Treatment of cataplexy

Patent metadata

Field	Value
Publication number	US-11713292-B2
Application number	US-202117383707-A
Country	US
Kind code	B2
Filing date	Jul 23, 2021
Priority date	Mar 13, 2013
Publication date	Aug 1, 2023
Grant date	Aug 1, 2023

Abstract

The present invention relates to a method of treating cataplexy in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds.

First claim

We claim:

1. A method of treating cataplexy in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I):

or a pharmaceutically acceptable salt or ester thereof;
wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms;
x is; and
R 1 and R 2 are hydrogen.

2. The method of claim 1 , wherein the compound of Formula I is an enantiomer of Formula I substantially free of other enantiomers or an enantiomeric mixture wherein one enantiomer of Formula I predominates.

3. The method of claim 2 , wherein the enantiomer of Formula I predominates to the extent of about 90% or greater.

4. The method of claim 2 , wherein the enantiomer of Formula I predominates to the extent of about 98% or greater.

5. The method of claim 1 , wherein the enantiomer of Formula Ia is the (R) or (D) enantiomer.

6. The method of claim 1 , wherein the enantiomer of Formula Ia is the (S) or (L) enantiomer.

7. The method of claim 2 , wherein the enantiomer of Formula I substantially free of other enantiomers is the compound of Formula Ib or an enantiomeric mixture wherein the compound of Formula Ib predominates:

or a pharmaceutically acceptable salt or ester thereof.

8. The method of claim 7 , wherein the compound of Formula Ib predominates to the extent of about 90% or greater.

9. The method of claim 7 , wherein the compound of Formula Ib predominates to the extent of about 98% or greater.

10. The method of claim 1 , wherein the cataplexy is associated with narcolepsy.

11. The method of claim 1 , wherein the cataplexy is secondary to a condition that lowers hypocretin levels in the subject.

12. The method of claim 11 , wherein the condition is selected from the group consisting of brain tumor, astrocytomas, glioblastoma, glioma, subependynoma, craniopharyngioma, arterio-venous malformations, ischemic events, multiple sclerosis, head injury, brain surgery, paraneoplastic syndromes, Neimann-Pick type C disease, and encephalitis.

13. The method of claim 1 , wherein the therapeutically effective amount of the compound of Formula I is from about 0.01 mg/kg/dose to about 150 mg/kg/dose.

14. The method of claim 1 , wherein the therapeutically effective amount of the compound of Formula I is from about 1 mg/day to about 7000 mg/day.

15. The method of claim 1 , wherein the compound of Formula I is administered orally.

16. The method of claim 1 , wherein the compound of Formula I is administered in the form of a capsule or tablet.

17. The method of claim 1 , wherein the compound of Formula I is administered in the form of a capsule or tablet at a dose of about 25 mg to about 300 mg without any excipients.

18. The method of claim 1 , wherein the compound of Formula I is the hydrochloride salt.

Assignees

• Axsome Malta Ltd
• Sk Biopharmaceuticals Co Ltd

Inventors

• Khayrallah Moise A
• Bream Gary
• Butts Stephen E

Classifications

• A61P21/00

  Drugs for disorders of the muscular or neuromuscular system · CPC title

• C07C271/02 Primary

  Carbamic acids; Salts of carbamic acids (unsubstituted carbamic acid or salts thereof C01B21/12) · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/27 Primary

  of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine · CPC title