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    • 8. 发明授权
    • Adenosine A2a receptor antagonists
    • 腺苷A2a受体拮抗剂
    • US07041666B2
    • 2006-05-09
    • US10304504
    • 2002-11-26
    • Julius J. MatasiJohn P. CaldwellDeen TulshianLisa S. SilvermanBernard R. Neustadt
    • Julius J. MatasiJohn P. CaldwellDeen TulshianLisa S. SilvermanBernard R. Neustadt
    • C07D487/04A61K31/519A61P25/18A61P25/16A61P25/28
    • C07D487/04
    • Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, or —CH═CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
    • 公开了具有结构式或其药学上可接受的盐或溶剂化物的化合物,其中R是任选取代的杂芳基,任选取代的苯基,环烯基,-C(-CH 2 CH 2)CH 3 ,-C≡C-CH 3,-CH-C(CH 3)2,或-CH-CH-CH 3 ; R 2是-WX,-NR 19(CH 2)2 -WX和-NR O SUP CH 3(CH 3 CH 3)-WX或R 2是烷基,烯基和-NR 18 R 12, 19,每个任选取代的-WX; R 3是H,卤素,烷基,三氟甲基,烷氧基,烷氧基烷基,羟基烷基,烷基氨基,烷基氨基烷基,二烷基氨基,二烷基氨基烷基,氨基烷基,芳基,杂芳基或CN; -CH(OH) - , - CH(CH 3) - , - (CH 3 CH 3) - , - (CH 3 CH 3) n - - (CH 2)n - 或 - (CH 2)n - / > - ; W是芳基或杂芳基,各自任选被取代; X是H,NH 2或取代的氨基,或X是-R 18 -Y-Z; 和n,R 19,Y和Z如说明书中所定义; 其药物组合物,以及通过将本发明化合物给予需要这种治疗的患者来治疗中风或中枢神经系统疾病的方法。