Nk1-antagonist combination and method for treating synucleinopathies

一种共核蛋白、拮抗剂的技术，应用在共核蛋白病领域，达到减缓症状进展、延迟发作的效果

Pending Publication Date: 2020-01-24
TALENT THERAPY CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0055] Therefore, the problem of providing safe, long-term, effective treatment with pramipexole for patients with synucleinopathies remains unresolved

Method used

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  • Nk1-antagonist combination and method for treating synucleinopathies
  • Nk1-antagonist combination and method for treating synucleinopathies
  • Nk1-antagonist combination and method for treating synucleinopathies

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Experimental program
Comparison scheme
Effect test

Embodiment approach

[0184] According to one embodiment, said 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine is selected from:

[0185] -(S)-6-Propylamino-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine (INN: pramipexole) and its pharmaceutically acceptable salts, especially is its dihydrochloride monohydrate (USAN: pramipexole hydrochloride), the dosage / unit form is equivalent to 0.125mg to 45mg, preferably 0.125mg to 40-42mg pramipexole dihydrochloride monohydrate, with Equivalent to 0.375 mg to 45 mg, preferably greater than 6 mg to 45 mg or 6.5 mg to 45 mg, usually 0.375 mg to 40-42 mg, preferably greater than 6 mg to 40-42 mg or 6.5 mg to 40-42 mg pramipexole dihydrochloride monohydrate daily dose administration;

[0186] -(R,S)-6-Propylamino-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine (racemate) and its pharmaceutically acceptable salts, Dosage / unit form is from 0.25mg to 90mg, preferably greater than 12mg to 90mg, usually 0.25mg to 80mg, said dosage comprises the equivalent of 0.12...

Embodiment 1

[0279] The ability of NK1-antagonists to prevent the adverse effects of 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine in humans was tested.

[0280] A Phase I study was conducted in subjects receiving oral doses of pramipexole dihydrochloride monohydrate ("pramipexole") with or without aprepitant. The study was a single-center, single-blind, placebo-controlled study.

[0281] The purpose of this study was to demonstrate that aprepitant can safely alleviate the gastrointestinal side effects of pramipexole at therapeutic and even supratherapeutic doses.

[0282] To enroll in the study, participants (ages 18 to 60) must be in good health during the study period, refrain from drinking beverages containing xanthines, quinine and caffeine, and refrain from prolonged periods of intense physical activity. All subjects signed an informed consent form, indicating that they understood the purpose of the study and the procedures required for the study, and were willing to par...

Embodiment 2

[0299] A Phase I study was conducted in subjects who received a single oral dose of pramipexole dihydrochloride monohydrate ("pramipexole") with or without a single oral dose of aprepitant. The study was a single-center, single-blind study.

[0300] The purpose of this study was to demonstrate that aprepitant can safely relieve pramipexole given at doses equal to or higher than those approved in the treatment of Parkinson's disease or shown to be effective in the treatment of depression in clinical trials gastrointestinal side effects.

[0301] To enroll in the study, participants must meet the following key inclusion / exclusion criteria:

[0302] key inclusion criteria

[0303] 1. Include male and female subjects aged 20-45 years (inclusive).

[0304] 2. Females of childbearing potential must agree to abstain from alcohol or otherwise use the following two medically acceptable forms of contraception from the screening period until 14 days after the study withdrawal visit: c...

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Abstract

The present invention describes the use of a NK1-antagonist, in combination with 6- propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to facilitate the treatment of a patient suffering from asynucleinopathy by enabling a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose to act without the typical adverse effects caused by pramipexole dihydrochloride monohydrate when administered alone.

Description

[0001] related application [0002] This application claims the benefit of US Provisional Patent Application Serial No. 62 / 483,555, filed April 10, 2017, the disclosure of which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to the field of treatment of synucleinopathies, ie neurodegenerative diseases of the human central nervous system, and in particular to the treatment of neurotoxic processes due to oligomerization and aggregation of alpha-synuclein. [0004] Purpose of the invention [0005] The present invention relates to pharmaceutical combinations (including fixed dose combinations) comprising 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine or a pharmaceutically acceptable salt thereof or solvates and neurokinin receptor subtype 1 antagonists ("NK1-antagonists"), and their use for the treatment of synucleinopathies, in particular for the treatment of blood plasma exosomes / total α-co- CNS neurot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/438A61K31/445A61K31/4747C07D401/00C07D401/02C07D403/04
CPCA61K31/428A61K31/438A61K31/5377A61K45/06C07D277/82C07D413/06A61P25/16A61P25/28A61K31/675A61P25/00A61K2300/00A61P1/08
Inventor T·N·蔡斯K·E·克拉伦斯-史密斯
Owner TALENT THERAPY CO
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