(R)-1-(5-chloro-6-methyl-1-(5-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)-piperidine-4-carboxamide | 1268712-61-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (R)-1-(5-chloro-6-methyl-1-(5-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)-piperidine-4-carboxamide
• 英文别名: (R)-1-(5-chloro-6-methyl-1-(5-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)-piperidine-4-carboxaniide；1-[5-chloro-6-methyl-1-[5-(trifluoromethyl)pyridin-2-yl]benzimidazol-2-yl]-N-[(3R)-oxolan-3-yl]piperidine-4-carboxamide
• CAS: 1268712-61-3
• 化学式: C₂₄H₂₅ClF₃N₅O₂
• 分子量: 507.943
• InChiKey: QECAXCOOSOUHJQ-QGZVFWFLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  35
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  72.3
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 (MPGES1) INHIBITORS<br/>[FR] INHIBITEURS DE PROSTAGLANDINE E SYNTHASE-1 (MPGES1) MICROSOMALE
  申请人：NOVASAID AB

  公开号：WO2011023812A1

  公开（公告）日：2011-03-03

  A compound of formula (I): as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from inflammatory diseases, nociceptive pain, auto-immune disease, breathing disorders, fever, cancer, inflammation related anorexia, Alzheimer's disease and cardiovascular diseases.

  公式（I）的化合物，以及其药用盐，以及包括该化合物的药物组合物。该化合物用于治疗选择自炎性疾病、伤害性疼痛、自身免疫疾病、呼吸系统疾病、发热、癌症、与炎症相关的厌食症、阿尔茨海默病和心血管疾病的紊乱。
• [EN] NOVEL PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGES-1 INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS PIPÉRIDINYLE BENZOIMIDAZOLE UTILISÉS COMME INHIBITEURS DE LA MPGES-1
  申请人：CADILA PHARMACEUTICALS LTD

  公开号：WO2014204370A1

  公开（公告）日：2014-12-24

  The compounds 1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol- 2-yl)-N-((3S,4R)-4-hydroxytetrahydrofuran-3-yl)piperidine-4-carboxamide and l-(6-chloro-5- methy1-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-((3S,4R)-4- hydroxytetrahydrofuran-3-yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of these compounds. The compound are useful for the treatment and/or prevention of a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia.

  化合物1-(5-氯-6-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-((3S,4R)-4-羟基四氢呋喃-3-基)哌啶-4-甲酰胺和1-(6-氯-5-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-((3S,4R)-4-羟基四氢呋喃-3-基)哌啶-4-甲酰胺，以及其药学上可接受的盐，以及包含这些化合物中任何一种的药物组合物。这些化合物可用于治疗和/或预防选择自炎症性疾病；自身免疫疾病；疼痛；呼吸障碍；癌症；心血管疾病；神经退行性疾病；骨疾病；由家族性腺瘤性息肉症（FAP）病情导致的障碍；膀胱过度活跃；发热；以及与炎症相关的厌食症的障碍。
• [EN] PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGE-1 INHIBITORS<br/>[FR] DÉRIVÉS DE PIPÉRIDINYLBENZOIMIDAZOLE UTILISÉS COMME INHIBITEURS DE MPGE-1
  申请人：CADILA PHARMACEUTICALS LTD

  公开号：WO2014204371A1

  公开（公告）日：2014-12-24

  The compounds (R)-1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H- benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide and (R)-1-(6-chloro- -methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3- yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of thesecompounds. The compoundsareuseful for the treatmentand/or preventionof a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia.

  化合物(R)-1-(5-氯-6-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-(四氢呋喃-3-基)哌啶-4-羧酰胺和(R)-1-(6-氯-6-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-(四氢呋喃-3-基)哌啶-4-羧酰胺，以及其药学上可接受的盐，以及包含这些化合物中的任何一种的药物组合物。这些化合物可用于治疗和/或预防炎症性疾病；自身免疫疾病；疼痛；呼吸障碍；癌症；心血管疾病；神经退行性疾病；骨疾病；由家族性腺瘤性息肉症（FAP）引起的疾病；膀胱过度活跃；发热；以及与炎症相关的厌食症。
• NOVEL PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGES-1 INHIBITORS
  申请人：NovaSAID AB

  公开号：US20160194308A1

  公开（公告）日：2016-07-07

  The compounds 1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-((3S,4R)-4-hydroxytetrahydrofuran-3-yl)piperidine-4-carboxamide and 1-(6-chloro-5-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-((3S,4R)-4-hydroxytetrahydrofuran-3-yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of these compounds. The compound are useful for the treatment and/or prevention of a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia.

  化合物1-(5-氯-6-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-((3S,4R)-4-羟基四氢呋喃-3-基)哌啶-4-羧酰胺和1-(6-氯-5-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-((3S,4R)-4-羟基四氢呋喃-3-基)哌啶-4-羧酰胺，以及其药学上可接受的盐，和包含这些化合物中的任何一种的药物组合物。这些化合物可用于治疗和/或预防炎症性疾病；自身免疫性疾病；疼痛；呼吸系统疾病；癌症；心血管疾病；神经退行性疾病；骨质疾病；由家族性腺瘤性息肉症（FAP）引起的疾病；过度活跃的膀胱；发热；和与炎症相关的厌食症。
• PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGE-1 INHIBITORS
  申请人：NOVASAID AB

  公开号：US20160122330A1

  公开（公告）日：2016-05-05

  The compounds (R)-1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide and (R)-1-(6-chloro-1-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of these compounds. The compounds are useful for the treatment and/or prevention of a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia.

  化合物(R)-1-(5-氯-6-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-(四氢呋喃-3-基)哌啶-4-羧酰胺和(R)-1-(6-氯-1-甲基-1-(6-(三氟甲基)吡啶-2-基)-1H-苯并[d]咪唑-2-基)-N-(四氢呋喃-3-基)哌啶-4-羧酰胺，以及其药学上可接受的盐，以及包含这些化合物中任何一种的药物组合物。这些化合物可用于治疗和/或预防以下疾病：炎症性疾病；自身免疫性疾病；疼痛；呼吸系统疾病；癌症；心血管疾病；神经退行性疾病；骨疾病；由家族性腺瘤性息肉症（FAP）引起的疾病；过度活跃的膀胱；发热；以及与炎症相关的厌食症。