5H-[1,3]Thiazolo[2,3-B]quinazoline | 270-13-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 5H-[1,3]Thiazolo[2,3-B]quinazoline
• CAS: 270-13-3
• 化学式: C₁₀H₈N₂S
• 分子量: 188.25
• InChiKey: YVGLRYSPFBUOAT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  40.9
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] IMIDAZOLINE DERIVATIVES AS CXCR4 MODULATORS<br/>[FR] DÉRIVÉS D'IMIDAZOLINE UTILISÉS EN TANT QUE MODULATEURS DE CXCR4
  申请人：UNIV PARIS

  公开号：WO2020201096A1

  公开（公告）日：2020-10-08

  The present invention provides novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds of formula (I) can act as CXCR4 modulators that specifically target the CXCR4 minor pocket, and they have further been found to inhibit the production of inflammatory cytokines in immune cells, which renders these compounds highly advantageous for use in therapy, particularly in the treatment or prevention of an inflammatory disorder, an autoimmune disorder, an autoinflammatory disorder, or an interferonopathy, such as, e.g., lupus erythematosus, dermatomyositis or rheumatoid arthritis.

  本发明提供了化合物的新结构（I）及含有这些化合物的药物组合物。式（I）化合物可以作为CXCR4调节剂，特异性靶向CXCR4小口袋，并且进一步发现能够抑制免疫细胞中炎症细胞因子的产生，使得这些化合物在治疗中具有极大的优势，特别适用于治疗或预防炎症性疾病、自身免疫性疾病、自身炎症性疾病或干扰素病，例如红斑狼疮、皮肌炎或类风湿性关节炎。
• Thiazoloquinazoline derivatives, their preparation and pharmaceutical compositions containing same
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0142057A2

  公开（公告）日：1985-05-22

  Compounds of the formula wherein R1 is hydrogen, lower alkyl, lower cycfoalkyl, lower alkoxy, hydroxy frafogen lower alkylthio lower alkylsulfirryl lower alkylsulfonyl, di-lower alkyl- NiCH2)nO- or 2-hydroxyethoxy; n is 2 to 7; R2 is hydrogen lower alkyl or lower alkoxy; R5 is hydrogen or lower alkyl; provided that if R2 is otherthan hydrogen, R5 is hydrogen; O is one of the groups wherein R3 is hydrogen or methyl; R4 is hydrogen or lower alkyl; R5 is lower alkyl; m is 1 to 7; w is zero or one; Y is-NH-; -NH-CH2; -0-; or -S.; and A is an unsubstituted or substituted heterocyclic radical; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are useful as anti-allergic agents as well as agents for the treatment of vascular disorders.

  式中的化合物 其中 R1 是氢、低级烷基、低级环烷基、低级烷氧基、羟基芴基低级烷硫基低级烷磺酰基、二低级烷基- NiCH2)nO- 或 2-羟基乙氧基；n 是 2 至 7；R2 是氢低级烷基或低级烷氧基；R5 是氢或低级烷基；但如果 R2 不是氢，则 R5 是氢；O 是基团之一 其中 R3 是氢或甲基；R4 是氢或低级烷基；R5 是低级烷基；m 是 1 至 7；w 是 0 或 1；Y 是-NH-；-NH-CH2；-0-；或-S.；A 是未取代或取代的杂环基；以及其药学上可接受的酸加成盐。式 I 的化合物可用作抗过敏剂和治疗血管疾病的药物。
• NOVEL USE
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1177797A1

  公开（公告）日：2002-02-06

  Preventives and/or remedies for Parkinson's disease and symptoms associating therewith such as anxiety, depression and/or memory disorder which contain as the active ingredient an adenosine A1A2a receptor dual antagonist or salts thereof.

  帕金森病及其相关症状（如焦虑、抑郁和/或记忆障碍）的预防和/或治疗药物，其活性成分为腺苷 A1A2a 受体双重拮抗剂或其盐类。
• Method for the treatment of parkinson's disease comprising administering an A1A2a receptor dual antagonist
  申请人：Fujisawa Pharmaceutical Co. Ltd.

  公开号：US20040152659A1

  公开（公告）日：2004-08-05

  Preventives and/or remedies for Parkinson's disease and symptoms associating therewith such as anxiety, depression and/or memory disorder which contain as the active ingredient an adenosine A 1 A 2a receptor dual antagonist or salts thereof.

  帕金森病及其相关症状（如焦虑、抑郁和/或记忆障碍）的预防剂和/或治疗剂，其活性成分包含腺苷 A 1 A 2a 受体双重拮抗剂或其盐类。
• TRICYCLISCHE MERCAPTOMETHYLSUBSTITUIERTE 2,3-DIHYDRO-CHINAZOLIN-5-ONE UND 2,3-DIHYDRO-BENZO-[1,2,4]-THIADIAZIN-5,5-DIOXIDE ALS MATRIX METALLOPROTEINASE (MMP) INHIBITOREN
  申请人：IBFB GmbH Privates Institut für biomedizinische Forschung und Beratung

  公开号：EP1319010B1

  公开（公告）日：2003-12-17