IP Library Granted Patent US 10,702,522
Granted Patent B2
US 10,702,522 · App. 16/165,832 · Granted Jul 7, 2020

Methods and compositions for sleep disorders and other disorders

Inventors: Sharon Mates (New York, NY); Allen Fienberg (New York, NY); Lawrence P. Wennogle (Hillsborough, NJ)
Assignee: INTRA-CELLULAR THERAPIES, INC.
A61K31/4985A61K9/0053A61K31/198A61K31/44A61K31/5383A61K45/06C07D471/14C07D498/14
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Quick Facts
Patent No.
US 10,702,522
App. No.
16/165,832
Granted
Jul 7, 2020
Kind
B2
Abstract

Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.

Claims (13)

1. A method for the treatment of one or more sleep disorders comprising administering to a patient in need thereof a Compound of Formula I:

wherein X is O, —NH— or N(CH 3 ); and Y is —O— or C(O)—, in free or pharmaceutically acceptable salt form, wherein the amount of said Compound of Formula I administered is from 0.1 mg to 20 mg, in free or pharmaceutically acceptable salt form, provided that in the case of a salt, the weight is calculated as the free base, wherein the patient does not have schizophrenia.

2. The method according to claim 1 , wherein the sleep disorder is sleep maintenance insomnia.

3. The method according to claim 1 , further comprising one or more therapeutic agents selected from the group consisting of compounds that modulate GABA, 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-I drug, an anti-depressant, and an antipsychotic agent e.g., in free or pharmaceutically acceptable salt form.

4. The method according to claim 1 , further comprising administering one or more therapeutic agents selected from the group consisting of modafinil, armodafinil, doxepin, alprazolam, bromazepam, clobazam, clonazepam, clorazepate, diazepam, flunitrazepam, flurazepam, lorazepam, midazolam, nitrazepam, oxazepam, temazepam, triazolam, indiplon, zopiclone, eszopiclone, zaleplon, Zolpidem, gabaxadol, vigabatrin, tiagabine, EVT 201, estazolam, ketanserin, risperidone, eplivanserin, volinanserin, pruvanserin, MDL 100907, HY10275, APD125, AVE8488, repinotan, sarizotan, eptapirone, buspirone, MN-305, melatonin, ramelteon, VEC-162, PD-6735, agomelatine, lamotrigine, gabapentin, pregabalin, orexin, a 1,3-biarylurea, SB-334867-a, GW649868, a benzamide derivative, Org 50081, ritanserin, nefazodone, serzone, trazodone, Casopitant, 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, velafaxine, chlorpromazine, haloperidol, droperidol, fluphenazine, loxapine, mesoridazine molidone, perphenazine, pimozide, prochlorperazine promazine, thioridazine, thiothixene, trifluoperazine, clozapine, aripiparazole, olanzapine, quetiapine, ziprasidone and paliperidone, in free or pharmaceutically acceptable salt form.

5. The method of claim 1 wherein the sleep disorder is insomnia in a patient suffering from depression.

6. The method of claim 1 wherein the sleep disorder is insomnia in a patient suffering from psychosis.

7. The method of claim 1 wherein the sleep disorder is insomnia in a patient suffering from Parkinsons disease.

8. The method of claim 1 wherein the Compound of Formula I is in the form of the tosylate salt.

9. The method of claim 2 wherein the Compound of Formula I is in the form of the tosylate salt.

10. The method of claim 5 wherein the Compound of Formula I is in the form of the tosylate salt.

11. The method of claim 6 wherein the Compound of Formula I is in the form of the tosylate salt.

12. The method of claim 7 wherein the Compound of Formula I is in the form of the tosylate salt.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2022
From: MATES, SHARON; FIENBERG, ALLEN A.; WENNOGLE, LAWRENCE P.
To: INTRA-CELLULAR THERAPIES, INC.
Reel/Frame 059652/0386 →
Continuity (7)
Continuation 15467867 · Mar 23, 2017
Continuation 14885813 · Oct 16, 2015
Continuation 14066987 · Oct 30, 2013
Division 12994560
Provisional Application 61155032 · Feb 24, 2009
Provisional Application 61056433 · May 27, 2008
Related Publication 20190183888A1 · Jun 20, 2019
Cited By (22)
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