6-Methyl-2lambda6-thia-6-azaspiro[3.3]heptane 2,2-dioxide

• 分子结构分类: 有机化合物 - 有机硫化合物 - 磺酰类
• 英文名称: 6-Methyl-2lambda6-thia-6-azaspiro[3.3]heptane 2,2-dioxide
• 英文别名: 6-methyl-2λ6-thia-6-azaspiro[3.3]heptane 2,2-dioxide
• 化学式: C₆H₁₁NO₂S
• 分子量: 161.22
• InChiKey: VEBAEMDIPHZTFK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• 6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT
  申请人：Janssen Pharmaceutica NV

  公开号：US20170313691A1

  公开（公告）日：2017-11-02

  The present invention comprises compounds of Formula I. wherein: A 1 , A 2 , A 3 , A 4 , A 5 , R 1 , and R 2 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明涵盖了Formula I的化合物。 其中： A1，A2，A3，A4，A5，R1和R2在说明书中有定义。 该发明还涵盖了一种治疗或改善综合症、疾病或疾病的方法，其中该综合症、疾病为类风湿性关节炎或牛皮癣。该发明还涵盖了通过给哺乳动物施用Formula I中至少一种化合物的治疗有效量来调节RORγt活性的方法。
• OXINDOLE COMPOUNDS CARRYING A CO-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US20150344489A1

  公开（公告）日：2015-12-03

  The present invention relates to novel substituted oxindole derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising compounds I and their use for the treatment of vasopressin-related disorders.

  本发明涉及公式I的新型取代氧吲哚衍生物，其中变量如权利要求和描述中所定义。该发明还涉及包含化合物I的药物组合物，以及它们用于治疗与加压素相关的疾病。
• BICYCLO 2,3-BENZODIAZEPINES AND SPIROCYCLICALLY SUBSTITUTED 2,3-BENZODIAZEPINES
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160129011A1

  公开（公告）日：2016-05-12

  BET-protein-inhibitory, in particular BRD4-inhibitory bicyclo- and spirocyclically substituted 2,3-benzodiazepines of the general formula (I), pharmaceutical compositions comprising the compounds according to the invention, and the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders, are described. Furthermore, the use of BET protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control is described.

  BET蛋白抑制剂，特别是BRD4抑制剂，具有一般式(I)的双环和螺环替代的2,3-苯二氮䓬类化合物，以及包含该发明化合物的药物组合物，以及其用于治疗过度增殖性疾病，特别是肿瘤性疾病的预防和治疗方法被描述。此外，描述了BET蛋白抑制剂在良性增生、动脉粥样硬化疾病、败血症、自身免疫疾病、血管疾病、病毒感染、神经退行性疾病、炎症性疾病、动脉粥样硬化疾病和男性生育控制中的用途。
• TRICYCLIC COMPOUNDS USEFUL AS NEUROGENIC AND NEUROPROTECTIVE AGENTS
  申请人：INCEPTION 1, INC.

  公开号：US20140243313A1

  公开（公告）日：2014-08-28

  The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases.

  本发明涉及公式I化合物及其药学上可接受的盐，其在治疗神经退行性疾病和促进哺乳动物大脑中神经元的生成或存活方面有用。本发明还包括含有公式I化合物或其药学上可接受的盐的治疗有效量的药物组合物。本发明还涉及一种在神经退行性和相关疾病患者中促进神经元的生成或存活的方法。
• TRIFLUOROMETHYL ALCOHOLS AS MODULATORS OF RORyt
  申请人：Janssen Pharmaceutica NV

  公开号：US20160122336A1

  公开（公告）日：2016-05-05

  The present invention comprises compounds of Formula I. wherein: X, A 1 , A 2 , A 3 , A 4 , R 1 , R 2 , and R 3 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

  本发明涉及I式化合物，其中：X，A1，A2，A3，A4，R1，R2和R3在说明书中有定义。本发明还涉及一种治疗或改善综合症、障碍或疾病的方法，其中所述的综合症、障碍或疾病是类风湿性关节炎或银屑病。本发明还涉及一种通过给哺乳动物投予至少一种权利要求1中的化合物的治疗有效量来调节RORγt活性的方法。