Biphenyl derivatives, production thereof and uses as medicines
    16.
    发明授权
    Biphenyl derivatives, production thereof and uses as medicines 有权
    联苯衍生物,其生产和用途作为药物

    公开(公告)号:US06617325B1

    公开(公告)日:2003-09-09

    申请号:US10031585

    申请日:2002-05-15

    IPC分类号: A01N4366

    CPC分类号: C07D211/58

    摘要: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.

    摘要翻译: 本发明涉及通用化学式R a至R g的联苯基衍生物,n如权利要求1中所定义,它们是微粒体甘油三酯转移蛋白(MTP)的有价值的抑制剂的异构体和盐,特别是其生理上可接受的盐,药物 含有这些化合物及其用途以及其制备方法。

    Substituted indolinones with kinase inhibitory activity
    17.
    发明授权
    Substituted indolinones with kinase inhibitory activity 有权
    具有激酶抑制活性的取代的吲哚啉酮

    公开(公告)号:US06319918B1

    公开(公告)日:2001-11-20

    申请号:US09323499

    申请日:1999-06-01

    IPC分类号: A61K3155

    CPC分类号: C07D209/30 C07D209/34

    摘要: Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.

    摘要翻译: 通用结构式取代的吲哚酮对各种激酶和cyclin / CDK复合物的影响以及各种肿瘤细胞的增殖。 示例性化合物是:3-Z- [1-(4-(N-苄基-N-甲基 - 氨基甲基) - 苯基氨基)-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮和3-Z- [1- (4-(2,3,4,5-四氢 - 苯并(d)氮杂-3-基 - 甲基) - 苯基氨基)-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮。

    8-alkylthio-2-piperazino-pyrimido[5,4-d]-pyrimidines
    20.
    发明授权
    8-alkylthio-2-piperazino-pyrimido[5,4-d]-pyrimidines 失效
    8-烷硫基-2-哌嗪基 - 嘧啶并[5,4-d] - 嘧啶

    公开(公告)号:US4714698A

    公开(公告)日:1987-12-22

    申请号:US745095

    申请日:1985-06-17

    CPC分类号: C07D487/04

    摘要: The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.The new compounds may be prepared according to methods known for analogous compounds.

    摘要翻译: 本发明涉及通式(I)的新化合物,其中R 1表示烷基,R 2表示氢原子,任选被羟基取代的烷基(除了在α碳原子上),或表示环烷基 基团或烯丙基,苯基或苄基,R 3表示烯丙基,任选被羟基取代的烷基(除了在α碳原子上),或表示环烷基或R 2和R 3以及它们之间的氮原子 代表直链亚烷基亚氨基,其酸加成盐,特别是其酸加成盐与具有有价值的药理学性质的生理上可接受的无机或有机酸,特别是基于其选择性肿瘤-PDE抑制作用的转移抑制作用,以及 含有这些化合物的药物组合物或其生理上可接受的酸加成盐。 新化合物可以根据类似化合物已知的方法制备。