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An H3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease

A technology for Alzheimer's and inhibitors, applied in drug combinations, nervous system diseases, active ingredients of heterocyclic compounds, etc.

Inactive Publication Date: 2016-07-13
SANOFI SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there is a large unmet need for better and safer treatments for AD

Method used

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  • An H3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease
  • An H3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease
  • An H3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1: Preclinical Research

[0099]In the object recognition test, 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydro Oral administration of isoquinoline-7-sulfa hydrogen fumarate monohydrate (3 mg / kg) or donepezil hydrochloride (DNP) (3 mg / kg), respectively, enhanced memory in CD1 male mice 24 hours after administration , in contrast to the lack of cognitive-promoting effects observed 48 hours after administration of either molecule. However, 3 mg / kg of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydro The co-administration of isoquinoline-7-sulfa hydrogen fumarate monohydrate and 3 mg / kg donepezil hydrochloride had a significant procognitive effect 48 hours after administration. The cognitive-promoting effect of this co-administration at 48 hours indicated that 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1 , Potentiation effect of 2,3,4-tetrahydroisoquinoline-7-sulfa hydrogen fum...

Embodiment 2

[0101] Embodiment 2: clinical research

[0102] A randomized, double-blind, parallel-group, placebo-controlled clinical study was carried out to investigate the Efficacy, safety and tolerability of 1,2,3,4-tetrahydroisoquinoline-7-sulfonamide hydrogen fumarate monohydrate as adjunctive therapy to donepezil on cognitive performance.

[0103] More specifically, patients with mild to moderate Alzheimer's disease receiving stable donepezil therapy were randomized to receive 2-(cyclohexylmethyl)-N- {2-[(2S)-1-Methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide hydrogen fumarate monohydrate or placebo dose for 24 weeks, and a follow-up period of 10 weeks.

[0104] 291 patients (290 treated) participated in the study. The baseline characteristics of the randomized patients are described in Table 1.

[0105] Table 1: Randomized populations

[0106]

[0107]

[0108] The modified intention-to-treat (mITT) population were randomized patients who received...

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PUM

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Abstract

The disclosure relates to a compound 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide or a pharmaceutically acceptable salt thereof, intended for treatment of Alzheimer's disease and other types of dementia.

Description

[0001] The present invention relates to compound 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinone Use of phenoline-7-sulfonamide or a pharmaceutically acceptable salt thereof for treating Alzheimer's disease. Background of the invention [0002] Dementia is a brain disorder that seriously affects a person's ability to carry out normal daily activities. In older adults, Alzheimer's disease (AD) is the most common form of dementia and involves the parts of the brain that control thinking, memory and language. Despite intensive research worldwide, the causes of AD are unknown and there is no cure. [0003] Progressive decline in cognitive performance and incapacity in activities of daily living (ADL) are key features of Alzheimer's disease, and improvements in cognitive function (including memory, attention, or executive function), functional Capability and behavior are complex challenges, given the involvement of the numerous neurotra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61K31/4725A61P25/28
CPCA61K31/27A61K31/325A61K31/445A61K31/4725A61K31/55A61P25/00A61P25/18A61P25/20A61P25/28A61P43/00A61K2300/00C07D401/12C07D403/12
Inventor P·巴诺S·克劳德尔P·蒂莱-戈耶M·洛佩斯-格兰查J·普拉特J·施特梅林
Owner SANOFI SA
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