Method 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
EP3085231 A1 2016-10-26 [EP3085231] / 2016-10-26
申请号/申请日
2016EP-0151760 / 2009-05-27
发明人
WENNOGLE LAUWRENCE P;MATES SHARON;
申请人
INTRA CELLULAR THERAPIES;
主分类号
IPC分类号
A01N-043/42A61K-031/44A61P-025/14A61P-025/18A61P-025/20A61P-025/24
摘要
(EP3085231) 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-HT 2A , SERT and/or dopamine D 2 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 2009EP-0755263 2009-05-27 2009US-61155032 2009-02-24
主权利要求
(EP3085231) 1. A Compound of Formula I: (see diagramm) wherein X is -NH or -N(CH 3); and Y is -0- or -C(O)-, in free or pharmaceutically acceptable salt form, in a dose which selectively antagonizes 5- HT2A receptors for the treatment of a disorder involving serotonin 5-HT2A, dopamine D2 and serotonin reuptake transporter (SERT) pathway. 2. The compound according to claim 1, wherein the compound of Formula I is selected from a group consisting of: (see diagramm)(see diagramm) in free or pharmaceutically acceptable salt form. 3. The compound according to any of claims 1-2 wherein said one or more disorders is  psychosis with a co-morbid disorder of depression and/or sleep disorder; schizophrenia, in a patient suffering from depression;  depression in a patient suffering from psychosis, e.g., schizophrenia, or depression in a patient suffering from anti-psychosis, or depression in a patient suffering from Parkinson's disease; or  a sleep disorder, such as sleep maintenance disorder. 4. The compound according to any of claims 1-2 wherein said one or more disorders is dyskinesia, or example levodopa-induced dyskinesia in a patient suffering from Parkinson's disease, or wherein said one or more disorders is bipolar depression or cognition associated with schizophrenia. 5. The compound according to any of claims 1-4, wherein said patient is unable to tolerate the side effects of conventional antipsychotic drugs. 6. The compound according to any of claims 1-4, wherein said one or more disorders is depression and said patient is a patient suffering from psychosis or Parkinson's disease. 7. The compound according to any of claims 1-3, wherein said one or more disorders is sleep disorder and said patient is suffering from depression, psychosis, or Parkinson's disease. 8. The compound according to any of claims 1-7 wherein X is -N(CH3); and Y is - C(O)-, in free or pharmaceutically acceptable salt form. 9. The compound according to any of claims 1-8, further comprising one or more therapeutic agents selected from an anti-depressant, an antipsychotic agent, another hypnotic agent, and/or an agent used to treat Parkinson's disease or mood disorders in free or pharmaceutically acceptable salt form. 10. The compound according to any of claims 1-9, further comprising one or more therapeutic agents selected from a group consisting 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, velafaxine, droperidol, fluphenazine, loxapine, mesoridazine molidone, perphenazine, pimozide, prochlorperazine promazine, thioridazine, thiothixene, trifluoperazine, clozapine, aripiparazole, olanzapine, quetiapine, risperidone, and ziprasidone, in free or pharmaceutically acceptable salt form. 11. The compound according to any preceding claim wherein the effective amount of a Compound of Formula I is 1-5mg. 12. The compound according to any of claims 1-2 wherein said one or more disorders is: psychosis, e.g., schizophrenia, in a patient suffering from depression; depression in a patient suffering from psychosis, e.g., schizophrenia; mood disorders associated with psychosis, e.g., schizophrenia, or Parkinson's disease; or sleep disorders associated with psychosis, e.g., schizophrenia, or Parkinson's disease, and wherein the effective amount of a Compound of Formula I is 2.5mg-50mg, e.g., 2.5mg, 5mg, 10mg, or 20mg. 13. A pharmaceutical composition comprising a Compound of Formula I in pharmaceutically acceptable salt form (such as the tosylate salt) in admixture with a pharmaceutically acceptable diluent or carrier. 14. A pharmaceutical composition in oral unit dose form comprising 2.5mg, 5mg or 10 mg of a Compound of Formula I: (see diagramm) wherein NH or -N(CH3); and Y is -0- 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.
法律状态
(EP3085231) LEGAL DETAILS FOR EP3085231  Actual or expected expiration date=2029-05-27    Legal state=ALIVE    Status=PENDING     Event publication date=2009-05-27  Event code=EP/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=EP EP16151760  Application date=2009-05-27  Standardized application number=2016EP-0151760     Event publication date=2016-10-26  Event code=EP/A1  Event type=Examination events  Application published with search report  Publication country=EP  Publication number=EP3085231  Publication stage Code=A1  Publication date=2016-10-26  Standardized publication number=EP3085231     Event publication date=2016-10-26  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR    Event publication date=2017-04-05  Event code=EP/RIN1  Event type=Change of name or address  Event type=Administrative notifications  Inventor (correction) Inventor changed before grant    Event publication date=2017-04-05  Event code=EP/RIN1  Event type=Change of name or address  Event type=Administrative notifications  Inventor (correction) Inventor changed before grant    Event publication date=2017-06-07  Event code=EP/17P  Event indicator=Pos  Event type=Examination events  Request for examination filed Pruefungsantrag gestellt  Effective date of the event=2017-04-26     Event publication date=2017-06-07  Event code=EP/RBV  Event indicator=Pos  Event type=Designated states  Event type=Corrections  Designated contracting states (correction): Benannte vertragsstaaten (korr.) AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR MEMBER STATE LEGAL DETAILS FOR EP2320731  Actual or expected expiration date=2017-04-19    Legal state=DEAD    Status=REVOKED   Corresponding cc:  Designated or member state=EP Corresponding appl: EP09755263  Application date in the designated or member state=2009-05-27   Application number in the designated or member state=2009EP-0755263 Corresponding cc:  Designated or member state=EP Corresponding pat: EP2320731  Publication stage code in the designated or member state=A1  Publication date in the designated or member state=2011-05-18   Publication number in the designated or member state=EP2320731    Event publication date=2016-10-26  Event code=EP/AC  Event type=Examination events  Divisional application (art. 76) of: Corresponding cc:  Designated or member state=EP     Event publication date=2017-08-30  Event code=EP/STCHG  Patent status changed by the national office Corresponding cc:  Designated or member state=EP  MEMBER STATE LEGAL DETAILS FOR HK  Actual or expected expiration date=2029-05-27    Legal state=ALIVE    Status=PENDING   Corresponding cc:  Designated or member state=HK Corresponding appl: HK1230864    Event publication date=2017-12-15  Event code=EP/REG  Event code=HK/DE  Event type=Examination events  Reference to a national code Requests to designate patent in hong kong Requests to record published in hong kong Corresponding cc:  Designated or member state=HK
专利类型码
A1
国别省市代码
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