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    • 8. 发明申请
    • PYRROLOPYRIMIDINE COMPOUNDS
    • 吡咯烷酮化合物
    • US20100305143A1
    • 2010-12-02
    • US12677919
    • 2008-09-19
    • Allan JordanSimon BedfordKlenke BurkhardIan YuleKarinne Poullennec
    • Allan JordanSimon BedfordKlenke BurkhardIan YuleKarinne Poullennec
    • A61K31/519C07D487/04A61P29/00A61P3/10A61P35/00A61P11/06A61P11/00
    • C07D487/04
    • Compounds of formula (I) are A2B receptor antagonists: wherein Ri is optionally substituted aryl or an optionally substituted monocyclic heteroaryl group having 5 or 6 ring atoms; R2 and R3 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6)-alkyl; R4 and R5 are independently selected from hydrogen, optionally substituted C1-C6alkyl, optionally substituted aryl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, —NHR7—N(—R8)—R9, —NH—(C═O)—R10, —(C═O)—NH—R11, —(C═O)—O—R12, or halo; R6 is hydrogen, C1-C6 alkyl, aryl-(C1-C6)-alkyl, —(C═O)—NH—R13, —(C═O)—R14, aryl, heteroaryl, hydroxy-(C1-C6)-alkyl, or C3-C8 cycloalkyl-alkyl; and R7, R8, R9, R10, R11, R12, R13 and R14 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.
    • 式(I)化合物是A2B受体拮抗剂:其中R 1是任选取代的芳基或具有5或6个环原子的任选取代的单环杂芳基; R 2和R 3独立地选自氢或任选取代的C 1 -C 6烷基,C 1 -C 6烷氧基 - (C 1 -C 6) - 烷基,C 3 -C 8环烷基,芳基,杂芳基,芳基 - (C 1 -C 6) - 烷基或 杂芳基 - (C 1 -C 6) - 烷基; R 4和R 5独立地选自氢,任选取代的C 1 -C 6烷基,任选取代的芳基,在其环部任选取代的芳基 - (C 1 -C 6) - 烷基,-NHR 7 -N(-R 8)-R 9,-NH- (C = O)-R 10, - (C = O)-NH-R 11, - (C = O)-O-R 12或卤素; R6是氢,C1-C6烷基,芳基 - (C1-C6) - 烷基, - (C = O)-NH-R13, - (C = O)-R14,芳基,杂芳基,羟基 - (C1-C6) - 烷基或C 3 -C 8环烷基 - 烷基; 并且R 7,R 8,R 9,R 10,R 11,R 12,R 13和R 14独立地选自C 1 -C 6烷基,芳基,芳基 - (C 1 -C 6) - 烷基和杂芳基。