4-Amino-1-methyl-imidazo<4,5-d>pyridazin | 99969-12-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-Amino-1-methyl-imidazo<4,5-d>pyridazin
• 英文别名: 1-Methyl-4-amino-pyrazolo<3.4-d>pyrimidin；1-methyl-1H-imidazo[4,5-d]pyridazin-4-ylamine；1-Methylimidazo[4,5-d]pyridazin-4-amine
• CAS: 99969-12-7
• 化学式: C₆H₇N₅
• mdl: MFCD19204942
• 分子量: 149.155
• InChiKey: ORDUXUMYWFNCBI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  69.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4,7-dichloro-1-methyl-1H-imidazo[4,5-d]pyridazine 在 palladium on activated charcoal 、 乙醇 、 氨 、 sodium acetate 、 溶剂黄146 作用下， 生成 4-Amino-1-methyl-imidazo<4,5-d>pyridazin
  参考文献：
  名称：

  The Preparation of Several 4-Substituted Imidazo[4,5-d]pyridazines as Possible Purine Antimetabolites

  摘要：

  DOI：

  10.1021/ja01555a047

文献信息

• [EN] LIPID COMPOSITIONS FOR DELIVERY OF STING AGONIST COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSITIONS LIPIDIQUES POUR L'ADMINISTRATION DE COMPOSÉS AGONISTES DE STING ET LEURS UTILISATIONS
  申请人：MASSACHUSETTS INST TECHNOLOGY

  公开号：WO2021216572A1

  公开（公告）日：2021-10-28

  The present disclosure provides lipid compositions comprising lipid particles (e.g., lipid nanodiscs), wherein the lipid particles (e.g., lipid nanodiscs) comprise a STING agonist amphiphile conjugate, a phospholipid and a PEG-lipid. The compositions are used in methods to induce or promote immune responses, such as immune responses useful for the treatment of cancer or infectious disease.

  本公开提供了包含脂质粒子（例如脂质纳米盘）的脂质组合物，其中脂质粒子（例如脂质纳米盘）包含STING激动剂两亲分子共轭物、磷脂和PEG-脂质。该组合物用于诱导或促进免疫反应，例如用于治疗癌症或传染病的免疫反应。
• Cyclic di-nucleotide compounds as STING agonists
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10738074B2

  公开（公告）日：2020-08-11

  A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

  一类通式(II)、通式(II′)或通式(II″)的多环化合物，其中Base1、Base2、Y、Ya、Xa、Xa1、Xb、Xb1、Xc、Xc1、Xd、Xd1、R1、R1a、本文定义了 R2、R2a、R3a、R4、R4a、R5、R6、R6a、R7、R7a、R8 和 R8a，它们可用作 I 型干扰素产生的诱导剂，特别是 STING 活性剂。还提供了合成和使用这些化合物的工艺。
• Cyclic di-nucleotide compounds as sting agonists
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10766919B2

  公开（公告）日：2020-09-08

  A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

  一类通式(I)、通式(I′)或通式(I″)的多环化合物，其中Base1、Base2、Y、Ya、Xa、Xa1、Xb、Xb1、Xc、Xc1、Xd、Xd1、R1、R1a、R2、本文定义的 R2a、R3、R4、R4a、R5、R6、R6a、R7、R7a、R8 和 R8a 可用作 I 型干扰素产生的诱导剂，特别是 STING 活性剂。还提供了合成和使用这些化合物的工艺。
• Cyclic dinucleotide
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US10980825B2

  公开（公告）日：2021-04-20

  The present disclosure provides a compound having a STING agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases. The present disclosure relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.

  本公开提供了一种具有 STING 激动活性的化合物，该化合物有望用作预防或治疗 STING 相关疾病的药物。 本公开涉及一种由式（I）表示的化合物： 其中各符号如描述中所定义，或其盐类。
• Methods of modulating immune activity
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US11376272B2

  公开（公告）日：2022-07-05

  In one aspect, the invention provides methods of increasing immune response by administering postcellular signaling factors produced by cells exposed to a stress condition. In one aspect, the invention provides methods of increasing immune response by administering in combination (a) a Stimulator of Interferon Genes (STING) agonist and (b) a purinergic receptor agonist. The increase in immune response may be used, for example, for treatment of infection or cancer. The invention also provides screening assays for identification of compounds that induce production of postcellular signaling factors which are also immunostimulatory agents. The invention further provides methods for identifying postcellular signaling factors with immunostimulatory activity. In another aspect, the invention provides methods of decreasing immune response by administering to a cell, tissue or subject a purinergic receptor antagonist alone or in combination with a Stimulator of Interferon Genes (STING) antagonist.

  一方面，本发明提供了通过施用暴露于应激条件下的细胞产生的细胞后信号因子来提高免疫应答的方法。在一个方面，本发明提供了通过联合施用(a)干扰素基因刺激剂（STING）激动剂和(b)嘌呤能受体激动剂来增加免疫反应的方法。免疫反应的增强可用于治疗感染或癌症等。本发明还提供了筛选测定法，用于鉴定能诱导产生细胞后信号因子的化合物，这些细胞后信号因子也是免疫刺激剂。本发明进一步提供了鉴定具有免疫刺激活性的细胞后信号因子的方法。在另一方面，本发明提供了通过向细胞、组织或受试者单独施用嘌呤能受体拮抗剂或与干扰素基因刺激剂（STING）拮抗剂联合施用来降低免疫反应的方法。