2-iodo-5-methoxybenzo[d]thiazole | 1175278-06-4

• 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: 2-iodo-5-methoxybenzo[d]thiazole
• 英文别名: 2-iodo-5-methoxy-1,3-benzothiazole
• CAS: 1175278-06-4
• 化学式: C₈H₆INOS
• 分子量: 291.112
• InChiKey: HSYKQDKTTDLAEX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  50.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-iodo-5-methoxybenzo[d]thiazole 在 aluminum (III) chloride 、 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 30.0h， 生成 2-iodo-5-(2-methoxyethoxy)benzo[d]thiazole
  参考文献：
  名称：

  [EN] INHIBITORS FOR THE Β-CATENIN / T-CELL FACTOR PROTEIN–PROTEIN INTERACTION
  [FR] INHIBITORS POUR L'INTERACTION PROTÉINE-PROTÉINE BÊTA-CATÉNINE/FACTEUR DES LYMPHOCYTES T

  摘要：

  公开了β-连环蛋白/T细胞因子相互作用的抑制剂。这些抑制剂对β-连环蛋白/T细胞因子的选择性高于β-连环蛋白/钙粘蛋白和β-连环蛋白/APC相互作用。还公开了使用所述化合物治疗癌症的方法。

  公开号：

  WO2019191410A1
• 作为产物：
  描述：

  5-甲氧基-2-苯并噻唑胺 在 对甲苯磺酸 、 potassium iodide 、 sodium nitrite 作用下， 以 水 、 乙腈 为溶剂， 以67.8 %的产率得到2-iodo-5-methoxybenzo[d]thiazole
  参考文献：
  名称：

  发现用于预防动脉血栓形成的有效且选择性喹喔啉蛋白酶激活受体 4 (PAR4) 拮抗剂

  摘要：

  PAR4 是一种有前景的抗血栓靶点，相对于当前的抗血小板治疗，具有将疗效与出血风险分开的潜力。为了发现一种新型 PAR4 拮抗剂化学型，我们鉴定出了一种基于喹喔啉的 HTS hit 3 ，具有低 μM 效力。通过使用位置 SAR 扫描和构象约束核心的设计来优化 HTS 命中，导致发现了喹喔啉-苯并噻唑系列作为有效的选择性 PAR4 拮抗剂。先导化合物48在富含血小板的血浆 (PRP) 中对 γ-凝血酶激活 PAR4 具有 2 nM IC 50 ，且选择性相对于 PAR1 超过 2500 倍，在食蟹猴模型中表现出强大的抗血栓功效和最少的出血。

  DOI：

  10.1021/acs.jmedchem.3c01986

文献信息

• 2-AMINOPYRIDINE KINASE INHIBITORS
  申请人：Steinig Arno G.

  公开号：US20090197862A1

  公开（公告）日：2009-08-06

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有Formula I结构的2-氨基吡啶化合物，以及这些化合物的药用可接受的盐。Formula I的化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并可用于治疗和/或预防各种疾病和病况。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR、Tie-2、Flt3、FGFR3、Ab1、Aurora A、c-Src、IGF-1R、ALK、c-MET、RON、PAK1、PAK2和TAK1，并可用于治疗增生性疾病，如但不限于癌症。本发明还涉及一种包含Formula I化合物的药物组合物，或其药用可接受的盐，以及药用可接受的载体的药物组合物。本发明还涉及一种通过向患有由蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• 2-aminopyridine kinase inhibitors
  申请人：OSI Pharmaceuticals, LLC

  公开号：US08178668B2

  公开（公告）日：2012-05-15

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有I式结构的2-氨基吡啶化合物，以及这些化合物的药学上可接受的盐。I式化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并在治疗和/或预防各种疾病和病况方面有用。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR，Tie-2，Flt3，FGFR3，Ab1，Aurora A，c-Src，IGF-1R，ALK，c-MET，RON，PAK1，PAK2和TAK1，并可用于治疗增殖性疾病，例如但不限于癌症。本发明还涉及一种制备药物组合物的方法，该组合物包括I式化合物或其药学上可接受的盐的治疗有效量以及药学上可接受的载体。本发明还涉及一种通过向患有蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• Composition, film, near infrared cut filter, laminate, pattern forming method, solid image pickup element, image display device, infrared sensor, and color filter
  申请人：FUJIFILM Corporation

