3-chloro-6,7-dihydroisoquinolin-8(5H)-one | 1256821-77-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-chloro-6,7-dihydroisoquinolin-8(5H)-one
• 英文别名: 3-chloro-6,7-dihydro-5H-isoquinolin-8-one
• CAS: 1256821-77-8
• 化学式: C₉H₈ClNO
• 分子量: 181.62
• InChiKey: TZXOMPDQLSWHJJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  30
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS<br/>[FR] COMPOSÉS TÉTRAHYDROQUINOLINONE SUBSTITUÉS EN TANT QUE MODULATEURS DE ROR GAMMA
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2016185342A1

  公开（公告）日：2016-11-24

  The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了公式（I）的取代四氢喹啉酮及相关化合物，作为视黄酸受体相关孤儿受体（RORs）的调节剂，在RORγ调节剂方面具有治疗上的用途。这些化合物在治疗和预防疾病和/或紊乱方面具有用途，特别是它们在由RORγ受体介导的疾病和/或紊乱中的用途。本发明还提供了这些化合物的制备以及包含至少一种取代四氢喹啉酮或相关化合物的制剂和药物配方，以及其所用的药学上可接受的载体、稀释剂或赋形剂。
• [EN] COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-ALPHA AND THEIR METHODS OF USE<br/>[FR] COMPOSÉS ET COMPOSITIONS PERMETTANT D'INHIBER L'ACTIVITÉ DE HIF2-ALPHA ET LEURS PROCÉDÉS D'UTILISATION
  申请人：NOVARTIS AG

  公开号：WO2021220170A1

  公开（公告）日：2021-11-04

  The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease. The compounds are inhibitors or modulators of HIF2alpha.

  本发明涉及公式（I）的化合物或其药用可接受的盐形式，其中取代基如规范中所定义；制备该化合物的中间体；包含该化合物的药物组合物；以及利用该化合物治疗疾病。这些化合物是HIF2alpha的抑制剂或调节剂。
• METHOD FOR THE PREPARATION OF TETRAHYDROQUINOLINONE COMPOUNDS HAVING ROR-GAMMA MODULATING ACTIVITY
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3845526A1

  公开（公告）日：2021-07-07

  The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORy modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了取代的四氢喹啉酮和相关的式(I)化合物，它们作为视黄酸受体相关孤儿受体（RORs）的调节剂，特别是作为RORy调节剂，具有治疗作用。这些化合物可用于治疗和预防疾病和/或失调，特别是用于 RORγ 受体介导的疾病和/或失调。本发明还提供了包含至少一种取代的四氢喹啉酮或式（I）相关化合物的化合物和药物制剂的制备方法，以及药学上可接受的载体、稀释剂或赋形剂。
• Substituted tetrahydroquinolinone compounds as ROR gamma modulators
  申请人：Aurigene Discovery Technologies Limited

  公开号：US11229636B2

  公开（公告）日：2022-01-25

  The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了取代的四氢喹啉酮和相关的式(I)化合物，它们作为视黄酸受体相关孤儿受体（RORs）的调节剂，特别是作为RORγ调节剂，具有治疗作用。这些化合物可用于治疗和预防疾病和/或紊乱，特别是用于治疗由 RORγ 受体介导的疾病和/或紊乱。本发明还提供了包含至少一种取代的四氢喹啉酮或式（I）相关化合物的化合物和药物制剂的制备方法，以及药学上可接受的载体、稀释剂或赋形剂。
• SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS
  申请人：Aurigene Discovery Technologies Limited

  公开号：EP3294713A1

  公开（公告）日：2018-03-21