DK2771320T3 - Cyclohexylaminer - Google Patents
Cyclohexylaminer Download PDFInfo
- Publication number
- DK2771320T3 DK2771320T3 DK12781549.6T DK12781549T DK2771320T3 DK 2771320 T3 DK2771320 T3 DK 2771320T3 DK 12781549 T DK12781549 T DK 12781549T DK 2771320 T3 DK2771320 T3 DK 2771320T3
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- DK
- Denmark
- Prior art keywords
- propyl
- oxy
- iodide
- dimethylcyclohexanaminium
- compound
- Prior art date
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
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- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C219/12—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C219/14—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a six-membered aromatic ring
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- C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
- C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
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- C07C2601/14—The ring being saturated
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Claims (18)
1. Forbindelse valgt fra gruppen bestående af: N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2- (benzoyloxy) propyl] -N, N-diethylcyclohexanaminium chlorid; N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2,6-dimethoxybenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-fluorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-chlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2-methylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-chlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((3-fluorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-fluor-2- (trifluormethyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((3- (trifluormethyl) benzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2- (trifluormethyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2-nitrobenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((3,5-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-ethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((4- (trifluormethyl) benzoyl) oxy) propyl] cyclohexanaminium iodid; (S) -N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; (S) -N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((3-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,6-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] tetrahydro-2H- pyran-4-aminium iodid; N- [2 - ((2,3-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((Cyclohexanecarbonyl) oxy) propyl] -N, N-diethylcyclohexanaminium iodid; N- [2 - ((3-Chlorbenzo [b] thiophen-2-carbonyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((thiophen-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((thiophen-3-carbonyl) oxy) propyl] cyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((1-methyl-1H-pyrrol-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((benzo [b] thiophen-2carbonyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N, 4-trimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((3-methylthiophen-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N, 4-trimethylcyclohexanaminium iodid; N, N, 4-trimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2,6-dimethylbenzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4,6-trimethylbenzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((4-methylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-ethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (S) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (S) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium bromid; (R) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium bromid; 1Cyclohexyl-1- [2 - ((2-isopropylbenzoyl) oxy) propyl] pyrrolidin 1 ium bromid; 1Cyclohexyl-1- [2 - ((2-isopropylbenzoyl) oxy) propyl] piperidin-1 ium bromid; 1 - [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -1 - cyclohexylpyrrolidin-1 ium bromid; 1- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -1-cyclohexylpiperidin-1 ium bromid; 1- [2 - ((3-Chlorbenzo [b] thiophen-2-carbonyl) oxy) propyl] -1-cyclohexylpyrrolidin-1-ium-bromid; og 1- [2 - ((3-Chlorbenzo [b] thiophen-2-carbonyl) oxy) propyl] -1 -cyclohexylpiperidin-1 -iumbromid.
2. Forbindelse ifølge krav 1 valgt fra gruppen bestående af: N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2- (benzoyloxy) propyl] -N, N-diethylcyclohexanaminium chlorid; N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2,6-dimethoxybenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-fluorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-chlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2-methylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-chlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((3-fluorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-fluor-2- (trifluormethyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((3- (trifluormethyl) benzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2- (trifluormethyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2-nitrobenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((3,5-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((4-ethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((4- (trifluormethyl) benzoyl) oxy) propyl] cyclohexanaminium iodid; (S) -N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; (S) -N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((3-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,6-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] tetrahydro-2H- pyran-4-aminium iodid; N- [2 - ((2,3-dichlorbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((Cyclohexanecarbonyl) oxy) propyl] -N, N-diethylcyclohexanaminium iodid; N- [2 - ((3-Chlorbenzo [b] thiophen-2-carbonyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((thiophen-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4-isopropylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((thiophen-3-carbonyl) oxy) propyl] cyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((1-methyl-1H-pyrrol-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((benzo [b] thiophen-2carbonyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,6-dimethylbenzoyl) oxy) propyl] -N, N, 4-trimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((3-methylthiophen-2-carbonyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N, 4-trimethylcyclohexanaminium iodid; N, N, 4-trimethyl-N- [2 - ((2,4,6-trimethylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((2,6-dimethylbenzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4,6-trimethylbenzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N, N-dimethyl-N- [2 - ((4-methylbenzoyl) oxy) propyl] cyclohexanaminium iodid; N- [2 - ((4- (tert-butyl) benzoyl) oxy) ethyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2-ethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; N- [2 - ((2,4-dimethylbenzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (S) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (R) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium iodid; (S) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium bromid; og (R) -N- [2 - ((4- (tert-butyl) benzoyl) oxy) propyl] -N, N-dimethylcyclohexanaminium bromid.
