1-methyl-1H-imidazo[4,5-d]pyridazine | 33457-15-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 1-methyl-1H-imidazo[4,5-d]pyridazine
• 英文别名: 3-Methylimidazo[4,5-d]pyridazine
• CAS: 33457-15-7
• 化学式: C₆H₆N₄
• 分子量: 134.14
• InChiKey: UQRZJJYINNFOBO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE<br/>[FR] COMPOSÉS PYRIMIDINES BICYCLIQUES INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA, ET PROCÉDÉS D'UTILISATION
  申请人：GENENTECH INC

  公开号：WO2010138589A1

  公开（公告）日：2010-12-02

  Formula (I) ((Ia) and (Ib)) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

  公式（I）（（Ia）和（Ib））化合物，其中（i）X1为N且X2为S，（ii）X1为CR7且X2为S，（iii）X1为N且X2为NR2，或（iv）X1为CR7且X2为O，包括其立体异构体，互变异构体，代谢物和药用可接受盐，用于抑制PI3K的δ异构体，并用于治疗由脂质激酶介导的疾病，如炎症，免疫和癌症。公开了使用公式（I）化合物进行体外，体内和体内诊断，预防或治疗哺乳动物细胞中的这类疾病或相关病理状况的方法。
• DIOXINO- AND OXAZIN-[2,3-D]PYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
  申请人：Genentech, Inc.

  公开号：US20140065136A1

  公开（公告）日：2014-03-06

  Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

  公式I中的二氧代二氧代噁唑啉和噁唑啉[2,3-d]嘧啶PI3K抑制剂化合物具有抗癌活性、抗炎活性或免疫调节性质，更具体地具有PI3激酶调节或抑制活性。描述了使用公式I中的三环PI3K抑制剂化合物的方法，用于体外、体内和体内对哺乳动物细胞、生物体或相关病理条件进行诊断或治疗。
• PURINE COMPOUNDS SELECTIVE FOR PI3K P110 DELTA, AND METHODS OF USE
  申请人：Li Jun

  公开号：US20120015931A1

  公开（公告）日：2012-01-19

  The invention provides compounds having the general formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 and n are defined herein, compositions including the compounds and method of using the compounds to treat a disease or disorder mediated by the p110 delta isoform of PI3 kinase selected from immune disorders, cancer, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

  该发明提供了具有一般公式的化合物：及其立体异构体、互变异构体或药用可接受的盐，其中R1、R2、R3、R4和n在此处定义，包括这些化合物的组合物和使用这些化合物治疗由PI3激酶p110 δ异构体介导的疾病或紊乱的方法，所述疾病或紊乱选自免疫紊乱、癌症、心血管疾病、病毒感染、炎症、代谢/内分泌功能紊乱和神经系统疾病。
• [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。
• Useful indole compounds
  申请人：Bartolini Wilmin

  公开号：US20070203209A1

  公开（公告）日：2007-08-30

  Indoles having various activities, including indoles that are CRTH2 are described. The compounds are useful for treating asthma, neuropathic pain, allegic rhinitis and other disorders.

  本文描述了具有多种活性的吲哚类化合物，包括CRTH2的吲哚类化合物。这些化合物可用于治疗哮喘、神经病性疼痛、过敏性鼻炎和其他疾病。