. The pharmaceutical composition according to claim 8 , wherein the further therapeutic agent is for the treatment of idiopathic pulmonary fibrosis.

10. The pharmaceutical composition according to claim 4 comprising the compound of the formula:

11. The pharmaceutical composition according to claim 10 , comprising a further therapeutic agent.

12. The pharmaceutical composition according to claim 11 , wherein the further therapeutic agent is for the treatment of idiopathic pulmonary fibrosis.

13. A method of inhibiting ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2), which method comprises contacting the ENPP2 with a compound according to claim 1 , or a pharmaceutically acceptable salt, or a solvate, or a pharmaceutically acceptable salt of a solvate thereof.

14. The method of inhibiting ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2) according to claim 13 , which method comprises contacting the ENPP2 with the compound of the formula:

or a pharmaceutically acceptable salt thereof.

15. The method of inhibiting ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2) according to claim 13 , which method comprises contacting the ENPP2 with the compound of the formula:

Assignments (2)
CHANGE OF NAME Recorded Jun 4, 2026
From: GALAPAGOS
To: LAKEFRONT BIOTHERAPEUTICS
Reel/Frame 074845/0068 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 13, 2019
From: BRYS, REGINALD CHRISTOPHE XAVIER; DESROY, NICOLAS; HECKMANN, BERTRAND; JONCOUR, AGNES MARIE; PEIXOTO, CHRISTOPHE; BOCK, XAVIER MARIE; GALAPAGOS SASU
To: GALAPAGOS NV
Reel/Frame 050999/0215 →
Continuity (7)
Division 16146450 · Sep 28, 2018
Continuation 15583161 · May 1, 2017
Continuation 14977918 · Dec 22, 2015
Continuation 14572870 · Dec 17, 2014
Continuation 14205885 · Mar 12, 2014
Provisional Application 61781174 · Mar 14, 2013
Related Publication 20200239466A1 · Jul 30, 2020