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Combination of drugs for use in the treatment of Alzheimer's disease

一种阿尔茨海默氏、药学的技术，应用在5-HT6受体拮抗剂及其药学上可接受的盐领域，能够解决没有任何治愈和治疗痴呆等问题

Pending Publication Date: 2020-04-17
H LUNDBECK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Currently, there are no cures and treatments that can slow or stop the progression of dementia

Method used

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  • Combination of drugs for use in the treatment of Alzheimer's disease
  • Combination of drugs for use in the treatment of Alzheimer's disease
  • Combination of drugs for use in the treatment of Alzheimer's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0017] Embodiments of the present invention are disclosed below. The first embodiment is denoted El, the second E2, and so on.

[0018] E1 a 5-HT 6 Receptor antagonists or pharmaceutically acceptable salts thereof for the treatment of Alzheimer's disease by improving or increasing the effect of acetylcholinesterase inhibitor therapy wherein Alzheimer's disease patients carry one or two ApoE4 etc. bit gene.

[0019] E2 In one embodiment of E1, 5-HT 6 The receptor antagonist is selected from the group consisting of Idalupyridine, AVN-211 and RVT-101, or the 5-HT 6 A pharmaceutically acceptable salt of a receptor antagonist.

[0020] E3 In one embodiment of E1 or E2, 5-HT 6 The receptor antagonist is Idalupridine or a pharmaceutically acceptable salt thereof.

[0021] E4 In one embodiment of E1 or E3, 5-HT 6 The receptor antagonist is Idalupridine hydrochloride.

[0022] E5 In one embodiment of E1 or E2, 5-HT 6 The receptor antagonist is AVN-211 or a pharmaceutically acc...

example 1

[0100] Example 1: Binding Affinity Determination and Results for Idalupridine

[0101] Previously, as Arnt J, et al. Lu AE58054, a 5-HT 6 receptor antagonist, reverse cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. [a 5-HT 6 Receptor antagonist Lu AE58054 reverses subchronic phencyclidine-induced cognitive impairment in a novel object recognition test in rats] Int J Neuropsychopharmacol 2010; 13:1021-1033 Determination of the 5-HT binding affinity of idalupridine. Reported results showing that N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine is effective and selective human 5-HT 6 Receptor Antagonist, Its Effect on Human 5-HT 6 The receptor, as well as other human 5-HT receptor subtypes, has the following affinities:

[0102]

[0103]

[0104] Table 1: Idalupridine Inhibition of 5-HT Receptors

example 2

[0105] Example 2: Phase III Study

[0106] The Phase III program was initiated by H.Lundbeck A / S (HLu) and consisted of three 24-week trials in patients over 50 years of age with mild-moderate AD (MMSE 12-22 at screening) , double-blind, parallel-group, placebo-controlled, fixed-dose (10, 30, and 60 mg QD) idalupridine as adjuvant AChEI study consisted of:

[0107]

[0108] Table 2: Phase III studies

[0109] Change from baseline to week 24 in the primary endpoint on the Alzheimer's Disease Assessment Scale-Cognitive Subscale (ADAS-cog). This endpoint addresses the primary objective of the study, which was to establish the efficacy of idalupridine as adjunctive therapy to donepezil in the symptomatic treatment of patients with mild-moderate AD.

[0110] Key secondary endpoints included change from baseline to week 24 in the Alzheimer's Disease Collaborative Study-Detailed Record of Activities of Daily Living (ADCS-ADL) total score.

[0111] The Mini-Mental State Examinat...

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Abstract

The present invention relates to 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease, wherein the Alzheimer's disease patient carries one or two ApoE4 alleles, comprising administering an effective dose of a 5-HT6 receptor antagonist to improve or augment the effect of an acetylcholinesterase inhibitor.

Description

technical field [0001] The present invention relates to 5-HT for the treatment of Alzheimer's disease 6 Receptor antagonists and pharmaceutically acceptable salts thereof, wherein the treatment further comprises the use of acetylcholinesterase inhibitors, and the Alzheimer's disease patient carries one or two ApoE4 alleles. Background technique [0002] Dementia is a clinical syndrome characterized by deficits in multiple cognitive areas unexplained by normal aging, marked decline in function, and absence of delirium. In addition, neuropsychiatric symptoms are often present at the time of first diagnosis and then increase in number and intensity over time as the disease progresses. The ε4 allele of the apolipoprotein E gene (APOE4) is known to be one of the most important genetic risk factors for Alzheimer's disease (AD) (Roses A.polipoprotein E alleles asrisk factors in Alzheimer's disease. [ApoE Protein E alleles as risk factors in Alzheimer's disease.] Ann Rev Med. [Ann...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4045A61K31/445A61K31/496A61K31/505A61K31/27A61K31/55A61K45/06A61P25/28
CPCA61K45/06A61K31/27A61K31/445A61K31/496A61K31/505A61K31/55A61P25/28A61K31/4045A61K2300/00A61K31/506
Inventor K·温德菲尔德
Owner H LUNDBECK AS
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