3. Sammensætning omfattende forbindelsen ifølge krav 1 eller 2.
4. Sammensætning ifølge krav 3 yderligere omfattende en TRPV1 receptor aktivator.
5. Sammensætningen ifølge krav 4, hvor TRPV1 receptor aktivator er valgt fra gruppen bestående af capsaicin, dihydrocapsaicin, nordihydrocapsaicin, lidocain, articain, procain, tetracain, mepivicaine, bupivicain, eugenol, kamfer, clotrimazol, N-arachidonoylvanillamine, anandamid, 2- aminoethoxydiphenyl borat, AM404, resiniferatoxin, phorbol 12-phenylacetat-13-acetat 20-homovanillate, olvanil, N-oleoyldopamine, N-arachidonyldopamine, 6'-iodoresiniferatoxin, en Ci8N-acylethanolamine, en lipoxygenase-derivat, nonivamid, en fed acyl amid afen tetrahydroisoquinolin inhibitor cystein-knude-peptid, N- [2- (3,4-dimethylbenzyl) -3-(pivaloyloxy) propyl] -2- [4- (2 -aminoethoxy) -3-methoxyphenyl] acetamid, N- [2- (3,4- dimethylbenzyl) -3- (pivaloyloxy) propyl] -N (4-hydroxy-3-methoxybenzyl) thiourinstof, hydroxy-a-sanshool, 2-aminoethoxydiphenyl borat, 10-shogaol, oleylgingerol, oleylshogaol, N- (4-tert-butylbenzyl) -N (4-hydroxy-3-methoxybenzyl) thiourinstof, aprindin, benzocain, butacain, kokain, dibucain, encainid, mexiletin, oxetacaine, prilocain, proparacain, procainamid, n-acetylprocainamide, chlorprocain, dyclonin, etidocain, levobupivacain, ropivacain, cyclomethycain, dimethocaine, propoxycain, trimecain, og sympocaine.
6. Sammensætningen ifølge krav 4, hvor TRPV1 receptor aktivator er lidocain.
7. Sammensætningen ifølge krav 4, som er formuleret til oral, intramuskulær, rektal, kutan, subkutan, topisk, transdermal, sublingual, nasal, vaginal, epidural, eller okulær administration til en patient.
8. Sammensætningen ifølge krav 4 omfattende mindst 0,2% af nævnte forbindelse eller fortrinsvis op til 5% af nævnte forbindelse eller 2% af nævnte TRPV1 receptor aktivator.
9. Forbindelse ifølge krav 1 eller 2 og en TRPV1 receptor aktivator til anvendelse ved behandling af smerte eller kløe hos en patient.
10. Forbindelse ifølge krav 1 eller 2 til anvendelse ved behandling af smerte eller kløe hos en patient.
11. Forbindelse ifølge krav 1 eller 2 til anvendelse i behandling overaktiv blære.
12. Forbindelse ifølge krav 1 eller 2 til anvendelse i behandling interstitiel cystitis.
13. Forbindelsen og TRPV1 receptor aktivator ifølge krav 9 til anvendelse ved behandling af smerte eller kløe, hvor TRPV1 receptor aktivator administreres før forbindelsen eller hvor TRPV1 receptor aktivator og forbindelsen administreres samtidig.
14. Forbindelsen og TRPV1 receptor aktivator ifølge krav 9 eller forbindelsen ifølge krav 10 til anvendelse ved behandling af smerte eller kløe, hvor smerten er neuropatisk smerte, inflammatorisk smerte, nociceptiv smerte, proceduremæssig smerte, eller hvor smerten er forårsaget af esophageal cancer, irritabelt tarmsyndrom, eller idiopatisk neuropati.
