SSTR2 Agonist Compounds for Effective Formulation and Administration
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Solution Overview
Problem
Existing compounds do not effectively act as somatostatin receptor 2 (SSTR2) agonists that can be efficiently formulated and administered to treat diabetes-related pathologies and other conditions such as diabetes, diabetic retinopathy, neuropathy, and nephropathy, among others, due to inefficiencies in activation and administration.
Innovation Solution
Development of compounds of Formula I and their pharmaceutically acceptable salts, which act as SSTR2 agonists, formulated into pharmaceutical compositions for effective treatment of diseases associated with somatostatin receptors.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing compounds are used as SSTR2 agonists, then some therapeutic activity is achieved, but the activation efficiency and administration effectiveness are insufficient
Solution Approach 1:
The patent applies parameter changes by systematically modifying the chemical structure of somatostatin analogs through variations in amino acid residues at specific positions (e.g., positions 3, 8, 13, 14, 18, 22, 23, 28). These structural parameter changes result in compounds with enhanced SSTR2 binding affinity and agonist activity, directly addressing the insufficient activation effectiveness of existing compounds while maintaining pharmacological utility for diabetes-related pathologies treatment
2Reliability
If new compounds with enhanced SSTR2 agonist activity are developed, then treatment efficacy is improved, but formulation and administration challenges arise
Solution Approach 1:
The patent addresses formulation and administration challenges by modifying physicochemical parameters of the compounds including solubility characteristics, molecular weight, and stability profiles through specific amino acid substitutions. These parameter changes enable the development of compounds that maintain high SSTR2 agonist activity while improving their suitability for pharmaceutical formulation and clinical administration
Solution Approach 2:
The patent employs intermediary approaches by developing pharmaceutical compositions that include the novel SSTR2 agonist compounds in combination with appropriate excipients, carriers, and formulation agents. These intermediaries facilitate the delivery and administration of the active compounds, bridging the gap between enhanced efficacy and practical administerability in clinical settings
Data Source
AI summary
The subject matter described herein is directed to somatostatin receptor activating compounds, methods of making the compounds, pharmaceutical compositions, and their use in the treatment of diseases associated with somatostatin receptors.