Formula A-D-Y Compounds for VEGF Inhibition and Drug Resistance
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Solution Overview
Problem
There is a lack of efficacious and safe drugs to treat cancer, particularly ovarian cancer, which often develops drug resistance, and diabetic retinopathy, which has suboptimal treatment options, along with inflammation that can lead to various chronic diseases.
Innovation Solution
Development of compounds of Formula A-D-Y, or their pharmaceutically acceptable salts, solvates, hydrates, cocrystals, or prodrugs, which exhibit anti-inflammatory, anti-cancer, and anti-angiogenic effects, and are formulated into compositions for topical administration to treat conditions like diabetic retinopathy and other ophthalmic disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional chemotherapy is used to treat ovarian cancer, then initial response rate is high (80%), but drug resistance develops rapidly (within 6 months)
Solution Approach 1:
The patent combines two or more compounds with different mechanisms of action into a fixed-dose combination formulation. This preliminary combination approach ensures that multiple therapeutic pathways are activated simultaneously from the start of treatment, preventing the development of resistance that occurs when single agents are used alone. The fixed-dose combination delivers both compounds at optimized ratios throughout the treatment course.
Solution Approach 2:
The invention creates a composite pharmaceutical formulation containing multiple active compounds (e.g., Compound 1 and Compound 2, or Compound 1 and Compound 3) in specific ratios. This composite approach integrates the benefits of each individual compound - one targeting DNA damage response and the other targeting protein synthesis or translation initiation - to achieve synergistic anti-cancer effects that overcome drug resistance mechanisms.
2Reliability
If injectable treatments are used for diabetic retinopathy, then some therapeutic effect is achieved, but treatments are expensive and associated with complications
Solution Approach 1:
The patent replaces the mechanical injection method with a topical ophthalmic formulation that can be administered as eye drops or ointment. This substitution eliminates the risks and costs associated with repeated injections while maintaining therapeutic efficacy through local delivery of the anti-angiogenic compounds directly to the retinal tissue.
Solution Approach 2:
The invention uses ophthalmic formulations containing the compound of Formula A-D-Y as an intermediary delivery system. These formulations are designed to provide sustained local concentrations of the active compound at the site of action (retina), achieving therapeutic effects without the need for systemic injection and thereby reducing complications and costs.
3Reliability
If inflammation is allowed to proceed unchecked, then immune defense function is maintained, but chronic inflammation leads to tissue destruction and various diseases
Solution Approach 1:
The patent selectively targets and inhibits specific pro-inflammatory pathways (such as NF-κB signaling) while preserving the overall immune defense function. By extracting or blocking only the harmful inflammatory signaling pathways that lead to tissue destruction, the compounds maintain beneficial immune responses while preventing chronic inflammation-associated damage and disease.
Data Source
AI summary
Compounds of the general Formula A-D-Y are disclosed with activity towards treating diseases related to inflammation, cancer, neurodegenerative diseases, and cardiovascular diseases. Pharmaceutical compositions, methods of making, and methods of use thereof are also described.