IP Library Granted Patent US 10,526,329
Granted Patent B2
US 10,526,329 · App. 16/146,450 · Granted Jan 7, 2020

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 10,526,329
App. No.
16/146,450
Granted
Jan 7, 2020
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 7 , 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 (10)

1. A process for preparing a compound of formula G:

comprising the steps of

(a) reacting a compound of formula C with Boc-piperazine to form a compound of formula

(b) reacting a compound of formula D with HCl to form a compound of formula

 and,

(c) reacting a compound of formula E with a compound of formula

2. The process of claim 1 further comprising step (d) reacting a compound of formula

with a compound of formula

to form a compound of formula

3. The process of claim 2 further comprising the step of obtaining the compound of formula (B) by reacting 4-fluorobenzoylacetonitrile with thiourea to obtain 2-Amino-4-(4-fluoro-phenyl)-thiazole-5-carbonitrile, and, 2-Amino-4-(4-fluoro-phenyl)-thiazole-5-carbonitrile transformed into the compound of formula (B) by an aminodisplacement reaction.

Assignments (2)
CHANGE OF NAME Recorded Jun 4, 2026
From: GALAPAGOS
To: LAKEFRONT BIOTHERAPEUTICS
Reel/Frame 074845/0068 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 28, 2018
From: BRYS, REGINALD CHRISTOPHE XAVIER; DESROY, NICOLAS; HECKMANN, BERTRAND; JONCOUR, AGNES MARIE; PEIXOTO, CHRISTOPHE; BOCK, XAVIER MARIE; GALAPAGOS SASU
To: GALAPAGOS NV
Reel/Frame 047009/0739 →
Continuity (6)
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 20190169184A1 · Jun 6, 2019
Cited By (1)
US 12,344,619