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    • 3. 发明专利
    • Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
    • NZ628969A
    • 2017-03-31
    • NZ62896913
    • 2013-02-14
    • MILLENNIUM PHARM INC
    • AFROZE ROUSHANBHARATHAN INDU TCIAVARRI JEFFREY PFLEMING PAUL EGAULIN JEFFREY LGIRARD MARIOLANGSTON STEVEN PSOUCY FRANCOIS RWONG TZU-TSHINYE YINGCHUN
    • C07B45/04A61K31/4162A61K31/519A61P35/00C07D487/04C07H5/04
    • Disclosed are { 2,3-dihydroxy-4-[(2-aryl-pyrazolo[1,5-a]pyrimidin-7-yl)amino]cyclopentyl} methyl sulfamate derivatives as represented by the general formula (I) as the depicted single stereochemical isomer, or as an enantiomeric, racemic, or disatereomeric mixture of the depicted single stereochemical isomer; and pharmaceutically acceptable salts of any of the foregoing, wherein: W is -N(R*3)-; Y is pyrazolo[1,5-a]pyrimidin-7-yl substituted in positions 2 with the group Z; wherein Z is an optionally substituted aryl, an optionally substituted fused aryl: or an optionally substituted heteroaryl; and wherein the remaining substituents are as defined herein. Representative compounds include (2,3-dihydroxy-4-(2-(3-(trifluoromethylthio)phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate as either a racemate or single enantiomer (s.e.), ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-phenylpyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate, ((1R,2R,3S,4R)-2,3-dihydroxy-4-{ [2-(1-naphthyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino} cyclopentyl)methyl sulfamate, ((1R,2R,3S,4R)-4-(2-(3,3-dimethyl-2,3-dihydrobenzofuran-7-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)-2,3-dihydroxycyclopentyl)methyl sulfamate, ((1R,2R,3S,4R)-4-(5-chloro-2-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)-2,3-dihydroxycyclopentyl)methyl sulfamate and ((1R,2R,3S,4R)-4-(2-(dibenzo[b,d]furan-4-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)-2,3-dihydroxycyclopentyl)methyl sulfamate. Also disclosed is a pharmaceutical composition comprising, a compound as defined above and a pharmaceutically acceptable carrier, for use in treating lung cancer, ovarian cancer, colon cancer, breast cancer, or lymphoma.