NCOA7-Activating Compounds for Pulmonary Vascular Inflammation
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Solution Overview
Problem
The precise causative mechanisms of vascular inflammation, particularly in pulmonary vascular diseases such as pulmonary arterial hypertension (PAH), remain enigmatic, and there is a need for effective therapeutics to treat inflammation and inflammatory diseases, including cardiovascular inflammation, vascular inflammation, autoimmune diseases, heart disease, lung disease, sepsis, cancer, and neurodegeneration.
Innovation Solution
Administering specific compounds or their pharmaceutically acceptable salts, such as those with structures described, or using gene editing methods like CRISPR/Cas9 to modify SNP rs11154337, to reduce inflammation and treat conditions like pulmonary arterial hypertension (PAH) and other inflammatory diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional therapies are used to treat inflammation, then existing treatments can be administered, but the precise causative mechanisms remain enigmatic and treatment effectiveness is limited
Solution Approach 1:
The patent modifies molecular parameters by creating compounds with specific structural features (R1-R12 substituents) that change the pharmacological parameters to effectively target and modulate inflammatory pathways, resolving the contradiction between treating inflammation and understanding the precise mechanisms through structure-activity relationship analysis
2Reliability
If new compounds are developed to treat inflammation, then treatment effectiveness improves, but the complexity of compound structure increases
Solution Approach 1:
The patent segments the compound structure into distinct functional modules (R1-R12 substituents attached to a core structure) where each segment can be independently optimized for specific inflammatory pathways, allowing systematic development of inflammation-reducing activity without excessive overall complexity
Solution Approach 2:
The patent creates a universal compound scaffold that can target multiple inflammatory pathways and conditions (vascular inflammation, autoimmune diseases, cancer, neurodegeneration) through a single structural platform, improving treatment effectiveness across diverse conditions without proportionally increasing structural complexity
3Measurement precision
If gene editing is used to treat inflammation, then treatment precision improves, but the complexity of the treatment approach increases
Solution Approach 1:
The patent uses CRISPR/Cas9 as an intermediary tool to precisely modify specific genetic sequences (SNP rs11154337) associated with inflammation susceptibility, achieving high treatment precision by targeting specific genetic markers while managing complexity through established gene editing protocols
Data Source
AI summary
Provided herein are methods of treating a patient, such as a human patient, having inflammation or an inflammatory disease or a disease in which inflammation is present, such as cardiovascular or vascular endothelium inflammation, such as pulmonary hypertension, restenosis, essential hypertension, atherosclerosis, stroke, sepsis, or a viral infection, such as a coronavirus infection, SARS-CoV-2. The methods comprise administering to the patient an amount of a compound as described herein effective to treat the patient. NCOA7-activating compounds and compositions also are provided. Also provided is a gene editing method of reducing inflammation or an inflammatory condition in a patient having a C at SNP rs 11154337, comprising editing the C to a G.