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Alkylsulfinyl-substituted thiazolide compounds
专利权人:
ROMARK LABORATORIES L.C.
发明人:
SEMPLE J. EDWARD,ROSSIGNOL JEAN-FRANCOIS
申请号:
NZ61141011
公开号:
NZ611410A
申请日:
2011.10.27
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed are 2-hydroxy-N-(5-(methylsulfinyl)thiazol-2-yl)benzamide derivatives and analogues as represented by the general Formula (I), or a pharmaceutically acceptable salt thereof, for treating a subject exposed to a hepatitis C virus infection, wherein R1 is selected from the group consisting of hydrogen and Q-C(=O)-; R2 to R5 are hydrogen; wherein one of R6 or R7 is hydrogen, and the other is independently selected from the group consisting of alkylsulfinyl, alkylsulfinylalkyl, alkenylsulfinyl, alkynylsulfinyl, cycloalkylsulfinyl, cycloalkenylsulfinyl, arylsulfinyl, arylalkylsulfinyl, arylalkenylsulfinyl, heteroarylsulfinyl, heteroarylalkylsulfinyl, heteroarylalkenylsulfinyl, and heterocycloalkylsulfinyl; or the R6 and R7 moieties may be combined together with the atoms to which they are attached and joined to form a 5-to 8-membered ring that incorporates a sulfinyl moiety; and wherein Q is R8, OR8, NHR8, or NR8R9; R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, heterocycloalkyl, heteroaryl, heteroarylalkyl, and heteroarylalkenyl; or R8 and R9, together with the atoms to which they are attached, may be joined to form a 5-to 8-membered heterocycloalkyl ring. Representative compounds of formula (I) include 2-hydroxy-N-(5-(methylsulfinyl)thiazol-2-yl)benzamide, 2-{ [4-(methylsulfinyl)-1,3-thiazol-2-yl]carbamoyl} phenyl acetate, 2-hydroxy-N-[4-(methylsulfinyl)-1,3-thiazol-2-yl]benzamide, 2-hydroxy-N-[5-(ethylsulfinyl)-1,3-thiazol-2-yl]benzamide, 2-hydroxy-N-[5-(cyclohexylsulfinyl)-1,3-thiazol-2-yl]benzamide, 2-hydroxy-N-[5-(phenylsulfinyl)-1,3-thiazol-2-yl]benzamide, 2-hydroxy-N-[5-(benzylsulfinyl)-1,3-thiazol-2-yl]benzamide, isopropyl 2-{ [4-(pyrimidin-2-ylsulfinyl)-1,3-thiazol-2-yl]carbamoyl} phenyl carbonate, 2-{ [5-oxo-4,6-dihydro-thieno[3,4-d]thiazol-2-yl]carbamoyl} phenyl acetate and 2-hydroxy-N-(4-oxo-thieno[2,3-d][1,3]thiazol-2-yl)benzamide.
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