IP Library › Granted Patent US 11,053,245
Granted Patent B2
US 11,053,245 · App. 14/394,469 · Granted Jul 6, 2021

Methods

Inventors: Sharon Mates (New York, NY); Robert Davis (New York, NY); Kimberly Vanover (New York, NY)
Assignee: INTRA-CELLULAR THERAPIES, INC.
C07D471/14A61K31/445A61K31/4985A61K31/5383A61K45/06C07D471/16
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Quick Facts
Patent No.
US 11,053,245
App. No.
14/394,469
Granted
Jul 6, 2021
Kind
B2
Abstract

Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

Claims (20)

1. A method for the treatment of non-remitting post-traumatic stress disorder, comprising administering to a patient in need thereof, who has not responded adequately to standard SSRI therapy selected from citalopram, sertraline, fluoxetine and/or paroxetine, an effective amount of a compound of Formula I:

wherein X is —N(CH 3 ); and Y is —C(O)—, in free or pharmaceutically acceptable salt form.

2. The method according to claim 1 , wherein the disorder is posttraumatic stress disorder and the wherein the method is effective to treat the symptoms of avoidance of stimuli and numbing of general responsiveness.

3. The method of claim 1 wherein the patient has not responded adequately to treatment with sertraline.

4. The method of claim 1 , wherein the administration of the compound of Formula I is an adjunct to the administration of one or more additional antidepressants.

5. The method of claim 4 , wherein the administration of one of more additional antidepressants is an adjunct to administration of the compound of Formula I.

6. The method of claim 4 , wherein the antidepressant is selected from one or more of amitriptyline, amoxapine, bupropion, citalopram, clomipramine, desipramine, doxepin, duloxetine, escitaloprame, fluoxetine, fluvoxamine, imipramine, isocarboxazid, maprotiline, mirtazapine, nefazodone, nortriptyline, paroxetine, phenlzine sulfate, protiptyline, sertraline, tranylcypromine, trazodone, trimipramine, and venlafaxine, in free or pharmaceutically acceptable salt form.

7. The method of claim 4 , wherein the antidepressant is one or more antidepressants selected from selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and tricyclic antidepressants.

8. The method of claim 7 wherein the antidepressant is a SSRI.

9. The method of claim 1 , wherein the compound of Formula I is administered orally as a composition comprising a pharmaceutically acceptable diluent or carrier as an oral unit dose form that is a tablet, or capsule.

10. The method of claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 1 mg to about 140 mg.

11. The method claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 1 mg to about 100 mg.

12. The method of claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 10 mg to about 100 mg.

13. The method of claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 10 mg to about 50 mg.

14. The method of claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 20 mg to about 40 mg.

15. The method of claim 1 , wherein the effective amount of the compound of Formula I is a daily dose of about 1 mg to about 10 mg.

16. The method of claim 1 further comprising administering one or more additional therapeutic agents selected from compounds that modulate GABA activity, a GABA-B agonist, a 5-HT modulator, a melatonin agonist, an ion channel modulator a serotonin-2 antagonist/reuptake inhibitor (SARIs), an orexin receptor antagonist, an H3 agonist, a noradrenergic antagonist, a galanin agonist, a CRH antagonist, human growth hormone, a growth hormone agonist, estrogen, an estrogen agonist, a neurokinin-1 drug, and an antipsychotic agent, in free or pharmaceutically acceptable salt form.

17. The method of claim 1 further comprising administering one or more additional therapeutic agents selected from a group consisting of modafinil, armodafinil, doxepin, alprazolam, bromazepam, clobazam, clonazepam, clorazepate, diazepam, flunitrazepam, flurazepam, lorazepam, midazolam, nitrazepam, oxazepam, temazapam, triazolam, indiplon, zopiclone, eszopiclone, zaleplon, Zolpidem, gabaxadol, vigabatrin, tiagabine, EVT 201 (Evotec Pharmaceuticals), estazolam, ketanserin, risperidone, eplivanserin, volinanserin (Sanofi-Aventis, France), pruvanserin, MDL 100907 (Sanofi-Aventis, France), HY10275 (Eli Lilly), APD125 (Arena Pharmaceuticals, San Diego, Calif.), AVE8488 (Sanofi-Aventis, France), repinotan, sarizotan, eptapirone, buspirone, MN-305 (MediciNova, San Diego, Calif.), melatonin, ramelteon (ROZEREM®, Takeda Pharmaceuticals, Japan), VEC-162 (Vanda Pharmaceuticals, Rockville, Md.), PD-6735 (Phase II Discovery), agomelatine, lamotrigine, gabapentin, pregabalin, orexin, a 1,3-biarylurea, SB-334867-a (GlaxoSmithKline, UK), GW649868 (GlaxoSmithKline), a benzamide derivative, Org 50081 (Organon-Netherlands), ritanserin, nefazodone, serzone, trazodone, Casopitant (GlaxoSmithKline), amitriptyline, amoxapine, bupropion, citalopram, clomipramine, desipramine, doxepin, duloxetine, escitaloprame, fluoxetine, fluvoxamine, imipramine, isocarboxazid, maprotiline, mirtazapine, nefazodone, nortriptyline, paroxetine, phenelzine sulfate, protiptyline, sertraline, tranylcypromine, trazodone, trimipramine, velafaxine, chlorpromazine, haloperidol, droperidol, fluphenazine, loxapine, mesoridazine molidone, perphenazine, pimozide, prochlorperazine promazine, thioridazine, thiothixene, trifluoperazine, clozapine, aripiparazole, olanzapine, quetiapine, risperidone, ziprasidone and paliperidone, in free or pharmaceutically acceptable salt form.

18. The method of claim 1 wherein the patient has also not responded to treatment with additional antidepressants selected from selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and tricyclic antidepressants.

19. The method of claim 5 , wherein the antidepressant is selected from one or more of amitriptyline, amoxapine, bupropion, citalopram, clomipramine, desipramine, doxepin, duloxetine, escitaloprame, fluoxetine, fluvoxamine, imipramine, isocarboxazid, maprotiline, mirtazapine, nefazodone, nortriptyline, paroxetine, phenlzine sulfate, protiptyline, sertraline, tranylcypromine, trazodone, trimipramine, and venlafaxine.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 3, 2019
From: MATES, SHARON; VANOVER, KIMBERLY; DAVIS, ROBERT
To: INTRA-CELLULAR THERAPIES, INC.
Reel/Frame 050619/0502 →
Continuity (6)
Provisional Application 61624291 · Apr 14, 2012
Provisional Application 61624292 · Apr 14, 2012
Provisional Application 61624293 · Apr 14, 2012
Provisional Application 61671713 · Jul 14, 2012
Provisional Application 61671723 · Jul 14, 2012
Related Publication 20150072964A1 · Mar 12, 2015
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