HRP20161290T1 - Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja - Google Patents

Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja Download PDF

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HRP20161290T1
HRP20161290T1 HRP20161290TT HRP20161290T HRP20161290T1 HR P20161290 T1 HRP20161290 T1 HR P20161290T1 HR P20161290T T HRP20161290T T HR P20161290TT HR P20161290 T HRP20161290 T HR P20161290T HR P20161290 T1 HRP20161290 T1 HR P20161290T1
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pyrimidin
methylamino
diamine
azetidin
amine
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Gilles Desmadryl
Christian Chabbert
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INSERM (Institut National de la Santé et de la Recherche Médicale)
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Claims (6)

1. Selektivni antagonist histaminskih H4 receptora za uporabu u liječenju i /ili prevenciji najmanje jednog od simptoma vestibularnih poremećaja, naznačen time što selektivni antagonist histaminskih H4 receptora: - ima KiH3:KiH4 odnos iznad 10:1, i - izabran je iz grupe koja se sastoji od: • -1- [(5-kloro-1H-benzimidazol-2-il)karbonil]-4-metilpiperazin, • 1-[(5-kloro-1H-indol-2-il) karbonil]-4-metilpiperazin, • 4-((3R)-3-Aminopirolidin-1-il)-6,7-dihidro-5H-benzo[6,7]ciklohepta[1,2-d]pirimidin-2-ilamin, • cis-4-(Piperazin-1-il)-5,6,7a,8,9,10,11,11a-oktahidrobenzofuro[2,3-h] kinazolin-2-amin, • 2-Izobutil-6-(3-(metilamino)-azetidin-1-il)pirimidin-4-amin, • 2-Izobutil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksilmetil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(4-Fluorobenzil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopropil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-terc-Butil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Izopropil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-(Ciklopropilmetil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 6-(3-(Metilamino)azetidin-1-il)-2-(fenoksimetil)pirimidin-4-amin, • 2-Ciklopropil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-terc-Butil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Izopropil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 6-((3R)-3-(Metilamino)pirolidin-1-il)-2-(fenoksimetil)pirimidin-4-amin • 6-(3-Aminoazetidin-1-il)-2-izobutilpirimidin-4-amin • 2-Izobutil-6-(3-metil-3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 6-((3R)-3-aminopirolidin-1-il)-2-izobutilpirimidin-4-amin, • 2-Ciklobutil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklobutil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Ciklopentil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopentil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(2,2-Dimetilpropil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-(2,2-Dimetilpropil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(2-Ciklopentiletil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksilmetil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopropilmetil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Cikloheksil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(4-Fluorobenzil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin tartarat, • N4-Izobutil-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N-Izobutil-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-4-amin, • N-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-4-amin, • N4-(2,2-Dimetilpropil)-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-Ciklopropil-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-Ciklobutil-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-(3-Metilamino-azetidin-1-il)-N4-(3,3,3-trifluoro-propil)-pirimidin-2,4-diamin, • N4-Ciklopropilmetil-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-(3,3-Dimetil-butil)-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-(3-Fluoro-benzil)-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-Ciklopentilmetil-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-Izobutil-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-[3-(Metilamino)azetidin-1-il]-N4-propil-pirimidin-2,4-diamin, • N4-(2-Metoksibenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(3R)-3-metilpiperazin-1-il]pirimidin-2,4-diamin, • N4-Etil-6-(4-metilpiperazin-1-il)pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-(4-metilpiperazin-1-il)pirimidin-2,4-diamin, • 