| 摘要 |
Disclosed are pyrazolo[1,5-a]pyrimidine derivatives as represented by the general formulae I or II or a pharmaceutically acceptable salt or ester, thereof; wherein: A is –(C(R4)2)n- wherein any one C(R4)2 may be optionally replaced with -O-, -S-, -S(O)p-, NH or NRa; n is 3, 4, 5 or 6; Ar is an optionally substituted heterocyclyl or aryl group; X is C(R13)(R14), N(CH2R14) or X is absent; Y is N or CR7; and wherein the remaining substituents are as defined herein. Representative compounds include N-(4-chloro-2-(((S)-2-(5-((S)-3-aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)-piperidin-1-yl)carbonyl)-phenyl) methanesulphonamide, N-(4-chloro-2-(((S)-2-(5-(azetidin-1-yl)-7-(morpholin-4-yl)-pyrazolo[1,5-a]pyrimidin-2-yl)-piperidin-1-yl)carbonyl)-phenyl) methanesulphonamide, N-(4-chloro-2-(((S)-2-(5-(3-hydroxyazetidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)-piperidin-1-yl)carbonyl)-phenyl) methanesulphonamide and N-(4-chloro-2-(((S)-2-(5-(3-cyano-4-hydroxypyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)-piperidin-1-yl)carbonyl)-phenyl) methanesulphonamide. Also disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above, or a pharmaceutically acceptable salt or ester thereof and a pharmaceutically acceptable carrier for the therapeutic or prophylactic treatment of a Pneumovirinae virus infection or a respiratory syncytial virus infection. |
