IP Library › Patent Application 15200228
Patent Application
App. No. 15/200,228

NOVEL SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

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Patent No.
US None
App. No.
15/200,228
Abstract

The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

Claims (33)

1 . (canceled)

2 . (canceled)

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15 . (canceled)

16 . A pharmaceutically acceptable salt of a compound according to Formula (I):

wherein the salt is a 1:1 free base/maleic acid salt.

17 . A pharmaceutically acceptable salt according to claim 16 , wherein the salt is in a crystalline form.

18 . A pharmaceutically acceptable salt according to claim 16 , wherein the salt exhibits peaks on a XRFD spectrum.

19 . A method for the prophylaxis and/or treatment of a condition selected from inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons, comprising administering an effective amount of a pharmaceutically acceptable salt according to claim 16 .

20 . The method according to claim 19 , wherein the pharmaceutically acceptable salt is administered in combination with another therapeutic agent.

21 . The method according to claim 19 , wherein the further therapeutic agent is an agent for the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

22 . A method for preparing a pharmaceutically acceptable salt of claim 16 comprising: combining the compound according to Formula I with maleic acid in an inert solvent; and precipitating said salt from said solvent.

23 . A method for preparing a pharmaceutically acceptable salt of claim 16 comprising: combining the compound of Formula I and maleic acid in a suitable solvent in order to achieve full dissolution; evaporating the solvent in order to achieve supersaturation; and crystallizing the salt.

24 . The method according to claim 22 , wherein the salt is obtained by mixing the compound of Formula I and the acid in a molar ratio of between 5:1 and 1:5 of Formula I: acid.

25 . The method according to claim 22 , wherein the solvent is selected from acetonitrile, dioxane, THF, acetone, DCM, and MeOH.

26 . The pharmaceutically acceptable salt according to claim 16 , obtainable by:

i) suspending 1 equivalent of the compound of Formula I in 20 volumes of 5% water in acetone at 25° C.,

ii) warming the suspension of step i) to 50° C.,

iii) adding 2.1 equivalent of maleic acid (1 M solution in THF) to the stirred suspension at 50° C. obtained in the previous step ii),

iv) cooling the mixture of step iii) to 25° C. at 1° C./min and stirring at 25° C. for 22 h,

v) separating by filtration the resulting solid obtained in the previous step iv),

vi) drying under suction said resulting solid obtained in the previous step v).

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 13, 2020
From: WIGERINCK, PIET
To: GALAPAGOS NV
Reel/Frame 051498/0134 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: SABOURAULT, NICOLAS LUC; GALAPAGOS SASU
To: GALAPAGOS NV
Reel/Frame 041812/0329 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: DE FAVERI, CARLA; LUNDBECK PHARMACEUTICALS ITALY SPA
To: GALAPAGOS NV
Reel/Frame 041812/0703 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: SHEIKH, AHMAD
To: ABBVIE INC.
Reel/Frame 041813/0005 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: ABBVIE INC.
To: GALAPAGOS NV
Reel/Frame 041813/0541 →