Methods and compositions for sleep disorders and other disorders 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
US2011071080 A1 2011-03-24 [US20110071080]US8598119 B2 2013-12-03 [US8598119] / 2011-03-242013-12-03
申请号/申请日
2009US-12994560 / 2009-05-27
发明人
MATES SHARON;FIENBERG ALLEN;WENNOGLE LAWRENCE;
申请人
INTRA CELLULAR THERAPIES;
主分类号
IPC分类号
A01N-043/00A01N-043/46A01N-043/58A01N-043/60A01N-043/62A01N-045/00A61K-031/495A61K-031/50A61K-031/535A61K-031/55A61K-031/56A61K-038/27A61P-005/06
摘要
(US8598119) 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.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2008US-61056433 2008-05-27 2009US-12994560 2009-05-27 2009US-61155032 2009-02-24 2009WO-US03261 2009-05-27
主权利要求
(US8598119) The invention claimed is: 1.  A method for the treatment of one or more 5-HT2A-related disorders, comprising administering to a patient in need thereof 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 a dose which selectively blocks the 5-HT2A receptor. 2. The method according to claim 1 wherein said one or more disorders is psychosis. 3. The method according to claim 1 wherein said one or more disorders is schizophrenia. 4. The method according to claim 1 wherein said one or more disorders is depression. 5. The method according to claim 1 wherein said patient is unable to tolerate the side effects of conventional antipsychotic drugs. 6. The method according to claim 5 wherein said antipsychotic drugs are selected from the group consisting of haloperidol, aripiparazole, clozapine, olanzapine, quetiapine, risperidone and zipasidone. 7. The method according to claim 1 wherein said one or more disorders is depression and said patient is a patient suffering from psychosis or Parkinson's disease. 8. The method according to claim 1 wherein said one or more disorders is sleep disorder and said patient is suffering from depression. 9. The method according to claim 1 wherein said one or more disorders is sleep disorder and said patient is suffering from psychosis. 10. The method according to claim 1 wherein said one or more disorders is sleep disorder and said patient is suffering from Parkinson's disease. 11. The method according to claim 1 wherein said one or more disorders is sleep disorder and said patient is suffering from depression and psychosis or Parkinson's disease. 12. The method according to claim 1 wherein at least one of the disorders is dyskinesia. 13. The method of claim 12 wherein the disorder is levodopa-induced dyskinesia in a patient suffering from Parkinson's disease. 14. The method according to claim 1, 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-1 drug, an anti-depressant, and an antipsychotic agent, in free or pharmaceutically acceptable salt form. 15. 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, 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. 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(CH3); and Y is  -- O --  or  -- C(O) -- , in free or pharmaceutically acceptable salt form, in an amount that selectively blocks the 5-HT2A receptor, such that it a) is sufficient to block said 5-HT2A receptor; and   b) either does not block, or minimally blocks the dopamine D2 receptor. 17. The method according to claim 16, wherein the sleep disorder is sleep maintenance insomnia. 18. The method according to claim 16, 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. 19. The method according claim 16, 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, 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. 20. The method according to claim 16, wherein the effective amount of the Compound of Formula I administered is 0.5-10 mg. 21. The method according to claim 16, wherein the amount of the Compound of Formula I administered is 2.5-5 mg. 22. The method according to claim 16, wherein the amount of the Compound of Formula I administered is less than 5 mg. 23. The method according to claim 16, wherein the amount of the Compound of Formula I administered is less than 2.5 mg. 24. The method of claim 16 wherein the sleep disorder is insomnia in a patient suffering from depression. 25. The method according to claim 1, further comprising administering one or more therapeutic agents selected from a group consisting of as L-dopa, co-careldopa, duodopa, stalova, symmetrel, benzotropine, biperiden, bromocryiptine, entacapone, pergolide, pramipexole, procyclidine, ropinirole, selegiline and tolcapone. 26. The method according to claim 16, further comprising administering one or more therapeutic agents selected from a group consisting of as L-dopa, co-careldopa, duodopa, stalova, symmetrel, benzotropine, biperiden, bromocryiptine, entacapone, pergolide, pramipexole, procyclidine, ropinirole, selegiline and tolcapone. 27. The method according to claim 1, wherein the compound of Formula I has the structure:   28. The method according to claim 1, wherein the dose of said Compound of Formula I is from 2.5 mg to 50 mg. 29. The method according to claim 16, wherein the compound of Formula I has the structure:
法律状态
(US8598119) LEGAL DETAILS FOR US2011071080  Actual or expected expiration date=2029-12-28    Legal state=ALIVE    Status=GRANTED     Event publication date=2009-05-27  Event code=US/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=US US12994560  Application date=2009-05-27  Standardized application number=2009US-12994560     Event publication date=2009-05-27  Event code=US/EXMR  Event type=Administrative notifications  USPTO Examiner Name Primary Examiner: CORDERO GARCIA, MARCELA M    Event publication date=2009-05-27  Event code=US/ART  Event type=Administrative notifications  USPTO Art Group  ART=1658     Event publication date=2009-05-27  Event code=US/SMALL  Event type=Administrative notifications  Appl Has Filed a Verified Statement of Micro to Small Entity Status Business Entity Status: SMALL    Event publication date=2009-05-27  Event code=US/AIA  Event type=Administrative notifications  First Inventor File Indicated:  AIA=No     Event publication date=2009-05-27  Event code=US/DK  Event type=Examination events  Attorney Docket Number Docket Nbr: IT-30-US    Event publication date=2009-05-27  Event code=US/CUST  Event type=Examination events  Attorney/Agent Customer Number Customer Nbr: 50446    Event publication date=2010-11-24  Event code=US/APE  Event type=Corrections  Preliminary amendments    Event publication date=2010-11-24  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2010-12-02  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2010-11-23  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNORS:MATES, SHARON FIENBERG, ALLEN A. WENNOGLE, LAWRENCE P. 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专利类型码
A1B2
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