JAK3 inhibitor VI | 623175-13-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: JAK3 inhibitor VI
• 英文别名: 2H-Indol-2-one, 1,3-dihydro-5-(3-pyridinyl)-3-(1H-pyrrol-2-ylmethylene)-；(3Z)-5-pyridin-3-yl-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one
• CAS: 623175-13-3
• 化学式: C₁₈H₁₃N₃O
• 分子量: 287.321
• InChiKey: IQNTXIMXKCURDC-YBEGLDIGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.8
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  5-溴氧化吲哚 在 哌啶 、 四(三苯基膦)钯 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 为溶剂， 生成 JAK3 inhibitor VI
  参考文献：
  名称：

  Mapping the kinase domain of janus kinase 3

  摘要：

  The utilization and impact of parallel synthesis on lead exploration around initial hit oxindole (1) are described. The emergent SAR, analogue design and functional impact will also be detailed. (C) 2003 Published by Elsevier Ltd.

  DOI：

  10.1016/s0960-894x(03)00657-7

文献信息

• [EN] NOVEL THERAPEUTIC USE OF INDOLINONE DERIVATIVES<br/>[FR] NOUVELLE UTILISATION THERAPEUTIQUE DE DERIVES D'INDOLINONE
  申请人：LEO PHARMA AS

  公开号：WO2005058309A1

  公开（公告）日：2005-06-30

  Certain oxindole compounds have been found to be effective in experimentally induced autoimmune encephalitis and are therefore suggested for the preparation of a medicament for the prevention, treatment or amelioration of multiple sclerosis, or to delay the onset of or reduce the relapse rate in multiple sclerosis.

  某些氧吲哚化合物已被发现在实验诱导的自身免疫性脑炎中具有有效性，因此建议用于制备用于预防、治疗或改善多发性硬化症的药物，或延缓多发性硬化症的发作或减少复发率。
• [EN] BENZOTHIOPHENE, BENZYLOXYBENZYLIDENE AND INDOLINE DERIVATIVES USEFUL FOR THE TREATMENT OF TUBERCULOSIS<br/>[FR] BENZOTHIOPHÈNE, BENZYLOXYBENZYLIDÈNE ET DÉRIVÉS DE L'INDOLINE UTILES POUR LE TRAITEMENT DE LA TUBERCULOSE
  申请人：ECOLE POLYTECH

  公开号：WO2016041972A1

  公开（公告）日：2016-03-24

  The present invention relates to benzothiophene, benzyloxybenzylidene and indoline-2-one derivatives and the use of said derivatives in the treatment and/or prevention of tuberculosis.

  本发明涉及苯并噻吩、苄氧基苯甲醛亚甲基和吲哚啉-2-酮衍生物，以及该衍生物在结核病的治疗和/或预防中的应用。
• Novel therapeutic use
  申请人：Bouerat Duvold Maud Elysa Laetitia

  公开号：US20070167488A1

  公开（公告）日：2007-07-19

  Certain oxindole compounds have been found to be effective in experimentally induced autoimmune encephalitis and are therefore suggested for the preparation of a medicament for the prevention, treatment or amelioration of multiple sclerosis, or to delay the onset of or reduce the relapse rate in multiple sclerosis.

  某些恶唑酮化合物已被发现在实验性自身免疫脑炎中具有疗效，因此建议用于制备用于预防、治疗或改善多发性硬化症的药物，或者延迟多发性硬化症的发作或减少复发率。
• Oxindoles which are inhibitors of CDK-1 and their application in therapeutics
  申请人：AVENTIS PHARMA SA

  公开号：US20040110770A1

  公开（公告）日：2004-06-10

  The present invention relates to a compound of formula (I): 1 wherein R5 is selected from the group consisting of 3-pyridyl, 5-pyrimidinyl, —CONH—(C 1 -C 4 alkyl), —NHCO—(C 1 -C 4 alkyl), halogen, —SO 2 NH 2 , —NO 2 , —CF 3 or thien-2-ylcarbonyl 2 and —CO 2 R where R can be hydrogen or C 1 -C 4 alkyl; and Ar is selected from the group consisting of 5-imidazolyl, 2-pyrrolyl optionally substituted by a C 1 -C 4 alkyl radical, 2-furyl or 2-thiazolyl, in the E or Z geometrical isomeric form or a mixture of the two geometrical isomeric forms. The invention is also directed to a method of treating primary and secondary tumours in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of formula I. The invention is also directed to a method of using a compound of formula I to treat cancer, inhibit the proliferation of a cell and induce cell apoptosis, comprising contacting a cell with an effective amount of the compound of formula I., The invention is also directed to a method of preparing the compound of formula I.

  本发明涉及一种式为(I)的化合物：其中R5选自3-吡啶基，5-嘧啶基，-CONH-(C1-C4烷基)，-NHCO-(C1-C4烷基)，卤素，-SO2NH2，-NO2，-CF3或噻吩-2-基酰基2和-CO2R，其中R可以是氢或C1-C4烷基；Ar选自5-咪唑基，2-吡咯基（可选择由C1-C4烷基基团取代），2-呋喃基或2-噻唑基，在E或Z几何异构体形式或两种几何异构体形式的混合物中。 本发明还涉及一种治疗患有原发性和继发性肿瘤的患者的方法，包括向患者投予式为I的化合物的治疗有效量。本发明还涉及一种使用式为I的化合物治疗癌症、抑制细胞增殖和诱导细胞凋亡的方法，包括用式为I的化合物的有效量与细胞接触。本发明还涉及一种制备式为I的化合物的方法。
• OXINDOLES INHIBITEURS DE CDK-1 ET LEUR APPLICATION EN THERAPEUTIQUE
  申请人：Aventis Pharma S.A.

  公开号：EP1366038B1

  公开（公告）日：2005-08-31