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    2-amino-6-anilino-purines and their use as medicaments
    6.
    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。