Claims for Patent: 9,168,258

Summary for Patent: 9,168,258

Title:	Methods and compositions for sleep disorders and other disorders
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.
Inventor(s):	Sharon Mates, Allen Fienberg, Lawrence P. Wennogle
Assignee:	Intra Cellular Therapies Inc
Application Number:	US14/066,987
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,168,258
Patent Claims:	1. A pharmaceutical composition in oral unit dose form comprising an amount of 10 mg or less of a Compound of Formula I: wherein X is O, —NH or —N(CH3); and Y is —O— or —C(O)—, in free or pharmaceutically acceptable salt form, in combination or association with a pharmaceutically acceptable diluent or carrier, provided that in the case of a salt, the weight is calculated as the free base, where the amount of the Compound of Formula I: a) is sufficient to block the 5-HT2A receptor; and b) either does not block, or minimally blocks the dopamine D2 receptor. 2. The pharmaceutical composition according to claim 1 wherein the oral unit dose form is a tablet. 3. The pharmaceutical composition according to claim 1 wherein the oral unit dose form is a capsule. 4. The pharmaceutical composition according to claim 1 wherein the amount of Compound of Formula I is 5 mg. 5. The pharmaceutical composition according to claim 1 wherein the amount of Compound of Formula I is 2.5 mg. 6. The pharmaceutical composition according to claim 1 wherein the Compound of Formula I is in free or pharmaceutically acceptable salt form. 7. The pharmaceutical composition according to claim 6 wherein the Compound of Formula I is in the form of the tosylate salt. 8. The pharmaceutical composition according to claim 6 wherein the amount of Compound of Formula I is 2.5 mg. 9. The pharmaceutical composition according to claim 6 wherein the amount of Compound of Formula I is 3 mg. 10. The pharmaceutical composition according to claim 6 wherein the amount of Compound of Formula I is 4 mg. 11. The pharmaceutical composition according to claim 6 wherein the amount of Compound of Formula I is 5 mg. 12. The pharmaceutical composition according to claim 6 wherein the amount of Compound of Formula I is 10 mg. 13. The pharmaceutical composition according to claim 1 wherein the Compound of Formula I is in the form of the tosylate salt. 14. The pharmaceutical composition according to claim 6, further comprising one or more therapeutic agents selected from the group consisting of compounds that modulate GABA activity, a GABAB 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, in free or pharmaceutically acceptable salt form. 15. The pharmaceutical composition according to claim 6, further comprising 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, temazapam, 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, risperidone, ziprasidone and paliperidone, in free or pharmaceutically acceptable salt form. 16. The pharmaceutical composition according to claim 6, further comprising one or more therapeutic agents selected from the group consisting of L-dopa, co-careldopa, duodopa, stalova, symmetrel, benzotropine, biperiden, bromocryiptine, entacapone, pergolide, pramipexole, procyclidine, ropinirole, selegiline and tolcapone. 17. The pharmaceutical composition according to claim 15 wherein the amount of Compound of Formula I is 2.5 mg. 18. The pharmaceutical composition according to claim 15 wherein the amount of Compound of Formula I is 5 mg. 19. The pharmaceutical composition according to claim 16 wherein the amount of Compound of Formula I is 2.5 mg. 20. The pharmaceutical composition according to claim 16 wherein the amount of Compound of Formula I is 5 mg.