SELECTIVE 5-LO INHIBITORS FOR THE TREATMENT OF BRONCHIAL ASTHMA
SELECTIVE 5-LO INHIBITORS FOR THE TREATMENT OF BRONCHIAL ASTHMA
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US 11,773,111B1
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الصحة - Health
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2023
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مكتب البراءات الأمريكي - US Patent Office
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Saadeldin Elsayed Ibrahim Shabaan, Al-Ahsa (SA); Hany Mohamed Abd El-Lateef Ahmed, Al-Ahsa (SA).
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Novel dual 5-LO inhibitors of well-validated electrophilic Michael acceptors and nitrogen-heterocycles are presented and designed to maintain specific structural features of currently known dual 5-LO inhibitors and to overcome their drawbacks. The Michael acceptors scaffold will act as a carrier and will provide a stable anchorage via covalent binding to cysteine/histidine residues within the catalytic cleft and/or the surface interface of the 5-LO; whereas, the nitrogen-heterocycles will ensure the access to the Fe(II) catalytic center. These combinations offer potential for more than one mode of iron chelation and 5-LO inhibition. The dual 5-LO inhibitors fall within the following general formula, with the substituents as defined in the attached specification, and are useful for treating bronchial asthma: