RPE-Regenerating Compounds for AMD and Geographic Atrophy
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Solution Overview
Problem
Current treatments for dry AMD and wet AMD do not address the damage to the retinal pigment epithelium (RPE) layer, and existing therapies for wet AMD only suppress neovascularization without being curative, while there are no approved treatments for dry AMD or its advanced form, geographic atrophy.
Innovation Solution
Compounds of formula (I) stimulate pigmentation and/or growth of mammalian RPE cells, promoting their repair and regeneration, thereby preventing and reversing vision loss by endogenously generating new healthy RPE cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for dry AMD and geographic atrophy are used, then disease progression is slowed or symptoms are managed, but RPE cell damage cannot be reversed and vision loss cannot be restored
Solution Approach 1:
Instead of trying to prevent RPE cell death or manage symptoms, the patent applies the other way round by directly inducing RPE cell proliferation and differentiation to regenerate lost cells. The compound of formula (I) reverses the conventional approach by actively promoting cell growth rather than just preventing cell death, thereby restoring the RPE layer and reversing vision loss.
2Reliability
If transplantation of induced pluripotent stem cells or mature RPE cells is performed, then RPE cell replacement is achieved, but the procedure is complex and requires invasive surgical intervention
Solution Approach 1:
The patent enables the RPE tissue to self-repair by stimulating endogenous cell proliferation and differentiation. Instead of requiring external transplantation procedures, the compound of formula (I) activates the body's own RPE cells to divide and differentiate, replacing damaged cells through a self-service mechanism that avoids complex surgical intervention.
3Object-affected harmful factors
If anti-VEGF agents are used for neovascular AMD, then neovascularization is suppressed, but RPE cell damage and atrophy are not addressed
Solution Approach 1:
The compound of formula (I) provides multi-functional treatment by simultaneously addressing multiple aspects of AMD pathology. It not only suppresses neovascularization like anti-VEGF agents but also promotes RPE cell proliferation and differentiation, thereby treating both neovascular and atrophic forms of AMD with a single versatile therapy.
Data Source
AI summary
A method of treating and/or preventing disease involving retinal pigment epithelium, including administering compound of formula (I)or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or a corresponding diastereomer thereof, wherein: R1, R11 and R12 are independently selected from the group consisting of hydrogen, fluoro, chloro, methoxy, trifluoromethyl, methyl and difluoromethoxy, whereby at least one of R1, R11 and R12 is not hydrogen, B is selected from the group consisting of a residue of formula (II), (III), (IV), (V), (VI) and (VII)wherein, “*” denotes point of attachment to remainder of the molecule, and R2, R3, R4, R5, R2I, R3I, R4I, R5I, R2II, R3II, R4II, R5II, R2III, R3III, R4III, R5III, R2IV, R3IV, R4IV, R5IV, R2V, R3V, R4V, R5V are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl and difluoromethoxy.