Quinazolinone - Derivatives and Their Applications
Our partner, a Hungarian University has developed the quinazolinone - derivatives and their use for preparation of pharmaceutical compositions having PARP enzyme inhibitory effect. The client is looking for a sales agreement, a license agreement or a R&D agreement opportunity. Abstract: The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula, that inhibit a DNA-repairing enzyme, poly (ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I); R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation process of the compounds described above. Innovation of the technology: A series of 4(3H)-quinazolinone derivatives were synthesized by alkylating the original cyclic compounds and by nitrile acylation of antranilic acid, which was followed by the closure of the quinazoline ring. 4-(3H)-quinazolinone derivatives containing S-ethyl sidechains substituted with tertiary amines on the carbon of position 2 proved to be the most effective PARP inhibitors among the synthesized and examined compounds. The effect of nitroxide or amino precursor forms was smaller than that of the tertiary amines, but similar to each other, nevertheless having free radical scavenger anility they might be favorable. The data show that the compounds of the present invention significantly decrease the effects of oxidative stress and inhibit poly (ADP-ribose) polymerase. The protecting effect of the above mentioned compounds mainly concern their effect on poly (ADP-ribose) -polymerase (PARP) inhibition, thus having a protecting role in every kind of pathological processes, where the protecting-effect of PARP inhibition has a great importance. Consequently, the compounds of the present invention greatly improve the status of the multiple organ failure syndrome present in sepsis (and its most severe form, septic shock) or in other diseases. Furthermore, they could be used in the treatment of renal failure, hepatic failure, neurodegenerative and inflammatory diseases, and diseases related to ischemia and reperfusion. Thus, the compounds of the present invention decrease the severity of infraction, type 2 diabetes and insulin resistance as well as the metabolic X syndrome, the rheumatoid arthritis and also decrease the tumor formation in chronic inflammations.
Sector: Medical Technologies
Area of Application: Protecting heart against doxorubicine induced cardiotoxicity. Protection against hypertenion induced cardiomyopathy. Protection against ischemic heart damages. Protection against brain damages. Potential areas of use: • Medical treatment • Healthcare • Pharmaceutical industry
Keywords: Medical treatment; Healthcare; Pharmaceutical industry; Quinazoline.
Advantages: Our inventive PARP-inhibiting chemicals decrease the severity of infarction, type 2 diabetes and insulin resistance as well as the metabolic X syndrome, the rheumatoid arthritis and also decrease the tumor formation in chronic inflammations.
Environmental aspects: Not Applicable
Development Status: Laboratory Model
Legal Protection: Patent
Transfer Terms: Joint Venture , Technology Licensing , Others , Sales
Target Countries: World Wide
Estimated cost (US$):
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Contact Person: Laser Consult Ltd (Hungary)
Address: H-6701 PO Box 1191.