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    Synthetic rigidin analogues as anticancer agents, salts, solvates and prodrugs thereof, and method of producing same
    23.
    发明授权
    Synthetic rigidin analogues as anticancer agents, salts, solvates and prodrugs thereof, and method of producing same 有权
    作为抗癌剂，其盐，溶剂化物和前体药物的合成嘧啶类似物及其制备方法

    公开(公告)号：US09334280B2

    公开(公告)日：2016-05-10

    申请号：US14584929

    申请日：2014-12-29

    申请人： New Mexico Technical Research Foundation

    发明人： Igor V. Magedov ,  Snezna Rogelj ,  Liliya V Frolova ,  Alexander Vladimir Kornienko

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： A compound having the Formula as follows: wherein R, R1 and R2 are selected from hydrogen, aryl, fused aryl, heteroaryl, saturated carbocylclic, partially saturated carbocyclic, saturated heterocyclic, partially saturated heterocyclic, C1-10 alkyl, haloalkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, alkenylalkyl, alkynylalkyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitroalkyl, cyanoalkyl, acetamidoalkyl, and acyloxyalkyl. A process for the preparation thereof is also provided.

    摘要翻译： 具有下式的化合物：其中R 1，R 2和R 2选自氢，芳基，稠合芳基，杂芳基，饱和碳环，部分饱和碳环，饱和杂环，部分饱和杂环，C 1-10烷基，卤代烷基，烯基，炔基 芳基烷基，芳基烯基，芳基炔基，杂芳基烷基，杂芳基烯基，烯基烷基，炔基烷基，碳环烷基，杂环烷基，羟基烷基，氨基烷基，羧基烷基，硝基烷基，氰基烷基，乙酰氨基烷基和酰氧基烷基。 还提供了其制备方法。

    Inhibitors of Bruton's tyrosine kinase
    28.
    发明授权
    Inhibitors of Bruton's tyrosine kinase 有权
    Bruton酪氨酸激酶抑制剂

    公开(公告)号：US09181257B2

    公开(公告)日：2015-11-10

    申请号：US14080640

    申请日：2013-11-14

    申请人： Pharmacyclics, Inc.

    发明人： Lee Honigberg ,  Erik Verner ,  Zhengying Pan

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  A61K31/00 ,  A61K45/06 ,  A61K9/48

    CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

    摘要： Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

    摘要翻译： 本文公开了与布鲁特酪氨酸激酶（Btk）形成共价键的吡唑并[3,4-d]嘧啶。 还描述了Btk的不可逆抑制剂。 公开了制备化合物的方法。 还公开了包含化合物的药物组合物。 公开了使用Btk抑制剂的方法，单独或与其它治疗剂组合用于治疗自身免疫性疾病或病症，异种免疫疾病或病症，癌症，包括淋巴瘤和炎性疾病或病症。