EMP2: Ethyl-Methyl, di Methyl, tri Methyl Pyruvate Acid Esters: A Tool for Regulating HbA1c and a Riboswitch Activator

Abstract

The invention is a novel series of compounds represented by general formula, its analogs, tautomeric forms, stereoisomers, pharmaceutically acceptable salts and polymorphs wherein said compound described is a group of antisense molecules possessing immediate global cellular penetration due to their molecular structure and lipophilicity. The molecules are combinations of ethyl and methyl pyruvates. They induce riboswitch activity and reduce target RNA and nucleic acids such as HbA1c. They reduce inflammation and enhance energy production. These features improve therapeutic outcomes of diabetes, neuropathy and cellular aging.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit of U.S. Provisional Application No. 61 / 521 / 747 titled “EMP2: Ethyl-Methyl, di Methyl, tri Methyl Pyruvate Acid Esters: A Tool for Regulating HbA1c and a Human Riboswitch Activator” field Aug. 09, 2011 at 23:33:42 EST, which is hereby incorporated by reference in its entirety.FIELD OF INVENTION[0002]This present invention describes a short systemic and antisense compound. Included are such compounds comprising chemically combined moieties of ethyl and methyl, di Methyl, tri Methyl pyruvic acid esters. Said compound is chemically combined in such a manner as to retain the individual properties of each separately and utilize the combinatorial valency and synergy of joining the two. Such a short targeted compound is useful for the reduction of target nucleic acids and / or proteins such as HbA 1 c, high-affinity nucleotide modifications useful for reducing a target RNA in vivo, in tissues, animals and humans w...

AI Technical Summary

Benefits of technology

[0016]This invention, ethyl pyruvate & methylated pyruvates (mono, di, tri), are lipophilic antisense permeants, each of which holds on to its own membrane penetrability, as well as acting collectively to produce a time-released delivery within the inner mitochondria. The combinational synergy is greater than each can effect individually. Their separate and combinatorial, targeted molecular capabilities are useful in reduction of target nucleic acids, and or proteins such as HbA1c, directly enabling improved therapeutic outcomes. Because of the active and passive energy delivery by the invention, all intracellular and intra-nuclear functions are upgraded and rebooted with enhanced intracellular crosstalk and signaling; the genome is also rebooted in an enhanced manner. The more efficient genomic guidance allows improved glucose control that disables oncoming crippling diseases from getting a foothold; energy stays the up-regulation of all cellular function that cannot allow cellular deterioration. The same guidance mechanism demonstrates certain esters of pyruvate have pharmaceutical effects, such as reducing the inflammatory response. Also, mitochondrial expression enacts changes, via the nuclear genomic creation of these sustaining organelles, to provide upstream molecular regulators: the master regulators being PGC1a and AMPK. The targets homeostatically and instantly recalibrate from PGC1a and AMPK with the downstream signaling molecules coming from the activities of SIRTS, FOXO, CAMP, CREB and PPARs. Their communication and crosstalk enable a synchrony of NADH / NAD / FAD / Acetyl fuel / PO4 regulation, as well as glycolysis with its electron and proton transfer and gradient balancing cellular requirements each and every picosecond with all the above molecules and their networking.

Problems solved by technology

Diseases such as type II diabetes (DM2) are caused by insufficient energy required to continuously maintain the structure and function in cells.

Finally, cytosolic and nuclear components are malfunctioning, and are in need of repair or replacement.