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    • 5. 发明申请
    • Huperzine a compound for treatment of Alzheimer's disease
    • 石杉碱是治疗阿尔茨海默病的化合物
    • US20070270454A1
    • 2007-11-22
    • US11798886
    • 2007-05-17
    • On LeeJenn-Tsang HwangChrong-Shiong HwangWan-Hsu YangChung YaoYuan-Jang TsaiChih LiuTsan HuChia-Mu TuPean-Jyy Jih
    • On LeeJenn-Tsang HwangChrong-Shiong HwangWan-Hsu YangChung YaoYuan-Jang TsaiChih LiuTsan HuChia-Mu TuPean-Jyy Jih
    • C07D221/22A61K31/473
    • C07D221/22
    • A huperzine A compound is provided. The huperzine A compound has following formula: wherein X comprises O or S, Y comprises —O—, —S—, —CH(R4)—, —C(R4)(R5)—, —C(R4)═C(R5)—, —C≡C—, —NH— or —N(R4)—, n is 0, 1 or 2, R3 is C(═X)—(Y)n-R1 provided that R2 is H or R2 and R3 are combined to form ═CH—Ar, wherein R1, R4 and R5 independently comprise hydrogen, C1-C32 alkyl, C1-C32 alkenyl, C1-C32 alkynyl, C1-C32 aryl or C1-C32 heteroaryl, in which alkyl, alkenyl, alkynyl, aryl or heteroaryl with one or more substituents comprising halogen, hydroxyl, alkoxy, aryloxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, imino, alkylimino, arylimino, acylamido, diacylamido, acylimido, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, thio, sulfonyl or sulfinyl, and Ar comprises aryl or heteroaryl.
    • 提供一种石杉碱化合物。 石杉碱A化合物具有下式:其中X包含O或S,Y包括-O - , - S - , - CH(R 4) - , - C(R 4) (R 5) - , - C(R 4) - C(R 5) - , - C≡C-, -NH-或-N(R 4) - ,n为0,1或2,R 3为C(-X) - (Y)n 条件是R 2是H或R 2和R 3 3被组合成 形式-CH-Ar,其中R 1,R 4和R 5独立地包含氢,C 1〜 C 32烷基,C 1 -C 32烯基,C 1 -C 32亚烷基 炔基,C 1 -C 32芳基或C 1 -C 32杂芳基,其中烷基,烯基 羟基,烷氧基,芳氧基,氨基,烷基氨基,芳基氨基,二烷基氨基,二芳基氨基,亚氨基,亚氨基亚氨基,芳基亚氨基,酰氨基,二酰氨基,酰基亚氨基,氰基,硝基,巯基, 氨基甲酰基,羧基,硫脲基,硫氰基 亚磺酰氨基,硫代,磺酰基或亚磺酰基,Ar包括芳基或杂芳基。
    • 9. 发明授权
    • Piperazinedione compounds
    • 哌嗪二酮化合物
    • US06635649B2
    • 2003-10-21
    • US09851077
    • 2001-05-08
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • A61K31496
    • C07D401/06C07D409/14
    • Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.
    • 哌嗪二酮化合物,分别为:< CUSTOM-CHARACTER FILE =“US06635649-20031021-P00900.TIF”ALT =“custom character”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/ >和 或双键; 当是单键,或C(R a R b)当为双键时; 当是单键或C(R )”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00005”/>是双键; Ar是杂芳基; 且R 3为H,烷基,芳基,杂芳基,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R d; R 1和R 2各自独立地是H,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R ; R a,R b,R c,R d和R e各自独立地是H,烷基,芳基,杂芳基,环基或杂环基。 任选地,R 5和R b一起是环基或杂环基; 并且还可任选地,R 1和R 5'或R 1和R b一起是环基或杂环基。 还公开了用上述哌嗪二酮化合物治疗肿瘤的方法。