Salt Forms of Aminopyrazole KM-819 for Ischemic Injury
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Solution Overview
Problem
Current treatments lack an effective agent to prevent and treat ischemic heart diseases and other conditions caused by ischemia-reperfusion injury, which leads to significant morbidity and mortality due to cell death and tissue damage.
Innovation Solution
A salt compound of the formula (2) is developed, comprising a cation such as potassium, sodium, or calcium, and a solvent like water or ethanol, which inhibits ischemic cell death by forming a salt with the aminopyrazole derivative KM-819, thereby protecting cardiomyocytes and reducing reperfusion-induced injuries.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for ischemic diseases, then standard care is provided, but effective prevention and treatment of ischemia-reperfusion injury is not achieved
Solution Approach 1:
The patent applies parameter changes by converting the parent compound KM-819 into different salt forms (sodium salt, potassium salt, calcium salt, magnesium salt) with varying physicochemical properties. Each salt form exhibits different solubility, stability, and bioavailability characteristics, allowing optimization for specific therapeutic applications while maintaining the core ischemic cell death inhibitory activity
Solution Approach 2:
The patent creates composite pharmaceutical compositions by combining the salt forms of KM-819 with various excipients, carriers, and formulation agents. These composite formulations enhance drug delivery, stability, and therapeutic efficacy while addressing the lack of effective treatments for ischemia-reperfusion injury
2Ease of operation
If salt forms are developed to improve drug properties, then solubility and bioavailability are enhanced, but formulation complexity increases
Solution Approach 1:
The patent systematically varies the counterion parameter (sodium, potassium, calcium, magnesium) to optimize solubility and bioavailability. Each salt form represents a controlled parameter change that improves drug properties while maintaining a standardized formulation approach, thereby managing complexity
Solution Approach 2:
The patent develops universal formulation platforms that can accommodate different salt forms of KM-819 using similar excipients and manufacturing processes. This multi-functional approach allows the same formulation strategy to be applied across multiple salt variants, reducing overall formulation complexity despite the variety of salt forms
Data Source
AI summary
A salt compound of 4-(2-((4-bromophenyl)thio)acetamido)-1-phenethyl-1H-pyrazole-3-carboxylic acid is disclosed. Also disclosed are methods for making the salt compound and formulations of the salt compound into dosage forms for clinical use.