6-[3-(Metilamino)azetidin-1-il]-N4-(2-metilbutil)pirimidin-2,4-diamin, • N4-(2,5-Difluorobenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(2,3-Difluorobenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-Butil-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-(2-metilciklopropil)pirimidin-2,4-diamin, • N4-Izobutil-6-(4-metil-1,4-diazepam-1-il)pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-(3-pirolidin-1-il-azetidin-1-il)pirimidin-2,4-diamin, • N4-Biciklo[1.1.1]pent-1-il-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • 6-[3-Metil-3-(metilamino)azetidin-1-il]-N4-propilpirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-(heksahidropirolo[1,2-a]pirazin-2(1H)-1-il)pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-(3-pirolidin-1-il-azetidin-1-il)pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(izopropilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(terc-Butil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-(1-metilciklopropil)pirimidin-2,4-diamin, • N4-(terc-Butil)-6-[(4aS*,7aS*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-piperazin-1-ilpirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin hidroklorid, • N4-(2,2-Dimetilpropil)-6-[(3aR*,7aS*)-oktahidro-5H-pirolo[3,2-c]piridin-5-il]pirimidin-2,4-diamin, • 6-Piperazin-1-il-N4-propilpirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[4aR,7aR]-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-izopropil-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • 4-[3-(Metilamino)azetidin-1-il]-6-(4-metilpiperidin-1-il)pirimidin-2-amin, • N4-(Ciklopentilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-Ciklobutil-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-propilpirimidin-2,4-diamin i • N4-Etil-6-(4-metil-1,4-diazepan-1-il)pirimidin-2,4-diamin.
2. Selektivni antagonist histaminskih H4 receptora za uporabu prema patentnom zahtjevu 1, pri čemu je najmanje jedan od spomenutih simptoma vestibularnih poremećaja izabran iz grupe koju čine vertigo, vrtoglavice, poremećaj ravnoteže i mučnina.
3. Selektivni antagonist histaminskih H4 receptora za uporabu prema patentnom zahtjevu 1 ili 2, gdje je vrtoglavica benigna paroksizmalna vrtoglavica ili obiteljska epizodična vrtoglavica.
4. Selektivni antagonist histaminskih H4 receptora za uporabu prema bilo kojem od patentnih zahtjeva 1 do 3, pri čemu je spomenuti vestibularni poremećaj izabran od vestibularnog neuritisa, nastupa Meniereove bolesti, endolimfatičnog hidropsa, perilimfatične fistule, povreda glave s vestibularnim poremećajima, krvarenja labirinta, kronične ili akutne labirintne infekcije, seroznog labirinta, barotraumatizma s vestibularnim poremećajima, vestibularnih sindroma nakon autoimune bolesti unutrašnjeg uha, vestibularne migrene, vestibularnih sindroma nakon kirurškog tretmana srednjeg uha, endolimfatične vrećice ili tumora pontocerebelarnog kuta, kanalopatija unutrašnjeg uha, kronične Menierove bolesti, vestibularnih švanoma, presbivestibulia i vestibularne ataksije.
5. Selektivni antagonist histaminskih H4 receptora za uporabu prema bilo kojem od patentnih zahtjeva 1 do 4, za primjenu preko bubnjića ili za sistemsku primjenu.
6. Farmaceutska kompozicija koja sadrži selektivni antagonist histaminskih H4 receptora prema bilo kojem od patentnih zahtjeva 1 do 5, za uporabu u liječenju i/ili prevenciji najmanje jednog od simptoma vestibularnih poremećaja.
HRP20161290TT 2008-12-24 2016-10-06 Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja HRP20161290T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20080306013 EP2201982A1 (en) 2008-12-24 2008-12-24 Histamine H4 receptor antagonists for the treatment of vestibular disorders
PCT/EP2009/067897 WO2010072829A1 (en) 2008-12-24 2009-12-23 Selective histamine h4 receptor antagonists for the treatment of vestibular disorders.
EP09798938.8A EP2382013B1 (en) 2008-12-24 2009-12-23 Selective histamine h4 receptor antagonists for the treatment of vestibular disorders.

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US (2) US9526725B2 (hr)
EP (3) EP2201982A1 (hr)
JP (2) JP5814126B2 (hr)
KR (1) KR101749285B1 (hr)
CN (2) CN107050030A (hr)
CA (1) CA2748159C (hr)
CY (1) CY1118106T1 (hr)
DK (1) DK2382013T3 (hr)
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PL (1) PL2382013T3 (hr)
PT (1) PT2382013T (hr)
RU (1) RU2589846C2 (hr)
SI (1) SI2382013T1 (hr)
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HUE039713T2 (hu) * 2012-06-08 2019-02-28 Sensorion H4 receptor inhibitorok tinnitus kezelésére
CN105017385B (zh) * 2015-07-02 2018-08-03 吉林大学 基于模拟人组胺受体4（hr4）表位的疫苗及其构建方法
CN111465602B (zh) 2017-10-17 2023-05-23 帕劳制药有限公司 4-氨基嘧啶化合物的合成

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