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    Pyrazolo[1,5-a]-1,3,5-triazine derivatives, preparation thereof, and therapeutic use thereof
    3.
    发明授权
    Pyrazolo[1,5-a]-1,3,5-triazine derivatives, preparation thereof, and therapeutic use thereof 有权
    吡唑并[1,5-a] -1,3,5-三嗪衍生物及其治疗用途

    公开(公告)号：US08691982B2

    公开(公告)日：2014-04-08

    申请号：US13203427

    申请日：2010-03-11

    申请人： Laurent Meijer ,  Hervé Galons ,  Benoit Joseph ,  Florence Popowycz ,  Nassima Oumata

    发明人： Laurent Meijer ,  Hervé Galons ,  Benoit Joseph ,  Florence Popowycz ,  Nassima Oumata

    IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    PYRAZOLO[1,5-A]-1,3,5-TRIAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    5.
    发明申请
    PYRAZOLO[1,5-A]-1,3,5-TRIAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权
    吡咯并[1,5-A] -1,3,5-三嗪衍生物，其制备方法及其治疗方法

    公开(公告)号：US20120184557A1

    公开(公告)日：2012-07-19

    申请号：US13203427

    申请日：2010-03-11

    申请人： Laurent Meijer ,  Hervé Galons ,  Benoit Joseph ,  Florence Popowycz ,  Nassima Oumata

    发明人： Laurent Meijer ,  Hervé Galons ,  Benoit Joseph ,  Florence Popowycz ,  Nassima Oumata

    IPC分类号： A61K31/53 ,  A61P35/00 ,  A61P25/28 ,  A61P25/08 ,  A61P29/00 ,  A61P33/00 ,  A61P31/12 ,  A61P31/14 ,  A61P3/10 ,  A61P25/00 ,  A61P13/12 ,  C07D487/04 ,  A61P19/02

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。