Organic Compounds
    26.
    发明申请
    Organic Compounds 审中-公开
    有机化合物

    公开(公告)号:US20090069360A1

    公开(公告)日:2009-03-12

    申请号:US12293257

    申请日:2007-03-14

    CPC分类号: C07D401/04

    摘要: The present invention relates to the discovery that certain compounds inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway, and is concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy.

    摘要翻译: 本发明涉及某些化合物抑制,调控和/或调节酪氨酸和丝氨酸/苏氨酸激酶和激酶样蛋白质,例如在MAP激酶信号通路中起作用的丝氨酸/苏氨酸激酶的RAF激酶,并且是 涉及含有这些化合物的组合物,以及使用它们治疗酪氨酸和丝氨酸/苏氨酸激酶和激酶样依赖性疾病如血管生成,癌症和心脏肥大的方法。

    7H-pyrrolo[2,3-d]pyrimidine derivatives
    27.
    发明授权
    7H-pyrrolo[2,3-d]pyrimidine derivatives 失效
    7H-吡咯并[2,3-d]嘧啶衍生物

    公开(公告)号:US07323469B2

    公开(公告)日:2008-01-29

    申请号:US10783000

    申请日:2004-02-20

    CPC分类号: C07D487/04

    摘要: The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.

    摘要翻译: 本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物,其中符号和取代基如说明书中所定义,其制备方法,包含该衍生物的药物组合物及其用途 衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

    2-amino-6-anilino-purines and their use as medicaments
    29.
    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

    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。