IP Library Granted Patent US 10,508,111
Granted Patent B2
US 10,508,111 · App. 15/769,260 · Granted Dec 17, 2019

6-[5-amino-6-(2-ethoxyethoxy)-imidazo[4,5-B]pyridin-3-yl]-nicotinonitrile derivatives and their use as IRAK inhibitors

Inventors: Reginald Christophe Xavier Brys (Mechelen, BE); Raphaël Jean Joël Geney (Romainville, FR); Agnès Marie Joncour (Romainville, FR); Julien Georges Pierre-Olivier Doyon (Beerse, BE); Frédéric Gilbert Labéguère (Frouzins, FR); Jean-Michel Lefrançois (Romainville, FR); Oscar Mammoliti (Mechelen, BE); Benoît Antoine Schmitt (Mechelen, BE); Steven Emiel Van Der Plas (Mechelen, BE); Christel Jeanne Marie Menet (Brussels, BE)
Assignee: GALAPAGOS NV
C07D471/04A61P29/00A61P37/00A61K45/06A61K2300/00
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Quick Facts
Patent No.
US 10,508,111
App. No.
15/769,260
Granted
Dec 17, 2019
Kind
B2
Abstract

The present invention discloses compounds according to Formula I: wherein R 1 , R 2 , and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.

Claims (41)

1. A compound according to Formula I:

wherein

Cy is

monocyclic C 3-7 cycloalkyl optionally substituted with one or more independently selected R 3 , or

4-7 membered monocyclic heterocycloalkyl comprising one or two heteroatoms independently selected from N, S, or O, optionally substituted with one or more independently selected R 3 ;

R 1 is

H,

—SO 3 H,

—P(═O)(OH) 2 ,

C 1-4 alkyl,

—C(═O)-(4-7 membered monocyclic heterocycloalkyl comprising one or two heteroatoms independently selected from N, S, or O), or

—C(═O)C 1-6 alkyl, which C 1-6 alkyl is optionally substituted with one or more independently selected R 4 groups;

R 2 is H or C 1-4 alkyl;

each R 3 is independently selected from:

OH,

═O,

halo, or

C 1-4 alkyl;

each R 4 is independently selected from:

—NR 5a R 5b ,

—C(═O)OH,

4-7 membered monocyclic heterocycloalkyl comprising one or two heteroatoms independently selected from N, S, or O, optionally substituted with one or more independently selected C 1-4 alkyl, or

—NHC(═O)—C 1-4 alkyl-NH 2 ; and

R 5a and R 5b are independently H or C 1-4 alkyl;

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

2. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Cy is monocyclic C 3-7 cycloalkyl substituted with one or two independently selected R 3 .

3. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Cy is tetrahydropyranyl or tetrahydrothiopyranyl, each of which is optionally substituted with one or two independently selected R 3 .

4. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R 3 is selected from OH, ═O, F, or —CH 3 .

5. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is according to Formula IIa, IIb, IIc, IId, IIe or IIf:

6. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R 4 is H, —CH 3 , —SO 3 H, or —P(═O)(OH) 2 .

7. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R 4 is —C(═O)C 1-6 alkyl, which C 1-6 alkyl is substituted with one or two independently selected R 4 .

8. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R 4 is —C(═O)C 1-6 alkyl, which C 1-6 alkyl is substituted with one or two independently selected —C(═O)OH, —NH 2 , —NHCH 3 , or —N(CH 3 ) 2 .

9. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein R 2 is H or —CH 3 .

10. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is

6-[6-[2-(2-hydroxy-ethoxy)-ethoxy]-5-(tetrahydro-pyran-4-ylamino)-imidazo[4,5-b]pyridin-3-yl]-nicotinonitrile, or

(S)-2-amino-3-methyl-butyric acid 2-{2-[3-(5-cyano-pyridin-2-yl)-5-(tetrahydro-pyran-4-ylamino)-3H-imidazo[4,5-b]pyridin-6-yloxy]-ethoxy}-ethyl ester.

11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound or pharmaceutically acceptable salt thereof, according to claim 1 .

12. A pharmaceutical composition according to claim 11 comprising a further therapeutic agent.

13. The pharmaceutical composition according to claim 12 , wherein the further therapeutic agent is an agent for the treatment of rheumatoid arthritis.

14. A method for treatment of rheumatoid arthritis in a human comprising administering an effective amount of the compound of claim 1 to the human.

15. A method for treatment of rheumatoid arthritis in a human comprising administering an effective amount of 6-[6-[2-(2-hydroxy-ethoxy)-ethoxy]-5-(tetrahydro-pyran-4-ylamino)-imidazo[4,5-b]pyridin-3-yl]-nicotinonitrile or (S)-2-amino-3-methyl-butyric acid 2-{2-[3-(5-cyano-pyridin-2-yl)-5-(tetrahydro-pyran-4-ylamino)-3H-imidazo[4,5-b]pyridin-6-yloxy]ethoxy}-ethyl ester to the human.

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Feb 15, 2022
From: GILEAD SCIENCES, INC.
To: GALAPAGOS NV
Reel/Frame 059020/0871 →
SECURITY INTEREST Recorded Aug 23, 2019
From: GALAPAGOS NV
To: GILEAD SCIENCES, INC.
Reel/Frame 050149/0161 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2018
From: BRYS, REGINALD CHIRSTOPHE XAVIER; GENEY, RAPHAËL JEAN JOËL; JONCOUR, AGNÈS MARIE; DOYON, JULIEN GEORGES PIERRE-OLIVIER; LABÉGUÈRE, FRÉDÉRIC GILBERT; LEFRANÇOIS, JEAN-MICHEL; MAMMOLITI, OSCAR; SCHMITT, BENOÎT ANTOINE; VAN DER PLAS, STEVEN EMIEL; MENET, CHRISTEL JEANNE MARIE
To: GALAPAGOS NV
Reel/Frame 045618/0097 →
Priority Claims (1)
GB 1518456.7 · Oct 19, 2015 · national
Continuity (1)
Related Publication 20180305351A1 · Oct 25, 2018