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    • 6. 发明授权
    • 2-amino-6-anilino-purines and their use as medicaments
    • 2-氨基-6-苯胺基嘌呤及其作为药物的用途
    • US06767906B2
    • 2004-07-27
    • US09927322
    • 2001-08-10
    • Patricia ImbachHans-Georg CapraroJürg ZimmermannGiorgio CaravattiPascal FuretWolfgang Karl-Diether Brill
    • Patricia ImbachHans-Georg CapraroJürg ZimmermannGiorgio CaravattiPascal FuretWolfgang Karl-Diether Brill
    • C07D47316
    • C07D473/16C07D473/40
    • 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.
    • 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。