DK2616068T3 - Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk - Google Patents

Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk Download PDF

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DK2616068T3
DK2616068T3 DK11760962.8T DK11760962T DK2616068T3 DK 2616068 T3 DK2616068 T3 DK 2616068T3 DK 11760962 T DK11760962 T DK 11760962T DK 2616068 T3 DK2616068 T3 DK 2616068T3
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ethyl
imidazol
methyl
acid
methylbenzyl ester
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Mohammed I Dibas
Ken Chow
John E Donello
Michael E Garst
Daniel W Gil
Liming Wang
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Allergan Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics

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  • Pharmacology & Pharmacy (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Claims (15)

1. Sammensætning omfattende en forbindelse med formlen I, dens individuelle enantiomerer, individuelle diastereoisomerer, hydrater, solvater, krystalformer, dens individuelle tautomerer eller et farmaceutisk acceptabelt salt deraf til anvendelse ved sænkning af intraokulært tryk i et berørt øje hos en human patient med behov for en sådan behandling ved administration af en terapeutisk effektiv mængde af sammensætningen;
Formel I hvor R1 er H eller Ci-3-alkyl; R2 er H eller Ci-3-alkyl; R3 er H; Ci-io-alkyl; en aromatisk eller ikke-aromatisk 5- til 10-leddet monocyklisk eller bicyklisk heterocyklus, der mindst indeholder ét heteroatom, der er udvalgt fra O eller N eller S eller kombinationer deraf; eller en monocyklisk eller bicyklisk C6-io-arylgruppe; og R er en ligekædet eller forgrenet Ci-io-alkylgruppe eventuelt substitueret med aminogrupper, arylgrupper og halogenatomer, og én methylengruppe kan erstattes af carbonyl, -NH-, carboxyl, amid, -S- eller -O-; en aromatisk eller ikke-aromatisk 5- til 10-leddet monocyklisk eller bicyklisk heterocyklus, der indeholder mindst ét heteroatom, der er udvalgt fra O eller N eller S eller kombinationer deraf, hvor heterocyklussen eventuelt er substitueret med Ci-e-alkyl, amino, halogen, -O(Ci-e-alkyl), -0C(0)(Ci-e-alkyl), -C(0)0(Ci-e-alkyl), -NHC(0)(Ci-e-alkyl), -C(0)NH(Ci-e-alkyl), -S(Ci-6-alkyl) grupper; eller en monocyklisk eller bicyklisk C6-io-arylgruppe eventuelt substitueret med Ci-6-alkyl, amino, halogen, -0(Ci-6-alkyl), -0C(0)(Ci-6-alkyl), -C(0)0(Ci-e-alkyl), -NHC(0)(Ci-e-alkyl), -C(0)NH(Ci-e-alkyl) eller -S(Ci-6-alkyl) grupper.
2. Sammensætning til anvendelse ifølge krav 1, hvor forbindelsen er af formlen II, dens individuelle diastereoisomerer, hydrater, solvater, krystalformer, individuelle tautomerer eller et farmaceutisk acceptabelt salt deraf,
Formel II hvor R1, R2, R3 og R er som defineret i krav 1
3. Sammensætning til anvendelse ifølge krav 1, hvor forbindelsen er af formlen III, dens individuelle diastereoisomerer, hydrater, solvater, krystalformer, individuelle tautomerer eller et farmaceutisk acceptabelt salt deraf,
Formel III hvor R1, R2, R3 og R er som defineret i krav 1.
4. Sammensætning til anvendelse ifølge krav 2, hvor R1 er Ci-3-alkyl, R2 er C1-3-alkyl, R3 er H og R er Ci-10-alkyl; eller hvor R1 er methyl, R2 er methyl, R3 er H og R er Ci-4-alkyl.
5. Sammensætning til anvendelse ifølge krav 2, hvor forbindelsen er udvalgt fra: iso-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2.2- dimethyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eddikesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; benzoesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-amino-3-methyl-smørsyre 3-[(S)-l-(lff-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester og 2- amino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eller hvor forbindelsen er udvalgt fra: iso-smørsyre 3-[(S)-l-(l-iso-butyryl-lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2.2- dimethyl-propionsyre 3-{(S)-l-[l-(2,2-dimethyl-propionyl)-lH-imidazol-4-yl]-ethyl>-2-methylbenzylester; eddikesyre 3-[(S)-l-(l-acetyl-lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; benzoesyre 3-[(S)-l-(l-benzoyl-lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3- methyl-smørsyre 2-methyl-3-{(S)-l-[l-(3-methyl-butyryl)-lH-imidazol- 4- yI]-ethyl}-benzylester; phenyl-propionsyre 2-methyl-3-{(S)-l-[l-(3-phenyl-propionyl)-lA/-imidazol-4-yl]-ethyl}-benzylester; 2-tert-butoxycarbonylamino-3-methyl-smørsyre 3-{(S)-l-[l-(2-tert-butoxy carbonylamino-3-methyl-butyryl)-lH-imidazol-4-yl]-ethyl}-2- methylbenzylester; 2-terf--butoxycarbonylamino-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-tert-butoxycarbonylamino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-{(S)-l-[l-(2-teri--butoxycarbonylamino-3-methyl-butyryl)-lH-imidazol-4-yl]-ethyl>-2-methylbenzylester; 2-(2-tert-butoxycarbonylamino-3-methyI-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-tert-butoxycarbonylamino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester og 2- fe/t-butoxycarbonylamino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester.
6. Sammensætning til anvendelse ifølge krav 1, hvor det berørte øje bevarer et intraokulært tryk på mindre end det intraokulære baselinetryk i mindst otte (8) timer; eller hvor det berørte øje bevarer et intraokulært tryk på mindre end det intraokulære baselinetryk i mindst ti (10) timer, eller hvor det berørte øje bevarer et intraokulært tryk på mindre end det intraokulære baselinetryk i mindst tolv (12) timer.
7. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen omfatter 0,0005 til 5 vægt-% af en forbindelse, der er udvalgt fra: iso-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2,2-dimethyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eddikesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; benzoesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3- methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester;
3-Phenyl-propionsyre 3-[(S)-l-(lAV-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-amino-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester og 2- amino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eller et farmaceutisk acceptabelt salt deraf; eller hvor sammensætningen omfatter 0,005 til 2 vægt-% af en forbindelse, der er udvalgt fra: iso-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methyl-benzyIester; 2.2- dimethyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eddikesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methyI-benzylester; benzoesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3- methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methyl-benzylester; 3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methyI-benzylester; 2-amino-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester og 2- amino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eller et farmaceutisk acceptabelt salt deraf.
8. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen omfatter 0,05 til 2 vægt-% af en forbindelse, der er udvalgt fra: iso-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2.2- dimethyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eddikesyre 3-[(S)-l-(lH-imidazoI-4-yl)-ethyl]-2-methylbenzylester; benzoesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methyI-benzylester; 3- methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-amino-3-methyl-smørsyre 3-[(S)-l-(lH-imidazoI-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazoI-4-yl)-ethyl]-2-methylbenzylester og 2-amino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eller et farmaceutisk acceptabelt salt deraf.
9. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen endvidere omfatter fra 0,001 til 1 vægt-% af et konserveringsmiddel.
10. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen endvidere omfatter fra 0,01 % til 0,5 vægt-% af et konserveringsmiddel.
11. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen endvidere omfatter fra 0,001 til 0,01 vægt-% af et konserveringsmiddel.
12. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen endvidere omfatter fra 0,01 til 1 vægt-% af et cosolvent.
13. Sammensætning til anvendelse ifølge krav 1, hvor sammensætningen endvidere omfatter fra 0,01 til 2 vægt-% af et viskositetsfremmende middel.
14. Farmaceutisk sammensætning til anvendelse ved sænkning af intraokulært tryk i et berørt øje hos et individ, hvilken sammensætning omfatter en forbindelse med en struktur
Formel II hvor R1, R2, R3 og R er som defineret i krav 1.
15. Farmaceutisk sammensætning ifølge krav 14, hvor er udvalgt fra: iso-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2,2-dimethyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; eddikesyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; benzoesyre 3-[(S)-l-(ltf-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-amino-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester; 2-(2-amino-3-methyl-butyrylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazo-4-yI)-ethyl]-2-methylbenzylester; 2-(2-amino-acetylamino)-3-methyl-smørsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester og 2-amino-3-phenyl-propionsyre 3-[(S)-l-(lH-imidazol-4-yl)-ethyl]-2-methylbenzylester.
DK11760962.8T 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk DK2616068T3 (da)

