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    PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS
    6.
    发明申请
    PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS 审中-公开
    作为脂质激酶抑制剂的吡唑并嘧啶

    公开(公告)号：US20090286779A1

    公开(公告)日：2009-11-19

    申请号：US12442606

    申请日：2007-09-27

    申请人： Patricia Imbach ,  Frederic Stauffer ,  Pascal Furet ,  Hans-Georg Capraro

    发明人： Patricia Imbach ,  Frederic Stauffer ,  Pascal Furet ,  Hans-Georg Capraro

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  C07D401/12 ,  C07D413/14 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： The invention relates to novel—at least 3,5-disubstituted-pyrazolo[1,5-a]pyrimidines of the formula I, wherein the symbols R1 to R4 are as defined in the specification, tautomers thereof or N-oxides thereof, or (preferably pharmaceutically acceptable) salts thereof, or hydrates or solvates thereof, as well as to related embodiments. The compounds are useful inter alia as protein kinase inhibitors, and thus e.g. useful in the treatment of diseases that respond to an inhibition of kinases of the PI3-kinase-related protein kinase family, especially lipid kinases and/or PI3 kinase (PI3K) and/or mTOR and/or DNA protein kinase and/or ATM and/or ATR and/or hSMG-1.

    摘要翻译： 本发明涉及式I的至少3,5-二取代 - 吡唑并[1,5-a]嘧啶，其中符号R1至R4如本说明书中所定义，其互变异构体或其N-氧化物，或 （优选药学上可接受的）盐，或其水合物或溶剂化物，以及相关实施方案。 所述化合物尤其可用作蛋白激酶抑制剂， 可用于治疗响应抑制PI3激酶相关蛋白激酶家族，特别是脂质激酶和/或PI3激酶（PI3K）和/或mTOR和/或DNA蛋白激酶和/或ATM的激酶的疾病，以及 /或ATR和/或hSMG-1。

    2-amino-6-anilino-purines and their use as medicaments
    8.
    发明授权
    2-amino-6-anilino-purines and their use as medicaments 失效
    2-氨基-6-苯胺基嘌呤及其作为药物的用途

    公开(公告)号：US06767906B2

    公开(公告)日：2004-07-27

    申请号：US09927322

    申请日：2001-08-10

    申请人： Patricia Imbach ,  Hans-Georg Capraro ,  Jürg Zimmermann ,  Giorgio Caravatti ,  Pascal Furet ,  Wolfgang Karl-Diether Brill

    发明人： Patricia Imbach ,  Hans-Georg Capraro ,  Jürg Zimmermann ,  Giorgio Caravatti ,  Pascal Furet ,  Wolfgang Karl-Diether Brill

    IPC分类号： C07D47316

    CPC分类号： C07D473/16 ,  C07D473/40

    摘要： This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is &agr;) —S(═O)k—NR6R7, in which  k is 1 or 2,  wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen &agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or &agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, &bgr;) N-(aryl lower alkyl)carbamoyl, or &ggr;) a radical of the formula —NH—S(═O)i—R8, in which  i is 1 or 2,  R8 is an aliphatic, carbocyclic or heterocyclic radical; or &dgr;) a radical of the formula —NH—C(═O)—R9,  and the other variable substituents are as defined herein. The inventive compounds inhibit p34cdc2/cyclin Bcdc13 kinase and protein tyrosine kinase pp60c-src and can be used for treatment of hyperproliferative diseases, for example tumour diseases, and diseases which respond to inhibition of the activity of protein tyrosine kinase pp60c-src, in particular osteoporosis.

    摘要翻译： 本申请公开了式Iin的2-氨基-6-苯胺基 - 嘌呤衍生物，其中q是1-5，和R1是α）-S（= O）k-NR6R7，其中k是1或2，其中在条件是R6和 R7不能同时为氢α1）R6，R7可以相同或不同，代表脂族，碳环，杂环，碳环脂族或杂环脂族基; 氢或低级脂族酰基; 口服α2）R6和R7一起是具有3个至多且包括9个C原子的亚烷基或亚烯基，其中1-3个C原子可以被氧，硫或氮取代，β）N-（芳基低级烷基）氨基甲酰基 （= O）i-R8的基团，其中i为1或2，R8为脂族，碳环或杂环基; 顺式）式-NH-C（= O）-R9的基团，其它可变取代基如本文所定义。 本发明化合物抑制p34 /细胞周期蛋白B 激酶和蛋白酪氨酸激酶pp60 ，并且可用于治疗过度增殖性疾病，例如肿瘤疾病和对抑制活性的疾病 蛋白酪氨酸激酶pp60 ，特别是骨质疏松症。