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Application of GLN-1062 salt in the preparation of drug for treating brain diseases related to cognitive disorders

一种认知障碍、药物的技术，应用在抵抗媒介传播的疾病、代谢疾病、药物组合等方向，能够解决差穿过血脑屏障、分布受限等问题，达到增强直接给药的效果

Inactive Publication Date: 2018-07-06
NEURODYN LIFE SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Polar galantamine is reabsorbed at the nasal epithelium but then only poorly crosses the blood-brain barrier because of its limited intracerebral drug distribution across the BBB

Method used

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  • Application of GLN-1062 salt in the preparation of drug for treating brain diseases related to cognitive disorders
  • Application of GLN-1062 salt in the preparation of drug for treating brain diseases related to cognitive disorders
  • Application of GLN-1062 salt in the preparation of drug for treating brain diseases related to cognitive disorders

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Experimental program
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Effect test

Embodiment Construction

[0081] The detailed description of the invention covers the following developments:

[0082] (1) In a preferred embodiment, a prodrug of galantamine that is significantly more lipophilic than its parent compound is provided, thereby increasing its passive transport across the blood-brain barrier (BBB) ​​into the brain.

[0083] (2) These prodrugs are pharmacologically inactive and do not produce any significant G1 or other side effects as long as they remain uncleaved in specific tissues. Following enzymatic cleavage, each molecule of prodrug forms one molecule of parent drug, resulting in the full pharmacological effect of the drug. If cleavage occurs preferentially in the brain due to increased distribution in the brain and the presence of suitable endogenous enzymes available therein, significantly higher drug concentrations and thus larger drug concentrations are produced at the target site in the CNS. medicinal benefits.

[0084] (3) Administration via the oral or nasal...

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Abstract

The present invention relates to the use of a gluconate, a saccharic acid salt or a lactate of GLN-1062 for the preparation of a drug for treating brain diseases related to cognitive disorders in a mammal, wherein the drug is administered by mucosa. The mucosal administration is selected from intranasal, sublingual or buccal administration. Due to the mode of administration and a chemical propertyof the compound of the invention, the selected administration route has optimal brain delivery.

Description

[0001] The application date of this application is July 29, 2013, the international application number is PCT / EP2013 / 065880, and the national application number is 201380039870.3. The divisional application of the invention patent application of "Brain Bioavailability of Lanthamine". technical field [0002] The present invention relates to selected routes of administration for CNS (Central Nervous System) therapeutic and highly soluble salts, solutions, emulsions or powder formulations thereof, which are selected due to the mode of administration and chemical nature of the compounds of the invention. The route of administration has optimal brain delivery. Therapeutic compounds of the present invention relate to lipophilic prodrugs of pharmacologically active compounds which, as prodrugs, are insensitive to their primary targets in the CNS, especially cholinesterase and / or nicotinic acetylcholine receptors. Active. The pharmacologically active parent drug is cleaved by endog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61K9/107A61K9/14A61K9/20A61P25/28
CPCA61K9/006A61K9/1075A61K9/2072A61K9/2846A61K31/55A61K31/00A61P11/00A61P21/00A61P25/00A61P25/02A61P25/04A61P25/08A61P25/16A61P25/18A61P25/28A61P25/30A61P25/32A61P25/34A61P29/00A61P29/02A61P3/02A61P39/02A61P43/00A61P9/00A61P9/10Y02A50/30A61K9/14A61K9/2086
Inventor 阿尔弗雷德·梅里克
Owner NEURODYN LIFE SCI