首页> 外国专利> OPTIMIZED COMBINED THERAPY AND ITS APPLICATION FOR THE TREATMENT OF MALIGNANT TUMOR AND AUTOIMMUNE DISEASE

OPTIMIZED COMBINED THERAPY AND ITS APPLICATION FOR THE TREATMENT OF MALIGNANT TUMOR AND AUTOIMMUNE DISEASE

机译:优化的联合疗法及其在恶性肿瘤和自身免疫性疾病中的应用

摘要

A series of new multi-substituted fluorine pyrazolopyrimidine compounds or salts are presented. The compounds are Bruton tyrosine kinase inhibitors (BTKs). The compounds have better kinase inhibition selectivity and pharmacokinetic properties. A method for producing compounds is also provided. Combination therapy is also presented, which includes compounds in combination with a composition of another targeted drug or with another drug. The optimized combination therapy has a cooperative effect, suppressing an existing tumor better than a unidirectional drug, and causing the complete disappearance of certain tumors. The optimized combination therapy cures the resistance of the tumor to the drug and the recurrence of the malignant tumor is better than the unidirectional drug, and the treatment cycle is shorter. The present invention also relates to a combination compound and a pharmaceutical formulation, wherein said combination compound acts as an active ingredient, wherein said pharmaceutical formulation is safer in lower doses and has a cooperative effect efficacy. A method of using compounds and their preparation for the treatment and suppression of an autoimmune disease or disorder, a heterogeneous autoimmune disease or disorder, an inflammatory disease, a malignant tumor or a disorder is also provided.
机译:提出了一系列新的多取代氟吡唑并嘧啶化合物或盐。这些化合物是Bruton酪氨酸激酶抑制剂(BTK)。该化合物具有更好的激酶抑制选择性和药代动力学特性。还提供了一种生产化合物的方法。还提出了组合疗法,其包括与另一种靶向药物的组合物或与另一种药物组合的化合物。优化的联合疗法具有协同作用,比单向药物更好地抑制了现有的肿瘤,并导致某些肿瘤的完全消失。优化的联合疗法可治愈肿瘤对药物的耐药性,恶性肿瘤的复发优于单向药物,治疗周期更短。本发明还涉及组合化合物和药物制剂,其中所述组合化合物充当活性成分,其中所述药物制剂在较低剂量下更安全并且具有协同作用功效。还提供了使用化合物及其制剂来治疗和抑制自身免疫性疾病或病症,异源性自身免疫性疾病或病症,炎性疾病,恶性肿瘤或病症的方法。

著录项

  • 公开/公告号EA201792066A1

    专利类型

  • 公开/公告日2018-03-30

    原文格式PDF

  • 申请/专利号EA20170092066

  • 发明设计人 ВЭЙ;

    申请日2016-03-18

  • 分类号C07D487/04;A61K31/519;A61K45/06;A61P37/02;A61P29;A61P5/14;A61P3/10;A61P21/04;A61P1/04;A61P13/12;A61P1/16;A61P25;

  • 国家 EA

  • 入库时间 2022-08-21 12:52:47

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