1,2,3,4-Tetrahydro-2-chinolyl-essigsaeureamid | 5100-73-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1,2,3,4-Tetrahydro-2-chinolyl-essigsaeureamid
• 英文别名: 2-(1,2,3,4-tetrahydro-quinolin-2-yl)-acetamide；2-(1,2,3,4-Tetrahydroquinolin-2-yl)acetamide
• CAS: 5100-73-2
• 化学式: C₁₁H₁₄N₂O
• 分子量: 190.245
• InChiKey: AQWPGULTUCJUOE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] RORγ MODULATORS<br/>[FR] MODULATEURS DE ROR&Ggr;
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2015035278A1

  公开（公告）日：2015-03-12

  Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

  描述了公式（I）的RORγ调节剂，或其药学上可接受的盐，其中所有取代基在此处定义。该发明包括公式I化合物的立体异构体形式，包括立体异构纯、立体混合和消旋形式，以及其互变异构体。还提供了包含相同化合物的药物组合物。这些化合物和组合物在调节细胞中的RORγ活性的方法以及治疗患有疾病或紊乱的受试者的方法中是有用的，其中受试者在调节RORγ活性方面会从中获益，例如自身免疫和/或炎症性疾病。
• [EN] CYCLIC AMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF INFLAMMATION-RELATED DISORDERS MEDIATED BY BRADYKININ<br/>[FR] DERIVES AMINES CYCLIQUES ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES LIES A L'INFLAMMATION INDUITS PAR LA BRADYKININE
  申请人：AMGEN INC

  公开号：WO2004092164A1

  公开（公告）日：2004-10-28

  Compounds of formula (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation mediated by Bradykinin. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes wherein q, t, R, Ra, Rb, Rc and R2 are as defined herein.

  公式（I）的化合物对于治疗疼痛和疾病，如由炎症介导的疾病，具有有效性。该发明涵盖了新型化合物，其药学上可接受的衍生物，药物组合物以及用于预防和治疗涉及疼痛、由Bradykinin介导的炎症等疾病和其他疾病或病况的方法。该发明还涉及制备此类化合物的方法，以及在这些方法中有用的中间体，其中q、t、R、Ra、Rb、Rc和R2如本文所定义。
• CYCLIC AMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF INFLAMMATION-RELATED DISORDERS MEDIATED BY BRADYKININ
  申请人：Amgen, Inc.

  公开号：EP1633743A1

  公开（公告）日：2006-03-15
• RORGAMMA MODULATORS
  申请人：Bristol-Myers Squibb Company

  公开号：EP3044219A1

  公开（公告）日：2016-07-20