SPECIFIC SALT, ANHYDROUS AND CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE
    5.
    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:US20120214995A1

    公开(公告)日:2012-08-23

    申请号:US13457991

    申请日:2012-04-27

    IPC分类号: C07D475/06

    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。

    CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE
    6.
    发明申请
    CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE 有权
    二氢异氰酸酯衍生物的结晶形式

    公开(公告)号:US20100280037A1

    公开(公告)日:2010-11-04

    申请号:US12670714

    申请日:2008-08-01

    CPC分类号: C07D475/00

    摘要: The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base 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 a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

    摘要翻译: 本发明涉及结晶形式的二氢啶二酮衍生物,即游离碱N- [反式-4- [4-(环丙基甲基)-1-哌嗪基]环己基] -4 - [[(R)-7- - 乙基-5,6,7,8-四氢-5-甲基-8-(1-甲基乙基)-6-氧代-2-蝶啶基]氨基] -3-甲氧基 - 苯甲酰胺制备其制备方法, 以及其在药物组合物中的用途。

    Process for preparing amino crotonyl compounds
    9.
    发明申请
    Process for preparing amino crotonyl compounds 审中-公开
    制备氨基巴豆酰化合物的方法

    公开(公告)号:US20050085495A1

    公开(公告)日:2005-04-21

    申请号:US10941116

    申请日:2004-09-15

    CPC分类号: C07D405/12

    摘要: The invention relates to an improved process for preparing 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylam ino)-1 -oxo-2-buten-1 -yl]am ino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline and related aminocrotonyl compounds and the preparation of a suitable salt of 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1 -oxo-2-buten-1 -yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline for use as a pharmaceutically active substance.

    摘要翻译: 本发明涉及一种制备4 - [(3-氯-4-氟苯基)氨基] -6 - {[4-(N,N-二甲基氨基)-1-氧代-2-丁烯-1-基 ] - ((S) - 四氢呋喃-3-基氧基) - 喹唑啉和相关的氨基巴豆基化合物,并制备合适的4 - [(3-氯-4-氟苯基)氨基] -6- { 用于药物活性物质的[4-(N,N-二甲基氨基)-1-氧代-2-丁烯-1-基]氨基} -7 - ((S) - 四氢呋喃-3-基氧基) - 喹唑啉。