IP Library Granted Patent US 9,782,398
Granted Patent B2
US 9,782,398 · App. 15/116,786 · Granted Oct 10, 2017

Pharmaceutical compositions comprising an antipsychotic drug and a VMAT2 inhibitor and uses thereof

Inventor: Samuel Roger Jesse Hoare (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
A61K31/473A61K31/4745A61K31/519A61K31/551A61K31/5513A61K45/06
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Quick Facts
Patent No.
US 9,782,398
App. No.
15/116,786
Granted
Oct 10, 2017
Kind
B2
Abstract

New methods of treating schizophrenia and schizoaffective disorder by administration of pharmaceutical compositions comprising an antipsychotic compound and a VMAT2 inhibitor to a subject in need thereof are provided.

Claims (12)

1. A method for treating a neuropsychiatric disorder in a subject comprising administering to the subject (a) an antipsychotic drug and (b) a VMAT2 inhibitor, wherein the therapeutically effective amount of the antipsychotic drug administered to the subject is less than the therapeutically effective amount of the antipsychotic drug when administered in the absence of the VMAT2 inhibitor wherein the neuropsychiatric disorder is schizophrenia, schizoaffective disorder, bipolar disorder, major depressive disorder (MDD) or autism and wherein the antipsychotic drug is aripiprazole, asenapine, clozapine, iloperidone, olanzapine, paliperidone, questiapine, risperidone, or ziprasidone and wherein the VMAT2 inhibitor is tetrabenazine (3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one), (2R,3R, 11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol (R,R,R DHTBZ), (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2yl ester, [(2R,3S,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2yl]methanol or 3-isobutyl-9,10-d6-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one (d6-TBZ).

2. The method of claim 1 , wherein the antipsychotic drug and the VMAT2 inhibitor are administered concurrently.

3. The method of claim 2 , wherein the antipsychotic drug and the VMAT2 inhibitor are formulated in the same pharmaceutical composition.

4. The method of claim 1 , wherein the antipsychotic drug is formulated in a first pharmaceutical composition and the VMAT2 inhibitor is formulated in a second pharmaceutical composition.

5. The method of claim 1 , wherein the therapeutically effective amount of the antipsychotic drug is 10 to 90% less than the therapeutically effective amount of the antipsychotic drug when administered in the absence of the VMAT2 inhibitor.

6. The method of claim 1 , wherein the therapeutically effective amount of the antipsychotic drug is at least 25% less than the therapeutically effective amount of the antipsychotic drug when administered in the absence of the VMAT2 inhibitor.

7. The method of claim 1 , wherein the therapeutically effective amount of the antipsychotic drug is at least 50% less than the therapeutically effective amount of the antipsychotic drug when administered in the absence of the VMAT2 inhibitor.

8. The method of any one of claims 1 , 2 - 4 , or 5 - 7 wherein the VMAT2 inhibitor is tetrabenazine (3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one).

9. The method of any one of claims 1 , 2 - 4 , or 5 - 7 wherein the VMAT2 inhibitor is (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol (R,R,R DHTBZ).

10. The method of any one of claims 1 , 2 - 4 or 5 - 7 wherein the VMAT2 inhibitor is (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester.

11. The method of any one of claims 1 , 2 - 4 , or 5 - 7 wherein the VMAT2 inhibitor is [(2R,3S,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-yl]methanol.

12. The method of any one of claims 1 - 7 , wherein the VMAT2 inhibitor is 3-isobutyl-9,10-d 6 -dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one (d 6 -TBZ).

Assignments (4)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2020
From: HOARE, SAMUEL ROGER JESSE
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 052002/0113 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2020
From: GRIGORIADIS, DIMITRI E.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 052002/0129 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2020
From: ASHWEEK, NEIL J.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 052002/0135 →
Continuity (2)
Provisional Application 61937223 · Feb 7, 2014
Related Publication 20160339011A1 · Nov 24, 2016