Dosage regimen for COMT inhibitors

• US 9,745,290 B2
• Filed: 04/17/2015
• Issued: 08/29/2017
• Est. Priority Date: 01/31/2007
• Status: Active Grant

• Current Assignee: BIAL Portela & Ca, SA
• Original Assignee: BIAL Portela & Ca, SA
• Inventors: Learmonth, David Alexander, Kiss, Laszlo Erno, Palma, Pedro Nuno Leal, Ferreira, Humberto dos Santos, Soares da Silva, Patricio Manuel V. A.
• Primary Examiner(s): CRUZ, KATHRIEN ANN
• Application Number:
  US14/689,397
• Publication Number:
  US 20160009699A1
• Time in Patent Office: 865 Days
• Field of Search: 514340
• 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: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 413/04 directly linked by a ring-member-to-ring-member bond

Abstract

The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.

Claims

1. An individual dosage unit comprising 1 to 500 mg of a compound of formula I

2. The individual dosage unit of claim 1, wherein the compound of general formula I is 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]-oxadiazol-5-yl]-3-nitrobenzene-1,2-diol.

3. The individual dosage unit of claim 1, wherein the individual dosage unit comprises 2 to 300 mg of the compound of formula I or a pharmaceutically acceptable salt thereof.

4. The individual dosage unit of claim 1, wherein the individual dosage unit comprises 3 to 100 mg of the compound of formula I or a pharmaceutically acceptable salt thereof.

5. The individual dosage unit of claim 1, wherein the individual dosage unit comprises 5 to 50 mg of the compound of formula I or a pharmaceutically acceptable salt thereof.

6. The individual dosage unit of claim 1, wherein the individual dosage unit comprises 5 mg of the compound of formula 1 or a pharmaceutically acceptable salt thereof.

7. The individual dosage unit of claim 1, wherein the individual dosage unit comprises 50 mg of the compound of formula I or a pharmaceutically acceptable salt thereof.

8. The individual dosage unit of claim 7, wherein the individual dosage unit is in the form of a tablet.

9. The individual dosage unit of claim 1, wherein the individual dosage unit is in combination with L-DOPA and/or an aromatic L-amino acid decarboxylase inhibitor.

10. The individual dosage unit of claim 2, wherein the individual dosage unit is in combination with L-DOPA and/or an aromatic L-amino acid decarboxylase inhibitor.

11. A method of treating Parkinson'"'"'s disease in a patient in need thereof comprising administering to the patient an individual dosage unit according to claim 1.

12. The method of claim 11, wherein the compound of general formula I is 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]-oxadiazol-5-yl]-3-nitrobenzene-1,2-diol.

13. A package comprising an individual dosage unit as defined in claim 1, wherein the package further comprises L-DOPA and/or an AADC inhibitor.

14. A package comprising an individual dosage unit as defined in claim 2.

15. An orally administrable tablet containing 50 mg of 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]-oxadiazol-5-yl]-3-nitrobenzene-1,2-diol.