REGIOSELECTIVE PREPARATION OF 2-AMINO-5-TRIFLUOROMETHYLPYRIMIDINE DERIVATIVES
    3.
    发明申请
    REGIOSELECTIVE PREPARATION OF 2-AMINO-5-TRIFLUOROMETHYLPYRIMIDINE DERIVATIVES 有权
    2-氨基-5-三氟甲基嘧啶衍生物的选择性制备

    公开(公告)号:US20120172596A1

    公开(公告)日:2012-07-05

    申请号:US13389068

    申请日:2010-08-13

    IPC分类号: C07D239/42 C07D239/34

    摘要: The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula T-H; and reacting the compound obtained with an amine of formula (II) [HN(R1)R2] to form a compound of formula (III) wherein X1, X2, T, R1 and R2 have the meanings as defined herein.

    摘要翻译: 本发明涉及制备式(III)的嘧啶的方法,所述方法包括使式(I)化合物与式T-H的氧,硫或氮亲核试剂反应; 并使所得化合物与式(II)的胺[HN(R 1)R 2]反应形成其中X 1,X 2,T,R 1和R 2具有如本文定义的含义的式(III)化合物。

    Process for the manufacture of fused piperazin-2-one derivatives
    4.
    再颁专利
    Process for the manufacture of fused piperazin-2-one derivatives 有权
    稠合哌嗪-2-酮衍生物的制备方法

    公开(公告)号:USRE43115E1

    公开(公告)日:2012-01-17

    申请号:US12850993

    申请日:2010-08-05

    IPC分类号: C07D475/00 C07D239/30

    CPC分类号: C07D475/00

    摘要: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.

    摘要翻译: 公开了制备通式(I)的稠合哌嗪-2-酮衍生物的方法,其中基团R1至R5,A1和A2具有权利要求书和说明书中给出的含义,特别是7,8- 二氢-5H-蝶啶-6-酮衍生物及其中间体。

    SPECIFIC SALT, ANHYDROUS AND CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE
    9.
    发明申请
    SPECIFIC SALT, ANHYDROUS AND CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE 有权
    二盐酸盐衍生物的特殊盐,无机和结晶形式

    公开(公告)号:US20070203146A1

    公开(公告)日:2007-08-30

    申请号:US11668681

    申请日:2007-01-30

    IPC分类号: A61K31/525 C07D475/08

    CPC分类号: C07D475/00

    摘要: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

    摘要翻译: 本发明涉及二氢二萜二酮衍生物的具体盐,即化合物N- [反式-4- [4-(环丙基甲基)-1-哌嗪基]环己基] -4 - [[(7R)-7 - 乙基-5,6,7,8-四氢-5-甲基-8-(1-甲基乙基)-6-氧代-2-吖啶基]氨基] -3-甲氧基 - 苯甲酰胺,其结晶形式为 水合物,其制备方法及其在药物组合物中的用途。