15. Forbindelsen og TRPV1 receptor aktivator ifølge krav 9 eller forbindelsen ifølge krav 10 til anvendelse ved behandling af smerte eller kløe, hvor administration er oral, intramuskulær, rektal, kutan, subkutan, topisk, transdermal, sublingual, nasal, vaginal, epidural, eller okulær.
16. Forbindelsen og TRPV1 receptor aktivator ifølge krav 9 til anvendelse ved behandling af smerte eller kløe, hvor forholdet mellem nævnte TRPV1 receptor aktivator til nævnte forbindelse er mindst ca. 4:1, og fortrinsvis hvor forholdet mellem nævnte TRPV1 receptor aktivator til forbindelsen er mellem 1:10 og 10:1.
17. Forbindelsen ifølge krav 11 eller krav 12 til anvendelse i behandling overaktiv blære eller interstitiel cystitis, hvor administration er a) via direkte instillation af forbindelsen i blæren eller urothelium, fortrinsvis indpodet som en lægemiddelopløsning, eller b) hvor forbindelsen er anbragt i nævnte blære eller urothelium som en udvidet release-formulering, fortrinsvis i form afen lægemiddelholdig reservoirer, et lægemiddel overtrukket materiale, et lægemiddel imprægneret materiale, eller en liposomal-lægemiddelformulering, eller c) hvor forbindelsen injiceres direkte ind i urinvejene.
18. Forbindelsen og TRPV1 receptor aktivator ifølge krav 9 til anvendelse ved behandling af smerte eller kløe, hvor TRPV1 receptor aktivator er valgt fra gruppen bestående af capsaicin, dihydrocapsaicin, nordihydrocapsaicin, lidocain, articain, procain, tetracain, mepivicaine, bupivicain, eugenol, kamfer, clotrimazol, N-arachidonoylvanillamine, anandamid, 2-aminoethoxydiphenyl borat, AM404, resiniferatoxin, phorbol 12-phenylacetat-13-acetat 20-homovanillate, olvanil, N-oleoyldopamine, N-arachidonyldopamine, 6'-iodoresiniferatoxin, en CisN-acylethanolamine, en lipoxygenase-derivat, nonivamid, en fed acyl-amid af en tetrahydroisoquinolin inhibitor cystein-knude-peptid, N- [2- (3,4-dimethylbenzyl) -3- (pivaloyloxy) propyl] -2- [4- (2 -aminoethoxy) -3-methoxyphenyl] acetamid, N- [2- (3,4-dimethylbenzyl) -3- (pivaloyloxy) propyl] -Ν'- (4-hydroxy-3-methoxybenzyl) thiourinstof, hydroxy-a-sanshool, 2-aminoethoxydiphenyl borat, 10-shogaol, oleylgingerol, oleylshogaol, N- (4-tert-butylbenzyl)-N '- (4-hydroxy-3-methoxybenzyl) thiourinstof, aprindin, benzocain, butacain, kokain, dibucain, encainid, mexiletin, oxetacaine, prilocain, proparacain, procainamid, n-acetylprocainamide, chlorprocain, dyclonin, etidocain, levobupivacain, ropivacain, cyclomethycain, dimethocaine, propoxycain, trimecain, og sympocain, og hvorTRPVI receptor aktivator fortrinsvis er lidocain.
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JP2017214376A (ja) | 2017-12-07 |
JP6835668B2 (ja) | 2021-02-24 |
JP6495654B2 (ja) | 2019-04-03 |
EP2771320A1 (en) | 2014-09-03 |
CA2853279A1 (en) | 2013-05-02 |
ES2596215T3 (es) | 2017-01-05 |
JP2015501320A (ja) | 2015-01-15 |
HUE032240T2 (en) | 2017-09-28 |
US8685418B2 (en) | 2014-04-01 |
US20140213552A1 (en) | 2014-07-31 |
WO2013063127A1 (en) | 2013-05-02 |
CA2853279C (en) | 2021-03-23 |
EP2771320B1 (en) | 2016-06-22 |
US20130101667A1 (en) | 2013-04-25 |
US9180115B2 (en) | 2015-11-10 |
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