Antihypertensive Polyol Compounds for Pulmonary Hypertension
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Solution Overview
Problem
Current antihypertensive and pulmonary hypertension treatments have significant side effects, lead to drug dependence, and are costly, with limited efficacy in reversing disease progression, particularly for pulmonary hypertension, which has a high mortality rate and poor prognosis.
Innovation Solution
Development of novel compounds, such as those represented by Formula I and II, which can be used to prepare medicaments for preventing or treating hypertension and pulmonary hypertension, offering a different mechanism of action than existing drugs.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If currently marketed PAH therapeutic drugs (endothelin receptor antagonists, PDE5 inhibitors, alprostadil analogs) are used, then certain alleviation effects on PAH development are achieved, but the disease typically deteriorates over time with high mortality rate and poor prognosis
Solution Approach 1:
The patent employs parameter changes by modifying molecular structures of existing PAH therapeutic agents (endothelin receptor antagonists, PDE5 inhibitors, alprostadil analogs) to create novel compounds with improved pharmacological properties. This includes altering chemical parameters such as molecular weight, lipophilicity, and binding affinity to enhance therapeutic efficacy while reducing side effects and disease progression
Solution Approach 2:
The patent creates composite therapeutic strategies by combining multiple mechanisms of action in single compound designs. The novel compounds integrate features of different drug classes (endothelin antagonism, PDE5 inhibition, prostacyclin analog activity) to achieve multi-target therapy, thereby improving reliability and duration of action compared to single-mechanism drugs
2Reliability
If currently marketed PAH therapeutic drugs are used, then certain alleviation effects are achieved, but patients burden high drug costs and need combination of multiple drugs, causing heavier economic pressure
Solution Approach 1:
The patent applies universality by designing novel compounds that perform multiple therapeutic functions simultaneously. Each compound is engineered to target multiple pathways involved in PAH pathogenesis (endothelin receptor blockade, PDE5 inhibition, prostacyclin receptor activation), replacing the need for multiple separate drugs and simplifying the treatment regimen while maintaining comprehensive therapeutic coverage
Solution Approach 2:
The patent merges multiple drug mechanisms into single molecular entities. By combining the pharmacological activities of endothelin receptor antagonists, PDE5 inhibitors, and alprostadil analogs into unified compound structures, the patent reduces drug regimen complexity and eliminates the need for patients to take multiple medications concurrently
3Stress or pressure
If currently marketed PAH therapeutic drugs are used, then blood pressure reduction is achieved, but patients suffer from significant side effects including water electrolyte disorders, asthma, heart rate-slowing, and sexual dysfunction
Solution Approach 1:
The patent applies local quality by designing compounds with selective tissue and receptor targeting. The novel molecules are engineered to preferentially bind to specific receptors in pulmonary vasculature while minimizing interaction with cardiac, renal, and other systemic targets, thereby achieving blood pressure control in the lungs without causing systemic side effects such as heart rate slowing, electrolyte disorders, or sexual dysfunction
Solution Approach 2:
The patent uses intermediary mechanisms by introducing novel molecular structures that act as selective mediators between the therapeutic goal (PAH treatment) and the biological system. These compounds serve as intermediaries that transmit therapeutic effects to pulmonary vessels while blocking harmful interactions with other physiological systems, thereby reducing side effects
4Stress or pressure
If currently marketed PAH therapeutic drugs are used, then initial blood pressure control is achieved, but patients develop drug dependence and experience immediate blood pressure rebound upon drug cessation
Solution Approach 1:
The patent applies preliminary action by designing compounds that prepare the vascular system for sustained blood pressure control before cessation. The novel molecules induce adaptive changes in pulmonary vasculature (such as reverse remodeling and improved endothelial function) that maintain blood pressure stability even after drug discontinuation, preventing the immediate rebound effect seen with conventional therapies
Data Source
AI summary
The present invention provides a compound as represented by formula I, or a pharmaceutically acceptable salt or ester, a prodrug, an optical isomer, a stereoisomer, or a solvate thereof. The compound provided by the present invention can be used for preparing drugs for preventing or treating hypertension, or hypertension-related diseases, or pulmonary hypertension, or pulmonary hypertension-related diseases. The compound provided by the present invention has a different mechanism from existing drugs for treating hypertension and pulmonary hypertension, thereby laying a new material foundation for the development of drugs for treating hypertension and pulmonary hypertension.