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Method for treating pruritus and/or itch

A composition and medicine technology, applied in the field of treating pruritus and/or pruritus, can solve the problem that pruritus does not have symptomatic benefits and the like

Inactive Publication Date: 2019-06-04
NEURIM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in a recent study, topical administration of a TRPV1 antagonist had no symptomatic benefit in humans on histaminergic or non-histaminergic-induced pruritus (Gibson, Robertson et al., 2014)

Method used

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  • Method for treating pruritus and/or itch
  • Method for treating pruritus and/or itch
  • Method for treating pruritus and/or itch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Synthesis of N-[2-(1H-indol-3-yl)-ethyl]-cymanamide

[0071]

[0072] Reaction Scheme for the Synthesis of N-[2-(1H-Indol-3-yl)-Ethyl]-Permanamide

[0073]

[0074] a: DME, Py, TEA, DCC, NHS

[0075] General Procedures for the Synthesis of N-[2-(1H-Indol-3-yl)-Ethyl]-Pyramide

[0076] In a four-neck round bottom flask (100 mL), tryptamine (0.85 g, 5.3 mmol)) was dissolved in DME (40 mL) and Py (0.9 mL) was added. The mixture was stirred at room temperature for 30 minutes, then added manic acid (0.68g, 4.8mmol), then NHS (0.61g, 5.3mmol), DCC (1.1g, 5.3mmol), TEA (0.7mL, 56.1mmol); The mixture was stirred overnight then checked by LC-MS. The brown suspension was filtered on Gooch and the solid was washed with water (100 mL). CH for aqueous phase 2 Cl 2 (3X100mL), washed with brine (2x10mL), washed with MgSO 4 Dry, filter and evaporate under reduced pressure. The resulting sticky solid was suspended and stirred in MTBE (20 mL) for 30 minutes. The solid was ...

Embodiment 2

[0083] Synthesis of N-[2-(5-Methoxy-Indol-3-yl)-Ethyl]-Karmanamide

[0084]

[0085] Reaction Scheme for the Synthesis of N-[2-(5-Methoxy-Indol-3-yl)-Ethyl]-Cymanamide

[0086]

[0087] i.DMF, HOBt, 1.1 equivalents, EDC 1.1 equivalents, NEt3 2.5 equivalents, room temperature, 6h

[0088] General steps for the synthesis of N-[2-(5-methoxy-indol-3-yl)-ethyl]-almanamide

[0089] Under an argon atmosphere, a 100 ml three-neck round bottom flask was filled with comanic acid (500 mg, 1 eq) and 5-methoxytryptamine (760 mg, 1.1 eq), dissolved in DMF (25 ml), and passed The ice bath was adjusted to 0 °C. Then HOBt (1-hydroxybenzotriazole monohydrate, 530 mg, 1.1 equivalents), EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) were added under magnetic stirring salt, 750 mg, 1.1 eq) and triethylamine (1.25 ml, 2.5 eq). The mixture was stirred at 0 °C for another 15 minutes and then allowed to react at room temperature for 6 h. The course of the reaction was fol...

Embodiment 3

[0095] Synthesis of [2-(5-methoxy-1H-indol-3-yl)ethyl]carbamate 2-methyl-4-oxo-4H-pyran-3-yl ester:

[0096]

[0097] Reaction scheme for the synthesis of 2-methyl-4-oxo-4H-pyran-3-yl [2-(5-methoxy-1H-indol-3-yl)ethyl]carbamate

[0098]

[0099] a: triethylamine, triphosgene, CH 2 Cl 2 , at 10°C for 2h

[0100] 1: 2-methyl-4-oxo-4H-pyran-3-yl [2-(5-methoxy-1H-indol-3-yl)ethyl]carbamate

[0101] To 5-methoxytryptamine hydrochloride (1g, 0.0044mol) in CH 2 Cl 2 To the suspension in (7ml) was added triethylamine (1.8ml, 0.0132mol) and the mixture was stirred at room temperature for 30 minutes. After adding maltol (0.5 g, 0.0044 mol), the reaction mixture was cooled in an ice-water bath, then triphosgene (0.4 g, 0.0015 mol) was added in CH 2 Cl 2 (1 ml), keeping the temperature below 10°C, and stirring at the same temperature for 2h. The mixture was evaporated under reduced pressure to give an oily residue which was purified by flash chromatography (EtOAc-Cy, 80:20 t...

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Abstract

The invention relates to a medicament for treating pruritus and itch in a patient suffering from dermatological and non-dermatological conditions leading to such symptoms, which comprises at least onecompound selected from a pyrone-indole derivative, in an effective amount, and optionally one or more other therapeutically active agents.

Description

[0001] Cross References to Related Applications [0002] This application claims the filing date benefit of Provisional Patent Application Serial No. 62 / 378,435, filed August 23, 2016, the disclosure of which is hereby incorporated by reference in its entirety under 35 U.S.C. § 119(e). technical field [0003] The present invention generally relates to the treatment of pruritus and / or itching (itch), the use of pyrone-indole compounds in the preparation of medicaments for the treatment of pruritus and / or itching, and the relief of Drugs for pruritus or pruritus in patients with dermatological and non-dermatological conditions of pruritus. Background technique [0004] Itching is an uncomfortable sensation on the skin that induces the desire to scratch (Bautista, Wilson et al., 2014). Pruritus, defined as a sensation prompting an urgency to scratch, can be acute (<6 weeks) or chronic (>6 weeks) (Lavery, Stull et al., 2016). This symptom can significantly impair the qu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/351A61K31/4045A61P17/04
CPCA61K31/351A61K31/4045A61P17/04A61K31/404A61K9/0014A61K9/06A61K47/44A61K45/06A61K9/0031A61K9/0019A61K9/006A61K9/0073A61K9/08A61K9/12A61K9/122A61K9/107A61K47/26A61K47/36A61K47/38A61K47/22A61K47/24A61K47/46
Inventor M.劳顿
Owner NEURIM PHARMA
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