2H-Benzotriazole Derivatives for Premature Ejaculation Control
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Solution Overview
Problem
Current treatments for premature ejaculation, such as dapoxetine, suffer from poor bioavailability and high clinical discontinuation rates due to dose-dependent side effects and poor efficacy, necessitating the development of new drugs with improved efficacy and reduced side effects.
Innovation Solution
Development of a novel 2H-benzotriazole derivative and its pharmaceutically acceptable salts, which are synthesized through specific chemical reactions and formulated into pharmaceutical compositions for oral and injectable forms, targeting the underlying neurotransmitter disorders associated with premature ejaculation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If dapoxetine is used to treat premature ejaculation, then ejaculation control is improved, but bioavailability is poor and side effects increase
Solution Approach 1:
The patent modifies the chemical structure of dapoxetine by introducing a benzotriazole group and various substituents (X, Y, Z, R parameters) to create derivatives with improved pharmacokinetic properties. This structural parameter change aims to enhance bioavailability while maintaining or improving ejaculation control efficacy and reducing dose-dependent side effects.
2Reliability
If dapoxetine dose is increased to improve curative effect, then ejaculation control improves, but side effects increase and clinical discontinuation rate increases
Solution Approach 1:
The patent creates multiple benzotriazole derivative compounds with varying substituent parameters (X=C3-C4-alkyl or C3-C4-alkoxy, Y=CH or N, Z=O or S, R=halogen atoms) to achieve optimal balance between curative effect and side effect profile, allowing effective treatment at lower doses.
3Duration of action of stationary object
If dapoxetine is administered continuously to maintain treatment effect, then ejaculation control is maintained, but cumulative discontinuation rate reaches 90% or more after two years
Solution Approach 1:
The patent develops benzotriazole derivatives with improved pharmacokinetic parameters including enhanced bioavailability and favorable metabolic profiles, aiming to maintain effective ejaculation control over extended treatment periods with better patient tolerance and satisfaction.
Data Source
AI summary
The invention discloses a benzisothiazole compound as well as a pharmaceutical composition and application thereof, belongs to the technical field of medicines, and particularly relates to a 2H-benzotriazole substituted benzisothiazole compound with a novel structure as shown in a formula (I), a pharmaceutical composition containing the compound and application of the compound in preparation of medicines for treating and/or preventing premature ejaculation. Through in-vivo activity test research, the compound has obviously higher anti-premature ejaculation activity than the on-sale drug dapoxetine.