(R)-4-(5-((R)-1,2-dihydroxyethyl)-3-fluoropyridin-2-yl)-2-methyl-N-(6-methylbenzo[d]thiazol-2-yl)piperazine-1-carboxamide | 1416788-54-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (R)-4-(5-((R)-1,2-dihydroxyethyl)-3-fluoropyridin-2-yl)-2-methyl-N-(6-methylbenzo[d]thiazol-2-yl)piperazine-1-carboxamide
• 英文别名: (2R)-4-[5-[(1R)-1,2-dihydroxyethyl]-3-fluoropyridin-2-yl]-2-methyl-N-(6-methyl-1,3-benzothiazol-2-yl)piperazine-1-carboxamide
• CAS: 1416788-54-9
• 化学式: C₂₁H₂₄FN₅O₃S
• 分子量: 445.518
• InChiKey: MOYYIRTYGZTKTA-DYVFJYSZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  130
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• FUNCTIONALLY-MODIFIED OLIGONUCLEOTIDES AND SUBUNITS THEREOF
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140330006A1

  公开（公告）日：2014-11-06

  Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

  提供了包含修改的亚单位间连接和/或修改的3'和/或5'-末端基团的功能修饰寡核苷酸类似物。所公开的化合物对于治疗需要抑制蛋白质表达或纠正异常mRNA剪接产物以产生有益治疗效果的疾病是有用的。
• TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF
  申请人：Ando Shigeru

  公开号：US20140329829A1

  公开（公告）日：2014-11-06

  The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R 1 , R 4 , R 8 , R 9 , and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.

  本公开涉及化合物公式(I)及其药学上可接受的衍生物，其中R1，R4，R8，R9和m的定义如本文所述，包括含有化合物公式(I)或其药学上可接受的衍生物的有效量的组合物，以及用于治疗或预防疼痛、与骨关节炎相关的疼痛、骨关节炎、尿失禁、溃疡、炎症性肠病和肠易激综合征等疾病的方法，包括向需要治疗的动物中施用化合物公式(I)或其药学上可接受的衍生物的有效量。
• TRPV1 antagonists including dihydroxy substituent and uses thereof
  申请人：Purdue Pharma L.P.

  公开号：US10450308B2

  公开（公告）日：2019-10-22

  The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.

  本公开涉及式 (I) 化合物 及其药学上可接受的衍生物，其中 R1、R4、R8、R9 和 m 如本文所定义；包含有效量的式 (I) 化合物或其药学上可接受的衍生物的组合物；以及治疗或预防诸如疼痛、与骨关节炎相关的疼痛、骨关节炎、UI、溃疡、IBD 和 IBS 等病症的方法，包括向有需要的动物施用有效量的式 (I) 化合物或其药学上可接受的衍生物。
• [EN] TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF<br/>[FR] ANTAGONISTES DE TRPV1 COMPRENANT UN SUBSTITUANT DIHYDROXY ET LEURS UTILISATIONS
  申请人：PURDUE PHARMA LP

  公开号：WO2012176061A9

  公开（公告）日：2013-03-14
• US9273043B2
  申请人：——

  公开号：US9273043B2

  公开（公告）日：2016-03-01