Medicaments for slowing Parkinson's disease

• US 10,357,468 B2
• Filed: 05/27/2015
• Issued: 07/23/2019
• Est. Priority Date: 11/28/2014
• Status: Active Grant

• Current Assignee: BIAL Portela & Ca, SA
• Original Assignee: BIAL Portela & Ca, SA
• Inventors: Soares da Silva, Patricio Manuel Vieira Araujo, Rocha, Jose Francisco da Costa de Pinho
• Primary Examiner(s): Ulm, John D
• Application Number:
  US15/528,886
• Publication Number:
  US 20170340593A1
• Time in Patent Office: 1,518 Days
• Field of Search: None
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/4439 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole nicotine A61K31/465
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Opicapone, levodopa and an AADC inhibitor are described for use in slowing the progression of Parkinson'"'"'s Disease.

Claims

1. A method of slowing progression of Parkinson'"'"'s Disease which comprises administering to a patient not previously treated with a COMT inhibitor an effective amount of:

(i) levodopa;

(ii) an AADC inhibitor; and

(iii) opicapone, wherein the dose of opicapone is 15 mg to 100 mg once per day;

wherein the patient not previously treated with a COMT inhibitor refers to a patient

(1) experiencing a mean daily OFF time of up to 6 hours;

(2) having a PD diagnosis for up to 8 years;

(3) experiencing motor symptoms and/or motor complications for up to 4 years;

or

(4) taking an average daily dose of levodopa of up to 800 mg.

2. The method of claim 1, wherein the COMT inhibitor is opicapone.

3. The method of claim 1, wherein the patient has not previously been treated with levodopa.

4. The method of claim 1, wherein the slowing of the progression of Parkinson'"'"'s Disease involves a delay in the progression of Parkinson'"'"'s Disease by a period of at least one month.

5. The method of claim 1, wherein opicapone is administered once a day and levodopa is administered from 2 to 10 times a day.

6. The method of claim 1, wherein the dose of opicapone is 25 mg to 100 mg.

7. The method of claim 1, wherein the AADC inhibitor is carbidopa or benserazide.

8. The method of claim 1, wherein the levodopa is present in a unit dose of from 50 mg to 250 mg.

9. The method of claim 1, wherein the levodopa is present in a tablet at 100 mg.

10. The method of claim 1, wherein the AADC inhibitor is carbidopa or benserazide, wherein the levodopa and the AADC inhibitor are present in a single dosage unit.

11. The method of claim 10, wherein the single dosage unit is a tablet comprising 100 mg levodopa and 25 mg carbidopa for use 3, 4, 5 or 6 times a day and opicapone 50 mg for use once a day.

12. The method of claim 1, wherein the method is the first treatment provided to the patient for treatment of Parkinson'"'"'s Disease.

13. The method of claim 1, wherein the patient benefits by more than 0.25 hr in OFF period.

14. The method of claim 1, wherein the patient has previously been treated for Parkinson'"'"'s disease with a dopamine agonist or MAO-B inhibitor.

15. The method of claim 1, wherein the patient has not previously been treated for Parkinson'"'"'s disease with a dopamine agonist or MAO-B inhibitor.

16. A method of delaying progression of Parkinson'"'"'s Disease in patients treated with an effective dose of levodopa and an AADC inhibitor which comprises administering an effective dose of opicapone to said patient,

wherein the dose of opicapone is 15 mg to 100 mg once per day;

wherein the patient refers to a patient

(1) experiencing a mean daily OFF time of up to 6 hours;

(2) having a PD diagnosis for up to 8 years;

(3) experiencing motor symptoms and/or motor complications for up to 4 years;

or

(4) taking an average daily dose of levodopa of up to 800 mg.

17. The method of claim 16, wherein opicapone is administered once a day, wherein the dose of opicapone is 25 mg to 100 mg.

18. The method of claim 17, wherein the dose of opicapone is 50 mg.

19. The method of claim 16, wherein levodopa is administered 3, 4, 5 or 6 times a day, wherein levodopa is present in a unit dose of from 50 mg to 250 mg.

20. The method of claim 16, wherein the AADC is carbidopa or benserazide in a ratio of 1:

4 with levodopa.

21. The method of claim 19, wherein levodopa is used at 100 mg and carbidopa at 25 mg.