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公开(公告)号:US06413938B1
公开(公告)日:2002-07-02
申请号:US09367260
申请日:1999-08-25
申请人: Jeffrey H. Tidwell , Stanley D. Chamberlain , George A. Freeman , Joseph H. Chan , George W. Koszalka , Leroy B. Townsend , John C. Drach
发明人: Jeffrey H. Tidwell , Stanley D. Chamberlain , George A. Freeman , Joseph H. Chan , George W. Koszalka , Leroy B. Townsend , John C. Drach
IPC分类号: A61K3170
CPC分类号: C07H19/052 , A61K31/7056 , Y10S514/934
摘要: According to a first aspect of the invention there is provided compounds of formula (I): wherein: R1 is hydroxy; O-acetyl; or a halo atom; R2 is hydroxy; O-acetyl; or a halo atom; R3 is hydrogen; a halo atom; azido; C2-6alkenyl; C2-6alkynyl; C6-14aryl C2-6alkenyl; C6-14arylC2-6alkynyl —NR8R9 (where R8 and R9 may be the same or different and are hydrogen, C1-8alkyl, cyanoC1-8alkyl, hydroxyC1-8alkyl, haloC1-8alkyl, C3-7cycloalkyl, C1-8alkylC3-7cycloalkyl, C2-6alkenyl, C3-7cycloalkylC1-8alkyl, C2-6alkynyl, C6-14aryl, C6-14arylC1-8alkyl, heterocycleC1-8alkyl, C1-8alkylcarbonyl, C6-14arylsulfonyl, C1-8alkysulfonyl, or R8R9 together with the N atom to which they are attached form a 3,4,5 or 6 membered heterocyclic ring); —OR10 (where R10 is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl, C2-6alkenyl, C2-6alkynyl, C6-14aryl C2-6alkenyl or C6-14arylC2-6alkynyl); or —SR11 (where R11 is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl).
摘要翻译: 根据本发明的第一方面,提供式(I)的化合物:其中:R 1是羟基; O-乙酰基; 或卤原子; R 2为羟基; O-乙酰基; 或卤素原子; R 3是氢; 卤素原子 叠氮 C2-6烯基; C 2-6炔基; C6-14芳基C2-6烯基; C 6-14芳基C 2-6炔基-NR 8 R 9(其中R 8和R 9可以相同或不同,为氢,C 1-8烷基,氰基C 1-8烷基,羟基C 1-8烷基,卤代C 1-8烷基,C 3-7环烷基,C 1-8烷基C 3-7环烷基, C 1-6烷基,C 3-7环烷基C 1-8烷基,C 2-6炔基,C 6-14芳基,C 6-14芳基C 1-8烷基,杂环C 1-8烷基,C 1-8烷基羰基,C 6-14芳基磺酰基,C 1-8炔基磺酰基或R 8 R 9与它们所连接的N原子一起 形成3,4,5或6元杂环); -OR 10(其中R 10是氢,C 1-8烷基,C 6-14芳基或C 6-14芳基C 1-8烷基,C 2-6烯基,C 2-6炔基,C 6-14芳基C 2-6烯基或C 6-14芳基C 2-6炔基); 或-SR 11(其中R 11是氢,C 1-8烷基,C 6-14芳基或C 6-14芳基C 1-8烷基)。