1,2,3,4-Tetrahydro-1,5-naphthyridin-2-amine

• 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: 1,2,3,4-Tetrahydro-1,5-naphthyridin-2-amine
• 英文别名: 1,2,3,4-tetrahydro-1,5-naphthyridin-2-amine
• 化学式: C₈H₁₁N₃
• 分子量: 149.19
• InChiKey: RBOQWXOXPXVFQS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  50.9
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE<br/>[FR] TÉTRAHYDRONAPHTYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE ET COMPOSÉS BICYCLIQUES APPARENTÉS POUR L'INHIBITION DE L'ACTIVITÉ DE RORGAMMA ET LE TRAITEMENT DE MALADIE
  申请人：MERCK SHARP & DOHME

  公开号：WO2015095795A1

  公开（公告）日：2015-06-25

  The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

  这项发明提供了公式（I）的某些双环杂环化合物或其药学上可接受的盐，其中X1、X2、R1、R2、R3、R4和Cy如本文所定义。该发明还提供了包括公式（I）的这种化合物或其药学上可接受的盐的药物组合物，以及使用公式（I）的这种化合物或其药学上可接受的盐或包含相同的药物组合物治疗由RORgammaT介导的疾病或症状的方法。
• TETRAHYDRONAPHTHYRIDINE AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150111877A1

  公开（公告）日：2015-04-23

  The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.

  本发明提供四氢萘啶及相关化合物、制药组合物、抑制RORγ活性、减少受试者体内IL-17含量、以及使用这种四氢萘啶及相关化合物治疗免疫性疾病和炎症性疾病的方法。
• Tetrahydro[1,8]naphthyridine Sulfonamide and Related Compounds for Use as Agonists of RORy and the Treatment of Disease
  申请人：Lycera Corporation

  公开号：US20150133437A1

  公开（公告）日：2015-05-14

  The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.

  该发明提供了四氢[1,8]萘啶及其相关化合物，促进RORy活性和/或增加主体中iL-17数量的方法，并且提供了四氢[1,8]萘啶及其相关化合物的治疗用途。特别地，该发明提供了磺酰胺-四氢[1,8]萘啶及其相关化合物，使用这些化合物促进RORy活性和/或增加主体中iL-17数量的方法，并治疗激活免疫反应有益的医疗状况，如癌症和感染。
• Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
  申请人：Lycera Corporation

  公开号：US10208061B2

  公开（公告）日：2019-02-19

  The invention provides tetrahydro[1,8]naphthyridine and related compounds, pharmaceutical compositions, methods of promoting ROR activity, increasing the amount of IL-17 in a subject, and treating cancer using such tetrahydro[1,8]naphthyridine and related compounds.

  本发明提供了四氢[1,8]萘啶及相关化合物、药物组合物、促进 ROR 活性的方法、增加受试者体内 IL-17 含量的方法以及使用此类四氢[1,8]萘啶及相关化合物治疗癌症的方法。
• Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10221146B2

  公开（公告）日：2019-03-05

  The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

  本发明提供了某些式（I）的双环杂环化合物或其药学上可接受的盐，其中X1、X2、R1、R2、R3、R4和Cy如本文所定义。本发明还提供了包含这类式(I)化合物或其药学上可接受的盐的药物组合物，以及使用式(I)化合物或其药学上可接受的盐或包含它们的药物组合物治疗由RORgammaT介导的疾病或病症的方法。