Re: TETRACYCLIC AMIDE - A NOVEL CATARACT REVERSAL AGENT at Eyes Problems Forum

THE CATARACT REVERSAL AGENT CLAIMED, BASED ON ANIMAL AND HUMAN TRIALS ALREADY CARRIED OUT, TO BE A SAFE AND EFFECTIVE ONE-WEEK CURE

TETRACYCLIC UREA ADDUCT OF 2-BENZYLIDENE-1,3-INDANEDIONE

1) SYNTHESIS
2) TOXICOLOGY STUDIES ON HUMAN CORNEA, LENS AND RETINA CELL LINES TO CONFIRM SAFETY
3) ANIMAL STUDIES ON SENILE CATARACT TO CONFIRM LACK OF TOXICITY, AND EFFECTIVENESS TO RESTORE CLARITY TO
LENS
4) HUMAN CLINICAL TRIALS ON SENILE CATARACT (RANDOMIZED, DOUBLE-BLIND)

It is probably no accident that both this urea adduct, and NACA (N-acetylcysteine amide) which others have mentioned on CureZone, are AMIDES. With advancing age, both the soluble, chaperone CRYSTALLINS (which keep the lens clear), and the AMIDES which allow those crystallins to reach all parts of the lens, are leached out of the lens into the aqueous - leaving the lens highly vulnerable to oxidative challenge resulting in cataract, and making it impossible for the crystallins to reach the cataract once it forms. These two agents probably re-supply amide to the substance of the lens, allowing the small amounts of crystallins and reducing enzymes still being produced by secondary lens fibers on the equator of the lens, to reach the nucleus of the lens once again, and restore clarity to it. If we do nothing, then this compound, like others before and after it - although it has the potential to prevent and/or cure blindness due to cataract in a reasonable time frame without exposing 20 to 50 million people to the risk of surgery - will end up in the trash can. What we need is for someone out there to synthesize this urea adduct of 2-benzylidene-1,3-indanedione, and prove it is indeed safe and effective by following the steps 1) through 4) above. The synthesis is described at:

[2-benzylidene-1,3-indanedione is refluxed together with urea in glacial acetic acid for 25 minutes, whereupon red crystals should separate out. The reaction mixture is allowed to stand at room temperature for a further 2 hours, and the red crystals are then separated and recrystallized from acetic acid].

Urea itself is actually an amide with 2 amino groups, and so by this process, the indanedione has been converted into a cyclic amide. This cyclic amide is our cataract reversal agent, and can then be made up into eyedrops which we must confirm to be safe and effective as was claimed in 1992.

Another advantage of the compounds of the invention, besides the above mentioned, is that it is safe to use in vivo as shown in animal experiments on dogs and rabbits. These experiments lead to the transparency of the induced irradiated cataract, after applying the aqueous eye drops containing 0.05 ml Tween 60 per mole of compound III three times daily for a period up to 7 days. Transparency of the lens occurred without development of any side effects such as irritation or allergic reaction.

The application of formulations of the invention on cataractous human lens protein also gave similar beneficial results as mentioned above for the animals. In these tests the transparency of cataractous lens protein was demonstrated by the clinical improvement of vision, red reflex test and the comparison of ultrasonography pictures taken before and after treatment.

Direct photography of the anterior segment of the eye also showed the difference between the configuration of the lens before and after treatment.

I hope that, for the sake of humanity, someone out there reading this message who can get this compound synthesized and tested again, will act, and act fast.