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    • 5. 发明申请
    • POLYFLUORINATED COMPOUNDS ACTING AS BRUTON TYROSINE KINASE INHIBITORS
    • 作为BRUTON酪氨酸激酶抑制剂的多氟化合物
    • US20160200730A1
    • 2016-07-14
    • US15075033
    • 2016-03-18
    • Wei He
    • Wei He
    • C07D487/04
    • A61K31/519C07C303/38C07C311/08C07D487/04C07D519/00C07F5/025C07F5/04
    • Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
    • 本文描述了一系列新的多氟取代的吡唑并嘧啶化合物或其盐。 这些化合物是Bruton的酪氨酸激酶(BTK)抑制剂。 这些化合物可具有更好的BTK抑制选择性和药代动力学性质。 本文公开了这些化合物的合成方法。 本文公开了多氟取代的二苯甲酮和取代的苯氧基苯的新型合成方法。 还公开了包含本文所述的BTK抑制剂的药物组合物。 本发明还涉及包含本文所述的化合物作为活性成分的药物制剂。 本发明还包括通过施用BTK抑制剂及其制剂来治疗和抑制自身免疫性疾病,超敏反应性疾病,炎性疾病和癌症的治疗方法。