替罗替模 | 105523-37-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 替罗替模
• 中文别名: 噻丙莫德
• 英文名称: tiprotimod
• 英文别名: [2-(3-carboxy-1-propylthio)-4-methyl-1,3-thiazol-5-yl]acetic acid；4-[[5-(carboxymethyl)-4-methyl-1,3-thiazol-2-yl]sulfanyl]butanoic acid
• CAS: 105523-37-3
• 化学式: C₁₀H₁₃NO₄S₂
• 分子量: 275.35
• InChiKey: PZEUAMSVHLMPBZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  17
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  141
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-[[5-(2-Methoxy-2-oxoethyl)-4-methyl-1,3-thiazol-2-yl]sulfanyl]butanoic acid 生成 替罗替模
  参考文献：
  名称：

  1,3-thiazoles and their use as immunomodulators

  摘要：

  本发明涉及一般式为杂环-S-R的杂环硫化物的制备方法，特别是它们在免疫刺激、免疫修复和细胞静止治疗方面的应用，以及包含此类硫化物的制药剂，用于这些适应症。

  公开号：

  US04762848A1

文献信息

• [EN] SUBSTITUTED PYRAZINONE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION<br/>[FR] COMPOSES DE PYRAZINONE SUBSTITUES POUR LE TRAITEMENT DE L'INFLAMMATION
  申请人：PHARMACIA CORP

  公开号：WO2005035527A1

  公开（公告）日：2005-04-21

  Kinase inhibitors of Formula (I): wherein X, Ra, Rb, Rc, and Rd are as defined herein, are disclosed.

  Formula (I)的激酶抑制剂：其中X、Ra、Rb、Rc和Rd如本文所定义的那样。
• Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents
  申请人：PFIZER INC.

  公开号：US20030144280A1

  公开（公告）日：2003-07-31

  This invention relates to a compound of the formula: 1 or a pharmaceutically acceptable salt thereof, wherein A and R 1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R 2 is NH 2 ; R 3 and R 4 are each hydrogen, halo, (C 1 -C 4 )alkyl optionally substituted with halo and the like; and X 1 to X 4 are each hydrogen, halo, hydroxy, (C 1 -C 4 )alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.

  本发明涉及一种化合物的公式： 1 或其药用可接受的盐，其中A和R 1 各自为可选地取代的5至6成员的杂芳基，其中杂芳基可选择性熔合至碳环或5至6-杂芳基；R 2 为NH 2 ；R 3 和R 4 各自为氢，卤素，(C 1 -C 4 )烷基可选择性被卤素等取代；和X 1 至X 4 各自为氢，卤素，羟基，(C 1 -C 4 )烷基可选择性被卤素等取代。这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其它COX-2相关疾病。
• [EN] NITROSATED BENZOPYRAN COMPOUNDS AS NOVEL CYCLOOXYGENASE-2 SELECTIVE INHIBITORS<br/>[FR] COMPOSES BENZOPYRANNE NITROSES EN TANT QUE NOUVEAUX INHIBITEURS SELECTIFS DE LA CYCLOOXYGENASE-2
  申请人：PHARMACIA & UPJOHN CO LLC

  公开号：WO2006040676A1

  公开（公告）日：2006-04-20

  This invention specifically relates to novel cyclooxygenase 2 (COX-2) selective inhibitor compounds that donate, transfer or release nitric oxide, stimulate endogenous synthesis of nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. Compounds of particular interest and their analogs defined by formula (I) wherein Z, X, R1, R2, R3, and R4 are as described in the specification. This invention also relates to pharmaceutical compositions and methods for treating COX-2 mediated disorders, such as inflammation and inflammation related disorders.

  这项发明特指与新型环氧合酶2（COX-2）选择性抑制剂化合物有关，这些化合物可以提供、转移或释放一氧化氮，刺激内源性一氧化氮的合成，提高内源性内皮源性舒张因子的水平，或者是一氧化氮合酶的底物。特别感兴趣的化合物及其由式（I）中定义的类似物，其中Z、X、R1、R2、R3和R4如规范中所述。这项发明还涉及用于治疗COX-2介导的疾病，如炎症和与炎症相关的疾病的药物组合物和方法。
• [EN] CHROMENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS<br/>[FR] DERIVES DE CHROMENE A TITRE D'AGENTS ANTI-INFLAMMATOIRES
  申请人：PHARMACIA CORP

  公开号：WO2004087687A1

  公开（公告）日：2004-10-14

  The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (I). Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.

  该发明涉及在治疗与环氧合酶-2介导的疾病相关的情况中具有效用的方法和化合物。特别感兴趣的化合物是由式(I)定义的苯并吡喃和它们的类似物。其中Z、X、R1、R2、R3和R4如规范中所述。
• [EN] SUBSTITUTED THIOPHENE AMIDE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION<br/>[FR] COMPOSES D'AMIDE A SUBSTITUTION DE THIOPHENE POUR LE TRAITEMENT DE L'INFLAMMATION.
  申请人：PHARMACIA & UPJOHN CO LLC

  公开号：WO2005105777A1

  公开（公告）日：2005-11-10

  IKK-2-inhibiting compounds of Formula I: wherein R, X, Y, Z, R3, R4, R5, and are as defined herein, are disclosed.

  公式I中抑制IKK-2的化合物：其中R、X、Y、Z、R3、R4、R5如本文所定义。