替尼拉平 | 82650-83-7

• 物质功能分类: 原料药 - 抗肿瘤药 - 替尼类抗肿瘤药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 中文名称: 替尼拉平
• 英文名称: Tenilapine
• 英文别名: (2E)-2-[9-(4-methylpiperazin-1-yl)-5,12-dithia-8-azatricyclo[8.3.0.03,7]trideca-1(13),3,6,8,10-pentaen-2-ylidene]acetonitrile
• CAS: 82650-83-7
• 化学式: C₁₇H₁₆N₄S₂
• 分子量: 340.5
• InChiKey: RVQVUMIXBGFJLZ-SWGQDTFXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  23
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  99.1
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  替尼拉平 生成 Tenilapine
  参考文献：
  名称：

  STEINER, G.;TESCHENDORF, H. -J.;KREISKOTT, H.;HOFMANN, H. P.

  摘要：

  DOI：
• 作为产物：
  描述：

  (2E)-2-(9-chloro-5,12-dithia-8-azatricyclo[8.3.0.03,7]trideca-1(13),3,6,8,10-pentaen-2-ylidene)acetonitrile 生成 替尼拉平
  参考文献：
  名称：

  STEINER, G.;TESCHENDORF, H. -J.;KREISKOTT, H.;HOFMANN, H. P.

  摘要：

  DOI：

文献信息

• [EN] COMPOUNDS HAVING SEROTONIN 5-HT17 RECEPTOR ANTAGONIST ACTIVITY AND MUSCARINIC M4 RECEPTOR AGONIST ACTIVITY AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS<br/>[FR] COMPOSES PRESENTANT UNE ACTIVITE ANTAGONISTE DU RECEPTEUR DE LA SEROTONINE 5-HT17 ET UNE ACTIVITE AGONISTE DU RECEPTEUR MUSCARINIQUE M4 ET UTILISATION DE CES COMPOSES POUR LE TRAITEMENT DES TROUBLES PSYCHOTIQUES
  申请人：MITSUBISHI PHARMA CORP

  公开号：WO2004087124A1

  公开（公告）日：2004-10-14

  The present invention relates to novel treatments for schizophrenia, based on the concept of identifying agents capable of selectively binding to the serotonin 5-HT7 and muscarinic M4 receptors and the use of such compounds in treating schizophrenia. The present invention also relates to novel amidine compounds for treating schizophrenia, a method of manufacturing such compounds, pharmaceutical formulations comprising said compounds, as well as medical uses and methods of treatment using said compounds.

  本发明涉及基于识别能够选择性结合到5-羟色胺5-HT7和肌碱M4受体的药剂，并将这类化合物用于治疗精神分裂症的新型治疗方法。本发明还涉及用于治疗精神分裂症的新型胺基化合物，一种制造这类化合物的方法，包含该化合物的药物配方，以及使用该化合物进行治疗的医疗用途和治疗方法。
• Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
  申请人：——

  公开号：US20030078271A1

  公开（公告）日：2003-04-24

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

  这项发明涉及嘧啶和吲哚酮衍生物，它们是选择性GAL3受体拮抗剂。该发明提供了一种包含该发明化合物的治疗有效量和药用载体的药物组合物。该发明还提供了通过结合该发明化合物的治疗有效量和药用载体制备的药物组合物。该发明进一步提供了一种制备药物组合物的方法，包括结合该发明化合物的治疗有效量和药用载体。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用足以治疗受试者抑郁症和/或焦虑症的该发明化合物的量。该发明还提供了一种治疗受试者抑郁症和/或焦虑症的方法，包括向受试者施用包含药用载体和治疗有效量GAL3受体拮抗剂的组合物。
• GAL3 antagonists for the treatment of neuropathic pain
  申请人：——

  公开号：US20040092570A1

  公开（公告）日：2004-05-13

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor and are useful for the treatment of neuropathic pain and other abnormalities. This invention also provides a method of treating a subject suffering from an abnormality which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's abnormality. This invention also provides a method of treating an abnormality in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

  这项发明涉及嘧啶和吲哚酮衍生物，它们是选择性的GAL3受体拮抗剂，可用于治疗神经病痛和其他异常。这项发明还提供了一种治疗患有异常的受试者的方法，包括向受试者投予本发明中的化合物的有效剂量以治疗受试者的异常。这项发明还提供了一种治疗受试者异常的方法，包括向受试者投予包含药用载体和治疗有效量的GAL3受体拮抗剂的组合物。
• GAL3 receptor antagonists for the treatment of affective disorders
  申请人：——

  公开号：US20040110821A1

  公开（公告）日：2004-06-10

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. This invention provides a method of treating a subject suffering from an affective disorder which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's affective disorder. This invention also provides a method of treating an affective disorder in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

  这项发明涉及选择性拮抗剂对GAL3受体的嘧啶和吲哚酮衍生物。该发明提供了一种治疗患有情感障碍的受试者的方法，包括向受试者施用一定量的该发明化合物，以有效治疗受试者的情感障碍。该发明还提供了一种治疗受试者情感障碍的方法，包括向受试者施用包含药用可接受载体和治疗有效量GAL3受体拮抗剂的组合物。该发明进一步提供了一种制备药物组合物的方法，包括结合该发明化合物的治疗有效量和药用可接受载体。
• 2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
  申请人：——

  公开号：US20040082587A1

  公开（公告）日：2004-04-29

  This invention is directed to pyrimidine derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GalR3 receptor antagonist.

  这项发明涉及选择性拮抗剂对GalR3受体的嘧啶衍生物。该发明提供了一种包含本发明化合物的治疗有效量和药用载体的药物组合物。该发明还提供了一种通过结合本发明化合物的治疗有效量和药用载体制备的药物组合物。该发明还提供了一种制备药物组合物的方法，包括结合本发明化合物的治疗有效量和药用载体。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者投与一定量的本发明化合物以治疗受试者的抑郁症和/或焦虑症。该发明还提供了一种治疗受试者抑郁症和/或焦虑症的方法，包括向受试者投与一种含有药用载体和GalR3受体拮抗剂的组合物的治疗有效量。