4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives
    4.
    发明授权
    4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives 失效
    4-氨基-6-苯基 - 吡咯并[2,3-d]嘧啶衍生物

    公开(公告)号:US07390805B2

    公开(公告)日:2008-06-24

    申请号:US11686023

    申请日:2007-03-14

    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 tumour.

    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。

    Pyrimidine derivatives and processes for the preparation thereof
    5.
    发明授权
    Pyrimidine derivatives and processes for the preparation thereof 失效
    嘧啶衍生物及其制备方法

    公开(公告)号:US06251911B1

    公开(公告)日:2001-06-26

    申请号:US09269823

    申请日:1999-04-01

    IPC分类号: C07D48704

    CPC分类号: C07D487/04

    摘要: 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I wherein the substituents are as defined in claim 1, are described. These compounds inhibit the tyrosine kinase activity of the receptor for epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.

    摘要翻译: 描述了在取代基中如权利要求1所定义的式I的4-氨基-1H-吡唑并[3,4-d]嘧啶衍生物。这些化合物抑制表皮生长因子(EGF)和c的受体的酪氨酸激酶活性 -erbB2激酶,可用作抗肿瘤剂。

    Novel polycyclic hydrazones of rifamycins, their manufacture, and their
pharmaceutical compositions for treating tuberculosis
    6.
    发明授权
    Novel polycyclic hydrazones of rifamycins, their manufacture, and their pharmaceutical compositions for treating tuberculosis 失效
    利福霉素的新型多环腙,其制造及其用于治疗结核病的药物组合物

    公开(公告)号:US4681938A

    公开(公告)日:1987-07-21

    申请号:US763725

    申请日:1985-08-08

    申请人: Peter Traxler

    发明人: Peter Traxler

    摘要: Novel hydrazones derived from 3-formylrifamycin S or SV as the aldehydo component and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, independently of one another, each represents a hydrogen atom or C.sub.1-4 -alkyl,m and n, independently of one another, each represents an integer from 0 to 5,X represents C.sub.1-5 -alkylidene, benzylidene or C.sub.1-4 -alkoxymethylene,Y represents C.sub.1-5 -alkylidene, C.sub.1-4 -alkoxymethylene, oxy, thio or optionally substituted imino of the formula --N(R)-- wherein R represents hydrogen, C.sub.1-4 -alkyl, C.sub.3-5 -alkenyl, C.sub.3-12 -cycloalkyl or phenyl, orX and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C.sub.1-4 -alkyl radicals, andRif represents a radical of rifamycin S or SV that is bonded in the 3-position by the free valency,are distinguished by a high and long-lasting antituberculotic activity. They are manufactured in conventional manner, for example by condensation of their components.

    摘要翻译: 衍生自作为醛组分的3-甲酰基叶绿素S或SV的新型腙和作为肼基组分的双环或三环N-氨基哌嗪,并具有式(Ⅰ)的R1,R2,R3,R4,R5 和R 6彼此独立地表示氢原子或C 1-4 - 烷基,m和n彼此独立地表示0-5的整数,X表示C1-5亚烷基,亚苄基或C1- 4-烷氧基亚甲基,Y代表C1-5亚烷基,C1-4烷氧基亚甲基,氧基,硫代或式-N(R) - 的任选取代的亚氨基,其中R表示氢,C 1-4 - 烷基,C 3-5 - 烯基 ,C 3-8 - 环烷基或苯基,或X和Y一起代表1,2-亚环烷基或邻亚苯基,其各自可被一至三个C 1-4 - 烷基取代,Rif代表利福霉素S 或通过自由价键合在3位上的SV被高度和持久的抗结核活性区分。 它们以常规方式制造,例如通过其组分的冷凝。

    7H-pyrrolo[2,3-d]pyrimidine derivatives
    7.
    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。

    Protein kinase inhibitors
    8.
    发明申请
    Protein kinase inhibitors 审中-公开
    蛋白激酶抑制剂

    公开(公告)号:US20070149535A1

    公开(公告)日:2007-06-28

    申请号:US11635908

    申请日:2006-12-08

    IPC分类号: A61K31/498

    CPC分类号: A61K31/519 A61K31/695

    摘要: The present invention relates to angiogenesis inhibitors, in particular receptor tyrosine kinase inhibitors, and their use for the treatment of hyperproliferative diseases, angiogenesis and disorders depending on angiogenesis such as tumour forming cancers. It also relates to a method of inhibiting angiogenesis or treating a vascular anomaly in a mammal comprising administering to the mammal an amount of an Eph receptor inhibitor which is effective for inhibiting angiogenesis or for treating the vascular anomaly in the mammal. Further, the present invention relates to the use of compounds for the treatment of angiogenesis related disorders involving a protein kinase, preferably a tyrosine kinase, and to some specific forms of said compounds as a medicament. Compounds useful in the practice of the invention have the general formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification.

    摘要翻译: 本发明涉及血管生成抑制剂,特别是受体酪氨酸激酶抑制剂,以及它们用于治疗过度增殖性疾病,血管生成和取决于血管发生如肿瘤形成癌症的病症的用途。 它还涉及抑制哺乳动物血管生成或治疗血管异常的方法,其包括向哺乳动物施用一定量的有效抑制血管发生或治疗哺乳动物血管异常的Eph受体抑制剂。 此外,本发明涉及化合物用于治疗涉及蛋白激酶(优选酪氨酸激酶)的血管发生相关疾病以及作为药物的所述化合物的一些特定形式的用途。 可用于本发明实践的化合物具有通式I,其中R 1,R 2,R 3,R 4和R 5如说明书中所定义。