benzothiazol-5-yl-(6-chloro-pyrazin-2-yl)-amine | 1175018-53-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: benzothiazol-5-yl-(6-chloro-pyrazin-2-yl)-amine
• 英文别名: Benzothiazol-5-yl-(6-chloro-pyrazin-2-yl)-amine；N-(6-chloropyrazin-2-yl)-1,3-benzothiazol-5-amine
• CAS: 1175018-53-7
• 化学式: C₁₁H₇ClN₄S
• 分子量: 262.722
• InChiKey: JCAHIMFBLRQOFM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  78.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  benzothiazol-5-yl-(6-chloro-pyrazin-2-yl)-amine 、 吡啶-4-硼酸 在 四(三苯基膦)钯 sodium carbonate 作用下， 以 乙二醇二甲醚 、 水 为溶剂， 反应 22.0h， 以50%的产率得到N-(6-pyridin-4-ylpyrazin-2-yl)-1,3-benzothiazol-5-amine
  参考文献：
  名称：

  [EN] PYRAZINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHBITORS
  [FR] NOUVEAUX COMPOSÉS, LEUR UTILISATION ET LEUR PRÉPARATION

  摘要：

  公开号：

  WO2009095399A3
• 作为产物：
  描述：

  1,3-苯并噻唑-5-胺 、 2,6-二氯吡嗪 在 palladium diacetate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 16.0h， 以53%的产率得到benzothiazol-5-yl-(6-chloro-pyrazin-2-yl)-amine
  参考文献：
  名称：

  [EN] PYRAZINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHBITORS
  [FR] NOUVEAUX COMPOSÉS, LEUR UTILISATION ET LEUR PRÉPARATION

  摘要：

  公开号：

  WO2009095399A3

文献信息

• NOVEL COMPOUNDS, USE AND PREPARATION THEREOF
  申请人：Jensen Annika Jenmalm

  公开号：US20110098310A1

  公开（公告）日：2011-04-28

  The present invention relates to compounds of the general formula (I) wherein R 1 , R 2 and R 3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.

  本发明涉及一般式(I)所示的化合物，其中R1、R2和R3如本文所定义，可作为蛋白激酶的抑制剂，特别是Fms样酪氨酸激酶3（FLT3）的抑制剂。本发明还涉及将该化合物用于治疗、包含该化合物的药物组合物以及将该化合物用于制备用于预防和治疗血液恶性肿瘤，如AML、MLL、T-ALL、B-ALL和CMML、骨髓增生性疾病、其他增殖性疾病如癌症、自身免疫性疾病和皮肤疾病如银屑病和特应性皮炎的药物。
• Amino substituted pyrazines as inhibitors or protein kinases
  申请人：Jensen Annika Jenmalm

  公开号：US08436171B2

  公开（公告）日：2013-05-07

  The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). A species illustrative of members of the general formula is The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.

  本发明涉及通式（I）的化合物，其中R1，R2和R3如本文所定义，可作为蛋白激酶抑制剂，特别是Fms-like酪氨酸激酶3（FLT3）的抑制剂。通式成员的具体示例是本发明还涉及将该化合物用于治疗、包含该化合物的制药组合物以及将该化合物用于制备用于预防和治疗血液恶性肿瘤（如AML，MLL，T-ALL，B-ALL和CMML）、骨髓增生性疾病、其他增生性疾病（如癌症）、自身免疫性疾病和皮肤疾病（如银屑病和特应性皮炎）的药物的用途。
• Pyrazine derivatives and their use as protein kinase inhbitors
  申请人：Akinion Pharmaceuticals AB

  公开号：EP2671876A2

  公开（公告）日：2013-12-11

  The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.

  本发明涉及通式(I)的化合物，其中R1、R2和R3如本文所定义，可作为蛋白激酶，特别是Fms样酪氨酸激酶3（FLT3）的抑制剂。本发明还涉及本发明化合物在治疗中的用途、包含本发明化合物的药物组合物，以及本发明化合物在制备预防和治疗血液恶性肿瘤（如AML、MLL、T-ALL、B-ALL和CMML）、骨髓增生性疾病、其他增生性疾病（如癌症）、自身免疫性疾病和皮肤疾病（如牛皮癣和特应性皮炎）的药物中的用途。
• US8436171B2
  申请人：——

  公开号：US8436171B2

  公开（公告）日：2013-05-07
• [EN] NOVEL COMPOUNDS, USE AND PREPARATION THEREOF<br/>[FR] NOUVEAUX COMPOSÉS, LEUR UTILISATION ET LEUR PRÉPARATION
  申请人：BIOVITRUM AB PUBL

  公开号：WO2009095399A2

  公开（公告）日：2009-08-06

  The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.