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US38337010P 2010-09-16 2010-09-16
PCT/US2011/051990 WO2012037490A1 (en) 2010-09-16 2011-09-16 Ester pro-drugs of [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for lowering intraocular pressure

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DK16161921.8T DK3078376T3 (da) 2010-09-16 2011-09-16 Ester-pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til behandling af nethindesygdomme
DK19194325.7T DK3636263T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl]-methanol
DK16161922.6T DK3053576T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk
DK11760962.8T DK2616068T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk
DK11760963.6T DK2616069T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol
DK16161923T DK3050564T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl]-methanol
DK18160174.1T DK3348264T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk
DK18157147.2T DK3338777T3 (da) 2010-09-16 2011-09-16 Ester-pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til behandling af nethindesygdomme
DK16161920.0T DK3050563T3 (da) 2010-09-16 2011-09-16 Ester-pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til behandling af hudsygdomme og -tilstande

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DK19194325.7T DK3636263T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl]-methanol
DK16161922.6T DK3053576T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk

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DK18160174.1T DK3348264T3 (da) 2010-09-16 2011-09-16 Ester pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til sænkning af intraokulært tryk
DK18157147.2T DK3338777T3 (da) 2010-09-16 2011-09-16 Ester-pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til behandling af nethindesygdomme
DK16161920.0T DK3050563T3 (da) 2010-09-16 2011-09-16 Ester-pro-drugs af [3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl] methanol til behandling af hudsygdomme og -tilstande

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