Arachidonic acid analogs and methods for analgesic treatment using same 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
EP2504311 B1 2015-08-12 [EP2504311]EP2504311 A1 2012-10-03 [EP2504311] / 2015-08-122012-10-03
申请号/申请日
2010EP-0796199 / 2010-11-24
发明人
FALCK JOHN R;BROSTROM LANE;
申请人
CYTOMETIX;
主分类号
IPC分类号
A61K-031/16A61K-031/164A61K-031/17A61P-029/00C07C-233/09C07C-237/22C07C-275/20
摘要
(EP2504311) The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments.  Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described.  Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.  (From US9096494 B2)
机翻摘要
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地址
代理人
代理机构
;
优先权号
2009US-61264434 2009-11-25 2010WO-US58041 2010-11-24
主权利要求
(EP2504311) 1. A compound having the structure: (see diagramm) wherein: R 1 is H, or a C 1-C 6 alkyl, C 2-C 6 alkenyl, C 3-C 6 cycloalkyl or C 3-C 6 cycloalkenyl which is unsubstituted or substituted with at least one hydroxyl group; and R 2 is H, or a C 1-C 3 allcyl; or R 1 and R 2 form a C 3-C 6 heterocyclic ring with the nitrogen bonded to said R 1 and R 2; R 3 is (see diagramm) in which: R 4 is H, or a C 1-C 6 alkyl, C 2-C 6 alkenyl, C 3-C 6 cycloalkyl or C 3-C 6 cycloalkenyl; R 5 is a C 1-C 6 alkyl, C 1-C 6 alkoxy, or C 2-C 6 alkyl ether which is unsubstituted or substituted with one or more of hydroxyl, phenyl, phenyloxy, or fluorine, or R 5 is NR 7R 8, or C(O)NR 7R 8 in which R 7 and R 8 are independently selected from H, a C 1-C 6 alkyl, C 2-C 6 alkenyl, C 3-C 6 cycloalkyl, or C 3-C 6 cycloalkenyl group; R 6 is H, or a C 1-C 6 alkyl, C 2-C 6 alkenyl, C 3-C 6 cycloalkyl, or C 3-C 6 cycloalkenyl group; and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof. 2. The compound according to claim 1, wherein R 3 is (see diagramm) 3. The compound according to any one of claims 1 or 2, wherein R 5 is a linear C 5 alkyl group. 4. The compound according to any one of claims 1-3, wherein R 1 is a cyclopropyl group and R 2 is H. 5. The compound according to any one of claims 1-4, wherein R 4 is a C3 isopropyl group. 6. The compound according to any one of claims 1-5, wherein n is 1. 7. The compound according to claim 1, wherein the compound has the structure: (see diagramm) 8. The compound according to claim 1, wherein the compound has a structure selected from the group consisting of: (see diagramm) 9. A compound having a structure selected from the group consisting of: (see diagramm) ; and 10. A composition comprising a compound according to any one of claims 1-9 and a pharmaceutically acceptable carrier. 11. The composition of claim 10, wherein said composition is in the form of an injectable dosage, an oral dosage, an oil-in-water emulsion, or an anhydrous emulsion. 12. The composition of claim 10, wherein said composition comprises a cyclodextrin. 13. The composition of claim 10, further comprising an anesthetic agent. 14. A kit for providing analgesia to a subject, comprising a compound according to any one of claims 1-9 and a delivery device to administer said compound to the subject. 15. Use of a compound according to any one of claims 1-9 for the manufacture of a medicament for providing analgesia in a subject. 16. A compound according to any one of claims 1-9 for use in providing analgesia in a subject. 17. Use of a compound according to any one of claims 1-9 for the manufacture of a medicament for reducing fever in a subject. 18. A compound according to any one of claims 1-9 for use in reducing fever in a subject. 19. A method of providing an arachidonic acid (AA) analog, comprising the steps of : (see diagramm) 20. A method of providing an arachidonic acid (AA) analog, comprising the steps of : (see diagramm)
法律状态
(EP2504311) LEGAL DETAILS FOR EP2504311  Actual or expected expiration date=2030-11-24    Legal state=ALIVE    Status=GRANTED     Event publication date=2010-11-24  Event code=EP/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=EP EP10796199  Application date=2010-11-24  Standardized application number=2010EP-0796199     Event publication date=2012-10-03  Event code=EP/A1  Event type=Examination events  Application published with search report  Publication country=EP  Publication number=EP2504311  Publication stage Code=A1  Publication date=2012-10-03  Standardized publication number=EP2504311     Event publication date=2012-10-03  Event code=EP/17P  Event indicator=Pos  Event type=Examination events  Request for examination filed Pruefungsantrag gestellt  Effective date of the event=2012-06-14     Event publication date=2012-10-03  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AL 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 RS SE SI SK SM TR    Event publication date=2013-03-06  Event code=EP/DAX  Event indicator=Neg  Event type=Designated states  Request for extension of the european patent (to any country) deleted    Event publication date=2014-01-08  Event code=EP/17Q  Event indicator=Pos  Event type=Examination events  First examination report Erster pruefungsbescheid  Effective date of the event=2013-12-09     Event publication date=2015-04-01  Event code=EP/INTG  Event indicator=Pos  Event type=Examination events  Announcement of intention to grant  Effective date of the event=2015-03-04     Event publication date=2015-04-01  Event code=EP/RAP1  Event type=Change of name or address  Event type=Reassignment  Transfer of rights of an EP application Anmelder uebertragung (korr.) 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专利类型码
B1A1
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