  公开号：US10947389B2

  公开（公告）日：2021-03-16

  The composition includes two or more near infrared absorbing compounds having an absorption maximum in a wavelength range of 650 to 1000 nm and having a solubility of 0.1 mass % or lower in water at 23° C., in which the two or more near infrared absorbing compounds include a first near infrared absorbing compound having an absorption maximum in a wavelength range of 650 to 1000 nm, and a second near infrared absorbing compound having an absorption maximum in a wavelength range of 650 to 1000 nm which is shorter than the absorption maximum of the first near infrared absorbing compound, and a difference between the absorption maximum of the first near infrared absorbing compound and the absorption maximum of the second near infrared absorbing compound is 1 to 150 nm.

  该组合物包括两种或两种以上的近红外吸收化合物，其最大吸收波长范围为 650 至 1000 nm，在 23°C 水中的溶解度为 0.1 质量％或更低、其中，两种或两种以上的近红外吸收化合物包括：第一种近红外吸收化合物，其吸收最大值的波长范围为 650 至 1000 nm；第二种近红外吸收化合物，其吸收最大值的波长范围为 650 至 1000 nm，比第一种近红外吸收化合物的吸收最大值短，且第一种近红外吸收化合物的吸收最大值与第二种近红外吸收化合物的吸收最大值之间的差值为 1 至 150 nm。
• Composition, curable composition, cured film, near infrared cut filter, infrared transmitting filter, solid image pickup element, infrared sensor, and camera module
  申请人：FUJIFILM Corporation

  公开号：US11209582B2

  公开（公告）日：2021-12-28

  Provided are a composition that has excellent pigment dispersibility without affecting the color of a pigment in a visible range, a curable composition, a cured film, a near infrared cut filter, an infrared transmitting filter; a solid image pickup element, an infrared sensor, and a camera module. The composition includes: a pigment; a pigment derivative that includes a compound represented by Formula (1); and a solvent, in which R1 and R2 represent an aryl group or the like, R3 to R6 represent a cyano group, a heteroaryl group, or the like, R7 and R8 each independently represent —BR9R10 or the like, R9 and R10 each independently represent a hydrogen atom, a halogen atom, an alkyl group, an aryl group, a heteroaryl group, an alkoxy group, an aryloxy group, or a heteroaryloxy group, L represents a single bond or a linking group, X represents an acidic group or the like, m represents an integer of 1 to 10, and n represents an integer of 1 to 10.

  本发明提供了一种在不影响可见光范围内颜料颜色的情况下具有优异颜料分散性的组合物、一种可固化组合物、一种固化薄膜、一种近红外切割滤光片、一种红外透射滤光片；一种固体图像拾取元件、一种红外传感器和一种相机模块。组合物包括颜料；颜料衍生物，包括由式（1）表示的化合物；和溶剂，其中 R1 和 R2 代表芳基或类似物，R3 至 R6 代表氰基、杂芳基或类似物，R7 和 R8 各自独立地代表 -BR9R10 或类似物，R9 和 R10 各自独立地代表氢原子、卤素原子、烷基、芳基或类似物、烷基、芳基、杂芳基、烷氧基、芳氧基或杂芳基氧基，L 代表单键或连接基团，X 代表酸性基团或类似基团，m 代表 1 至 10 的整数，n 代表 1 至 10 的整数。
• Inhibitors for the β-catenin / T-cell factor protein-protein interaction
  申请人：H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

  公开号：US11530186B2

  公开（公告）日：2022-12-20

  Disclosed are inhibitors for the β-catenin/T-cell factor interaction. The inhibitors are selective for β-catenin/T-cell factor over β-catenin/cadherin and β-catenin/APC interactions. Methods of using the disclosed compounds to treat cancer are also disclosed.

  所公开的是β-catenin/T-细胞因子相互作用的抑制剂。这些抑制剂对β-catenin/T-细胞因子的选择性高于β-catenin/cadherin和β-catenin/APC相互作用。还公开了使用所公开的化合物治疗癌症的方法。