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Publication Number
US-9770431-B2
Publication Date
2017-09-26
Expiration Date
Abstract
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
Core Innovation
The disclosed invention relates to tiglien-3-one derivative compounds defined by formula (I) and, in particular, to compounds of formula (II). The compounds include a linker X selected from O, S, or NR25, and substituent-variable definitions for R1–R24, including alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heterocyclyl or heteroaryl groups that are optionally substituted. The structural scope further includes geometric isomers or stereoisomers and pharmaceutically acceptable salts of the compounds.
The disclosure positions the tiglien-3-one derivatives as agents for treating or preventing infections, including bacterial and nematode infections, and in the broader disclosure also protozoal and parasitic infections. The compounds are described for controlling infection and related disease conditions, including infections characterized by listed protozoal and bacterial targets and by nematodes and parasitic organisms.
The invention also addresses controlling cell proliferative disorders and cytotoxic uses associated with the disclosed compounds. The document further describes biological activity screening approaches and associated in vivo topical or intralesional tumor treatment results using specific disclosed embodiments, including EBI-46, EBI-47, EBI-59, and EBI-61.
In addition, the disclosure positions the compounds for agrochemical and pesticidal use, tying tiglien-3-one derivative compounds to pesticidal applications. The described embodiments and biological activities use listed screening bioassays and provide examples of effects linked to the disclosed compound structures.
Claims Coverage
The independent claim is directed to a treating method using compounds of formula (II), with inventive features centered on the specific formula-(II) chemical definition, including linker X and substituent-variable ranges, and the therapeutic indication for bacterial or nematode infection. No other independent claims are provided in the partial content.
Treatment of bacterial or nematode infection with a formula (II) compound
A method of treating a bacterial or nematode infection by administering to a subject in need thereof a compound of formula (II), including the definitions of X as O, S, or NR25 and the substituent-variable definitions for R1–R24 and related groups, optionally as geometric isomers or stereoisomers, or pharmaceutically acceptable salts.
Overall, the claim coverage provided centers on administering formula (II) tiglien-3-one derivative compounds with a defined linker and broad substituent-variable definitions to treat bacterial or nematode infections in a subject.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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