Benzisothiazole Composition for Premature Ejaculation With Fewer Side Effects
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Solution Overview
Problem
Current treatments for premature ejaculation, such as dapoxetine and local anesthetics, suffer from poor efficacy, adverse reactions, and low patient compliance, while SSRIs require gradual withdrawal to avoid syndromes, limiting their clinical use.
Innovation Solution
A novel 2H-benzotriazole-substituted benzisothiazole compound and its pharmaceutically acceptable salts, formulated in various dosage forms, are developed for treating premature ejaculation, offering improved efficacy and reduced adverse effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If dapoxetine is used to treat premature ejaculation, then ejaculation time is extended, but adverse reactions such as nausea, diarrhea, headache and insomnia occur
Solution Approach 1:
The patent modifies the chemical structure by introducing a 2H-benzotriazole substituent at specific positions (R1-R6) of the benzisothiazole core, changing the pharmacological parameters to achieve better therapeutic index with reduced adverse reactions while maintaining anti-premature ejaculation activity
Solution Approach 2:
The invention creates a composite molecular structure combining benzisothiazole core with 2H-benzotriazole substituent, where the synergistic interaction between these structural components produces improved pharmacological profile with both efficacy and reduced side effects
2Duration of action of moving object
If local anesthetics are used to delay ejaculation, then ejaculation time is extended, but erectile dysfunction occurs reducing sexual satisfaction
Solution Approach 1:
The patent changes the mechanism of action by designing a compound that acts on serotonin reuptake inhibition rather than local anesthesia, fundamentally altering the pharmacological parameters to avoid erectile dysfunction while extending ejaculation time
3Duration of action of moving object
If SSRIs are used to treat premature ejaculation, then ejaculation control is improved, but withdrawal syndromes occur requiring gradual tapering over 2-3 months
Solution Approach 1:
The patent optimizes the chemical structure to achieve potent serotonin reuptake inhibition at lower doses, changing the pharmacokinetic parameters to reduce accumulation and withdrawal effects, enabling shorter treatment courses without severe withdrawal syndromes
4Duration of action of moving object
If dapoxetine is used for treatment, then premature ejaculation is addressed, but clinical withdrawal rate is high increasing over time
Solution Approach 1:
The patent modifies the molecular structure to improve the therapeutic index by reducing adverse reactions, changing the reliability parameters to maintain patient compliance and reduce withdrawal rates over extended treatment periods
Data Source
AI summary
Provided are a benzisothiazole compound and application thereof, and a pharmaceutical composition and application thereof, which relate to the technical field of medications, and specifically relate to a 2H-benzotriazole-substituted benzisothiazole compound having a novel structure shown in a formula (I), as well as a pharmaceutical composition including the compound, and use of the pharmaceutical composition for the manufacture of a medicament for treatment and/or prevention of premature ejaculation. The anti-premature ejaculation activity of the compound is significantly higher than that of a marketed drug, namely dapoxetine, as studied by in vivo activity tests.