01-04-2021 дата публикации
Номер: US20210094941A1
Принадлежит:
The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted by an arylaminophenyl or heteroarylaminophenyl moiety. The compounds are potent inhibitors of the growth and propagation of the parasite in human blood and thus useful as pharmaceutical agents for the treatment of malaria. 2. A compound as claimed in wherein Z represents phenyl claim 1 , naphthyl claim 1 , 2 claim 1 ,3-dihydroindolyl claim 1 , 2 claim 1 ,3-dihydrobenzoxazinyl claim 1 , pyrazolyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl claim 1 , pyrazolo-[3 claim 1 ,4-b]pyridinyl claim 1 , indazolyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , imidazo[1 claim 1 ,5-a]pyridinyl claim 1 , imidazo-[4 claim 1 ,5-b]pyridinyl claim 1 , [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ,5-a]pyridinyl claim 1 , pyridinyl claim 1 , quinolinyl claim 1 , isoquinolinyl claim 1 , pyridazinyl claim 1 , pyrimidinyl or pyrazinyl claim 1 , any of which groups may be optionally substituted by one claim 1 , two or three substituents independently selected from halogen claim 1 , cyano claim 1 , Calkyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , trifluoroethyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyanocyclobutyl claim 1 , phenyl claim 1 , azetidinyl claim 1 , oxopyrrolidinyl claim 1 , morpholinyl claim 1 , oxazolyl claim 1 , methyloxadiazolyl claim 1 , triazolyl claim 1 , methyltetrazolyl claim 1 , oxo claim 1 , Calkoxy claim 1 , difluoromethoxy claim 1 , trifluoromethoxy claim 1 , difluoroethoxy claim 1 , trifluoroethoxy claim 1 , phenoxy claim 1 , methylenedioxy claim 1 , difluoromethylenedioxy claim 1 , Calkylsulfonyl claim 1 , di(C)alkylamino claim 1 , Calkylcarbonyl claim 1 , Calkoxycarbonyl and di(C)alkylsulfoximino.4. A compound as claimed in wherein Rrepresents hydrogen claim 3 , halogen claim 3 , cyano claim 3 , Calkyl claim 3 , trifluoromethyl claim 3 , ...
Подробнее