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    • 4. 发明授权
    • Pyrazolo[1,5-a]-1,3,5-triazine derivatives, preparation thereof, and therapeutic use thereof
    • 吡唑并[1,5-a] -1,3,5-三嗪衍生物及其治疗用途
    • US08691982B2
    • 2014-04-08
    • US13203427
    • 2010-03-11
    • Laurent MeijerHervé GalonsBenoit JosephFlorence PopowyczNassima Oumata
    • Laurent MeijerHervé GalonsBenoit JosephFlorence PopowyczNassima Oumata
    • C07D487/04A61K31/53A61P35/00
    • C07D487/04
    • A compound of formula (I), or a pharmaceutically acceptable salt thereof, where R1 is a (C1-C6)alkyl or (C3-C6)cycloalkyl group; R2 is a (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkenyl, (C1-C6)fluoroalkyl, (C1-C3)fluoroalkoxy, or (C1-C6)alkoxy(C1-C6)alkyl group, substituted: (i) with one to three hydroxyl groups, or (ii) with an NRaRb group, where Ra and Rb are independently a hydrogen atom or a (C1-C3)alkyl group; or a pyrrolidinylmethyl group substituted with one to three hydroxyl groups; R9 is the same as R2 or hydrogen; the R2 and R9 groups independently being substitutable with an —OCOR3 group, where R3 is a natural or unnatural amino acid derivative or a piperidyl group; alternatively, R2 and R9 together form a heterocyclic compound; X and Y are independently a substitutable phenyl or heteroaryl group, the heteroaryl group being a thienyl, pyridyl, pyrimidinyl, thiazolyl, pyrrolyl, or furanyl group; and R6 is a hydrogen or a (C1-C3)alkyl group.
    • 式(I)化合物或其药学上可接受的盐,其中R 1是(C 1 -C 6)烷基或(C 3 -C 6)环烷基; R2是(C1-C6)烷基,(C3-C6)环烷基,(C1-C6)烯基,(C1-C6)氟烷基,(C1-C3)氟烷氧基或(C1-C6)烷氧基(C1-C6) 烷基,取代:(i)具有一至三个羟基,或(ii)与NR a R b基团,其中R a和R b独立地是氢原子或(C 1 -C 3)烷基; 或被一至三个羟基取代的吡咯烷基甲基; R9与R2或氢相同; R 2和R 9独立地可以被-OCOR 3基团取代,其中R 3是天然或非天然氨基酸衍生物或哌啶基; 或者,R2和R9一起形成杂环化合物; X和Y独立地是可取代的苯基或杂芳基,杂芳基是噻吩基,吡啶基,嘧啶基,噻唑基,吡咯基或呋喃基; R6为氢或(C1-C3)烷基。