IP Library › Granted Patent US 10,376,520
Granted Patent B2
US 10,376,520 · App. 15/566,002 · Granted Aug 13, 2019

Methods for the treatment of cardiovascular disorders

Inventors: Piet Tom Bert Paul Wigerinck (Mechelen, BE); Gerben Albert Eleutherius Van 'T Klooster (Mechelen, BE)
Assignee: GALAPAGOS NV
A61K31/541A61K31/54A61K45/06A61P3/06A61P9/10
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Quick Facts
Patent No.
US 10,376,520
App. No.
15/566,002
Granted
Aug 13, 2019
Kind
B2
Abstract

The present invention discloses compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, pharmaceutical compositions comprising the same, and methods of treatment using the same, for use in the prophylaxis and/or treatment of cardiovascular disorders and/or dyslipidemia, by administering the compound according to Formula (I).

Claims (37)

1. A method for the prophylaxis and/or treatment of cardiovascular disorders and/or dyslipidemia, comprising:

administering to a patient in need thereof an effective amount of a compound according to Formula I:

or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, or an active metabolite thereof.

2. The method of claim 1 , wherein the salt of a solvate is a [Compound according to Formula I:HCl:3H 2 0] adduct.

3. The method of claim 1 , wherein the cardiovascular disorder is atherosclerosis.

4. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered in combination with a further therapeutic agent.

5. A method for the prophylaxis and/or treatment of cardiovascular disorders and/or dyslipidemia, comprising:

administering to a patient in need thereof a pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, excipient, or diluent and an effective amount of a compound according to Formula I:

or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, excipient, or diluent.

6. The method of claim 5 , wherein the pharmaceutical composition comprises comprising a further therapeutic agent.

7. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered to the patient, and wherein the patient is an individual presenting an abnormal lipid profile.

8. The method of claim 7 , wherein the abnormal lipid profile is characterized by [LDL] below 50 mg/dL (or below 1.3 mmol/L) and [HDL] below 40 mg/dL (or below 1.04 mmol/L).

9. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered to the patient, and wherein the patient is a clinical non RA-afflicted patient.

10. The method of claim 9 , wherein the patient's condition is measured by a DAS28(CRP) score.

11. The method of claim 10 , wherein the DAS28(CRP) score is less than 2.6.

12. The method of claim 10 , wherein the patient has a CRP level greater than 3 mg/L.

13. The method of claim 1 , wherein the patient is a clinical RA-afflicted patient and administration occurs at least once a week over a period of greater than 4 weeks.

14. The method of claim 1 , wherein the patient is a clinical RA-afflicted patient and the patient's condition is measured by a DAS28(CRP) score.

15. The method of claim 14 , wherein the DAS28(CRP) score is greater than 3.2.

16. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered at a dose of 100 mg twice a day.

17. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered at a dose of 200 mg once a day.

18. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is administered at a dose from 25 mg to 400 mg.

19. The method of claim 4 , wherein the further therapeutic agent is an agent for the prophylaxis and/or treatment of cardiovascular disease.

20. The method of claim 4 , wherein the further therapeutic agent is an agent for the prophylaxis and/or treatment of atherosclerosis.

21. The method of claim 5 , wherein the patient is an individual presenting an abnormal lipid profile.

22. The method of claim 21 , wherein the abnormal lipid profile is characterized by [LDL] below 50 mg/dL (or below 1.3 mmol/L) and [HDL] below 40 mg/dL (or below 1.04 mmol/L).

23. The method of claim 5 , wherein the patient is a clinical non RA-afflicted patient.

24. The method of claim 23 , wherein the patient's condition is measured by a DAS28(CRP) score.

25. The method of claim 24 , wherein the DAS28(CRP) score is less than 2.6.

26. The method of claim 24 , wherein the patient has a CRP level greater than 3 mg/L.

27. The method of claim 5 , wherein the patient is a clinical RA-afflicted patient, and wherein the pharmaceutical composition is administered at least once a week over a period of greater than 4 weeks.

28. The method of claim 5 , wherein the patient is a clinical RA-afflicted patient, and the patient's condition is measured by a DAS28(CRP) score.

29. The method of claim 28 , wherein the DAS28(CRP) score is greater than 3.2.

30. The method of claim 5 , wherein the compound or the pharmaceutically acceptable salt thereof is administered at a dose of 100 mg twice a day.

31. The method of claim 5 , wherein the compound or the pharmaceutically acceptable salt thereof is administered at a dose of 200 mg once a day.

32. The method of claim 6 , wherein the further therapeutic agent is an agent for the prophylaxis and/or treatment of cardiovascular disease.

33. The method of claim 6 , wherein the further therapeutic agent is an agent for the prophylaxis and/or treatment of atherosclerosis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2024
From: GALAPAGOS NV
To: ALFASIGMA S.P.A.
Reel/Frame 067126/0592 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2017
From: VAN 'T KLOOSTER, GERBEN ALBERT ELEUTHERIUS; WIGERINCK, PIET TOM BERT PAUL
To: GALAPAGOS NV
Reel/Frame 043850/0241 →
Priority Claims (5)
GB 1506228.4 · Apr 13, 2015 · national
GB 1507109.5 · Apr 27, 2015 · national
GB 1513344 · Jul 29, 2015 · national
GB 1513991.8 · Aug 7, 2015 · national
GB 1521542.9 · Dec 7, 2015 · national
Continuity (1)
Related Publication 20180185377A1 · Jul 5, 2018
Cited By (4)
US 12,234,235 US 12,329,758 US 12,502,394 US 12,558,360