Selective 5-LO inhibitors for the treatment of bronchial asthma

    公开(公告)号:US11773111B1

    公开(公告)日:2023-10-03

    申请号:US18071171

    申请日:2022-11-29

    CPC classification number: C07D513/04

    Abstract: 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 acceptor 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:

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