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    • 6. 发明申请
    • NAD+-dependent DNA ligase inhibitors
    • NAD +依赖性DNA连接酶抑制剂
    • US20070082920A1
    • 2007-04-12
    • US11244614
    • 2005-10-06
    • Yongsheng SongYongchun HouSandeep GuptaAimee ReedDebasis Ghosh
    • Yongsheng SongYongchun HouSandeep GuptaAimee ReedDebasis Ghosh
    • A61K31/519C07D487/02
    • C07D487/02
    • Disclosed herein are pyrido[2,3-d]pyrimidines having the structure wherein R1, and R2 are independently selected from nitro and amino; wherein R3 is selected from alkyl (C1-C10) and cycloalkyl (C3-C8); wherein R4 is selected from hydrogen, benzyl, alkyl (C1-C10), cycloalkyl (C3-C8), arylalkyl (C4-C8), and aryl (C3-C8); wherein R5 and R6 are independently selected from hydrogen, benzyl, alkyl (C1-C10), cycloalkyl (C3-C8), arylalkyl (C4-C14), and aryl (C3-C8); wherein R3 and R4 may form a ring; wherein R5 and R6 may form a ring or a heterocyclic structure; and wherein R5 and R6 are independently unsubstituted or substituted, wherein each substituent is independently selected from halogen, amino, alkyl (C1-C6), haloalkyl (C1-C6), alkoxy(C1-C6), alkylenedioxy, aryl, heteroaryl, and cycloalkyl (C3-C8). Also disclosed are methods for the preparation of compounds of Formula I and various intermediates. These compounds are useful as NAD+-dependent DNA ligase inhibitors.
    • 本文公开了具有其中R 1,R 2和R 2独立地选自硝基和氨基的结构的吡啶并[2,3-d]嘧啶; 其中R 3选自烷基(C 1 -C 10)和环烷基(C 3 -C 8); 其中R 4选自氢,苄基,烷基(C1-C10),环烷基(C3-C8),芳基烷基(C4-C8)和芳基(C3-C8); 其中R 5和R 6独立地选自氢,苄基,烷基(C1-C10),环烷基(C3-C8),芳基烷基(C4-C14)和 芳基(C3-C8); 其中R 3和R 4可以形成环; 其中R 5和R 6可以形成环或杂环结构; 并且其中R 5和R 6独立地是未取代的或取代的,其中每个取代基独立地选自卤素,氨基,烷基(C 1 -C 6),卤代烷基(C 1 -C 6 ),烷氧基(C1-C6),亚烷基二氧基,芳基,杂芳基和环烷基(C3-C8)。 还公开了制备式I化合物和各种中间体的方法。 这些化合物可用作NAD +依赖性DNA连接酶抑制剂。