3-(2,6-dichloro-4-trifluoromethylphenylamino)-N-(2-hydroxyethyl)-benzenesulfonamide | 1159282-09-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-(2,6-dichloro-4-trifluoromethylphenylamino)-N-(2-hydroxyethyl)-benzenesulfonamide
• 英文别名: 3-[2,6-dichloro-4-(trifluoromethyl)anilino]-N-(2-hydroxyethyl)benzenesulfonamide
• CAS: 1159282-09-3
• 化学式: C₁₅H₁₃Cl₂F₃N₂O₃S
• 分子量: 429.247
• InChiKey: IZTDMRKDOWDBPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  86.8
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• Spirocyclobutyl Piperidine Derivatives
  申请人：Bernstein Peter

  公开号：US20100130477A1

  公开（公告）日：2010-05-27

  Disclosed herein is at least one spirocyclobutyl piperidine derivative, at least one pharmaceutical composition comprising at least one spirocyclobutyl piperidine derivative disclosed herein, and at least one method of using at least one spirocyclobutyl piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.

  披露至少一种螺环环丁基哌啶衍生物，至少一种包含本文披露的至少一种螺环环丁基哌啶衍生物的药物组合物，以及至少一种使用本文披露的至少一种螺环环丁基哌啶衍生物治疗至少一种组胺H3受体相关状况的方法。
• POTASSIUM ION CHANNEL MODULATORS AND USES THEREOF
  申请人：Edwards Simon David

  公开号：US20120065270A1

  公开（公告）日：2012-03-15

  Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs wherein: Ar 1 and Ar 2 =aryl or heteroaryl; a=0 to 5; R 1 =alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R 1 is the same or different; b=0 to 5; R 2 =alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and where b is >1, each R 2 is the same or different; V=(CR 3a R 3b ) p SO 2 N(R 3b )X and (CR 3a R 3b ) p N(R 3b )SO 2 (X); W=NR 4a , O, S, S═O, SO 2 and C(R 4a R 4b ) 2 ; X=hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with ≧1 NR8R9 groups wherein R8 and R9+nitrogen atom form a saturated or partially unsaturated heterocyclic group which is optionally further substituted by ≧1 substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monoalkylamino, dialkylamino and hydroxyl; Y and Z each ═(CR 5a R 5b ) n1 , C═O, SO 2 , C(═O)NR 5a , C(═O)NR 5a SO 2 or C═O(R 5a R 5b ) n2 ; R 3a , R 3b , R 4a , R 4b , R 5a and R 5b each=hydrogen, alkyl, cycloalkyl, aryl or heteroaryl; n1 and n2 each =0 to 2; and p=0 to 2; are excellent selective modulators of potassium ion flux through KCNQ2, KCNQ3 and/or KCNQ2/3 channels, making them of use in treating and preventing a number of conditions including pain and lower urinary tract disorders.

  公式（I）的化合物及其药理学上可接受的盐和前药，其中： Ar1和Ar2 = 芳基或杂环芳基; a = 0到5; R1 = 烷基，卤素，卤代烷基，烷氧基，烷氧羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰胺基，烷氧羰基氨基，烷基磺酰基，烷基磺酰胺基和氰基，当a> 1时，每个R1相同或不同; b = 0到5; R2 = 烷基，卤素，卤代烷基，烷氧基，烷氧羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰胺基，烷氧羰基氨基，烷基磺酰基，烷基磺酰胺基和氰基，当b> 1时，每个R2相同或不同; V =（CR3aR3b）pSO2N（R3b）X和（CR3aR3b）pN（R3b）SO2（X）; W = NR4a，O，S，S═O，SO2和C（R4aR4b）2; X = 羟基烷基，烷氧基烷基，卤代烷氧基烷基，芳氧基烷基，聚烷基乙二醇残基，氨基烷基，单烷基氨基烷基，二烷基氨基烷基和被≧1个NR8R9基取代的烷基，其中R8和R9 +氮原子形成饱和或部分不饱和的杂环基团，该杂环基团可以选择地进一步取代为≧1个取代基，所选取代基从烷基，卤素，卤代烷基，烷氧基，烷氧羰基，羧基，硝基，氨基，单烷基氨基，二烷基氨基和羟基中选择; Y和Z各自═（CR5aR5b）n1，C═O，SO2，C（═O）NR5a，C（═O）NR5aSO2或C═O（R5aR5b）n2; R3a，R3b，R4a，R4b，R5a和R5b各自为氢，烷基，环烷基，芳基或杂环芳基; n1和n2各自= 0到2; p = 0到2; 它们是钾离子通量通过KCNQ2，KCNQ3和/或KCNQ2/3通道的优异选择性调节剂，因此可用于治疗和预防包括疼痛和下尿路障碍在内的多种疾病。
• Cyclopropyl Amide Derivatives 978
  申请人：Arnold James

  公开号：US20090076020A1

  公开（公告）日：2009-03-19

  Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.

  本公开至少包括一种环丙基酰胺衍生物，至少包括一种含有本公开的至少一种环丙基酰胺衍生物的药物组合物，以及至少包括一种使用本公开的至少一种环丙基酰胺衍生物用于治疗至少一种与组织胺H3受体相关疾病的方法。
• Cyclopropyl Amide Derivatives '978
  申请人：Arnold James

  公开号：US20120065193A1

  公开（公告）日：2012-03-15

  Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.

  本文披露了至少一种环丙基酰胺衍生物，至少一种包含本文披露的至少一种环丙基酰胺衍生物的药物组合物，以及使用本文披露的至少一种环丙基酰胺衍生物治疗至少一种组织胺H3受体相关疾病的至少一种方法。
• CYCLOPROPYL AMIDE DERIVATIVES
  申请人：ASTRAZENECA AB

  公开号：US20150216861A1

  公开（公告）日：2015-08-06

  Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.

  本文披露了至少一种环丙基酰胺衍生物，至少一种包含本文披露的至少一种环丙基酰胺衍生物的药物组合物，以及至少一种使用本文披露的至少一种环丙基酰胺衍生物治疗至少一种组织胺H3受体相关疾病的方法。