DK2382013T3 - Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme - Google Patents

Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme Download PDF

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DK2382013T3
DK2382013T3 DK09798938.8T DK09798938T DK2382013T3 DK 2382013 T3 DK2382013 T3 DK 2382013T3 DK 09798938 T DK09798938 T DK 09798938T DK 2382013 T3 DK2382013 T3 DK 2382013T3
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Gilles Desmadryl
Christian Chabbert
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Claims (6)

1. Selektiv Histamin H4-receptorantagonist til anvendelse til behandling og/eller forebyggelse af mindst ét symptom på vestibulære sygdomme, hvor den selektive Histamin H4-receptorantagonist: har et KiH3 :KiH4-forhold på over 10:1 og er udvalgt fra gruppen bestående af: • 1 -[(5-chlor-1 H-benzimidazol-2-yl)carbonyl] -4-methylpiperazin, • l-[(5-chlor-lH-indol-2-yl)carbonyl]-4-methylpiperazin, • 4-((3R)-3-aminopyrrolidin-l-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[l,2-d]pyrimidin-2-ylamin, • cis-4-(Piperazin-l-yl)-5,6,7a,8,9,10,l 1,1 la-octahydrobenzofuro[2,3-h]quinazolin-2-amin, • 2-isobutyl-6-(3-(methylamino)azetidin-l -yl)pyrimidin-4-amin, • 2-isobutyl-6-((3r)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-cyclohexylmethyl-6-((3r)-3-(methylamino)pyrrolidin-lyl)pyrimidin-4-amin, • 2-(4-fhrorbenzyl)-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclopropyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-tert-butyl-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 2-isopropyl-6-(3 -(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-(cyclopropylmethyl)-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 6-(3 -(methylamino)azetidin-1 -yl)-2-(phenoxymethyl)pyrimidin-4-amin, • 2-cyclopropyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-tert-butyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-isopropyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 6-((3r)-3-(methylamino)pyrrolidin-l-yl)-2-(phenoxymethyl)pyrimidin-4-amin, • 6-(3 -aminoazetidin-1 -yl)-2-isobutylpyrimidin-4-amin, • 2-isobutyl-6-(3-methyl-3-(methylamino)azetidin-l-yl)-pyrimidin-4-amin, • 6-((3r)-3 -aminopyrrolidin-1 -yl)-2-isobutylpyrimidin-4-amin, • 2-cyclobutyl-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 2-cyclobutyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-cyclopentyl-6-(3-(methylamino)azetidin-l -yl)pyrimidin-4-amin, • 2-Cyclopentyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-(2,2-dimethylpropyl)-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-(2,2-dimethylpropyl)-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-(2-cyclopentylethyl)-6-((3R)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-cyclohexylmethyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclopropylmethyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-cyclohexyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclohexyl-6-((3R)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-(4-fluorbenzyl)-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • N4-(cyclopropyhnethyl)-6-[(3R)-3-(methylammo)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-[(3R)-3-(methylammo)pyrrolidin-l-yl]pyrimidin-2,4-diamintartrat, • N4-isobutyI-6-[(3R)-3-(mcthylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin • N-isobutyl-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-4-amin, • N-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)pynOlidin-l-yl]pyrimidin-4-amin, • N4-(2,2-dimethylpropyl)-6-[(4aR*,7aR*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl] pyrimidin-2,4 -diamin, • N4-cyclopropyl-6-[(4aR*,7aR*)-octahydro-6H-pyrTol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin • N4-cyclobutyl-6-[(4aR*,7aR*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • 6-(3-methylamino-azetidin-l-yl)-N4-(3,3,3-trifluor-propyl)-pyrimidin-2,4-diamin, • N4-cyclopropylmethyl-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-(3,3-dimethyl-butyl)-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-(3-fluor-benzyl)-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-cyclopentylmethyl-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-isobutyl-6-[3 -(methylamino)azetidin-l -yl]pyrimidin-2,4-diamin, • 6- [3 -(methylamino)azetidin-1 -yl] -N4-propyl-pyrimidin-2,4-diamin, • N4-(2-methoxybenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[(3R)-3-methylpiperazin-l-yl]pyrimidin-2,4-diamin, • N4-ethyl-6-(4-methylpiperazin-1 -yl)pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-(4-methylpiperazin-1 -yl)pyrimidin-2,4-diamin, • 6-[3-(methylamino)azetidin-l-yl]-N4-(2-methylbutyl)pyrimidin-2,4-diamin, • N4-(2,5-difluorbenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,3-difluorbenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-butyl-6-[3-(methylamino)azetidin-l -yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-(2-methylcyclopropyl)pyrimidin-2,4-diamin, • N4-isobutyl-6-(4 -methyl-1,4-diazepan-1 -yl)pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-(3-pynOlidin-l-yl-azetidin-l-yl)pyrimidin-2,4-diamin, • N4-bicyclo[l. 1.1 ]pent-l -yl-6-[(3R)-3-(methylamino)pyrrolidin-l -yl]pyrimidin-2,4-diamin, • 6- [3 -methyl-3 -(methylamino)azetidin-1 -yl] -N4-propylpyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-(hexahydropyrrol[l,2-a]pyrazin-2(lH)-yl)pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-(3-pyrrolidin-l-yl-azetidin-l-yl)pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(isopropylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(tert-butyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-(l-methylcyclopropyl)pyrimidin-2,4-diamin, • N4-(tert-butyl)-6-[(4aS*,7aS*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-piperazin-1 -ylpyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diaminhydrochlorid, • N4-(2,2-dimethylpropyl)-6-[(3aR*,7aS*)-octahydro-5H-pyrrol[3,2-c]pyridin-5-yl] pyrimidin-2,4 -diamin, • 6-piperazin-1 -yl-N4-propylpyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-[4aR,7aR]-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin- 2.4- diamin, • N4-(2,2-dimethylpropyl)-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin- 2.4- diamin, • N4-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-isopropyl-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • 4- [3 -(methylamino)azetidin-1 -yl] -6-(4-methylpiperidin-1 -yl)pyrimidin-2-amin, • N4-(cyclopentylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pymmdin-2,4-diamin, • N4-cyclobutyl-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-propylpyrimidin-2,4-diamin og • N4-ethyl-6-(4-methyl-1,4-diazepan-1 -yl)pyrimidin-2,4-diamin.
2. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge krav 1, hvor mindst et symptom på vestibulær sygdom er udvalgt fra gruppen bestående af vertigo, svimmelhed, ubalance og kvalme.
3. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge krav 1 eller 2, hvor vertigo er en benign paroksysmal vertigo eller familiær episodisk vertigo.
4. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor den vestibulære sygdom er udvalgt fra vestibulær neurit, anfald af Meniéres sygdom, endolymfatiske hydrops, perilymfatisk fistel, hovedtraume med vestibulære sygdomme, labyrintblødning, kronisk eller akut labyrintinfektion, svær labyrintisk, barotraume med vestibulære sygdomme, vestibulære syndromer efter autoimmun sygdom i det indre øre, vestibulær migræne, vestibulære syndromer efter kirurgiske behandlinger af mellemøret, endolymfatiske sæk eller cerebello-pontinvinkeltumorer, indre øre-kanalopatier, kronisk Meniéres sygdom, vestibulære schwannomer, presbyvestibulia og vestibulær ataksi.
5. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge et hvilket som helst af kravene 1 til 4 til administration via trommehinden eller til systemisk administration.
6. Farmaceutisk sammensætning, der omfatter en selektiv Histamin H4 receptorantagonist ifølge et hvilket som helst af kravene 1 til 5 til anvendelse til behandling og/eller forebyggelse af mindst ét symptom på vestibulære sygdomme.
DK09798938.8T 2008-12-24 2009-12-23 Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme DK2382013T3 (da)

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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.

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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
ES2946551T3 (es) 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina

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