Nbi-921352 | 2154406-04-7

• 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: Nbi-921352
• 英文别名: 4-[[(3S)-1-benzylpyrrolidin-3-yl]-methylamino]-2-fluoro-5-methyl-N-(1,3-thiazol-4-yl)benzenesulfonamide
• CAS: 2154406-04-7
• 化学式: C₂₂H₂₅FN₄O₂S₂
• 分子量: 460.6
• InChiKey: UCSHINHOAVARGQ-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  102
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS<br/>[FR] COMPOSÉS BENZÈNESULFONAMIDES ET LEUR UTILISATION EN TANT QU'AGENTS THÉRAPEUTIQUES
  申请人：XENON PHARMACEUTICALS INC

  公开号：WO2017201468A1

  公开（公告）日：2017-11-23

  This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.

  本发明涉及苯磺酰胺化合物，包括它们的立体异构体、对映异构体、互变异构体或其混合物；或用于治疗与电压门控钠通道相关的疾病或病症的药用可接受盐、溶剂化物或前药，例如癫痫。
• Benzenesulfonamide compounds and their use as therapeutic agents
  申请人：Xenon Pharmaceuticals Inc.

  公开号：US10246453B2

  公开（公告）日：2019-04-02

  This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.

  本发明涉及苯磺酰胺化合物，作为其立体异构体、对映体、同系物或其混合物；或其药学上可接受的盐、溶液剂或原药，用于治疗与电压门控钠通道相关的疾病或病症，如癫痫。
• BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS
  申请人：Xenon Pharmaceuticals Inc.

  公开号：EP3458449A1

  公开（公告）日：2019-03-27
• [EN] PHARMACEUTICAL FORMULATIONS FOR TREATING DISEASES ASSOCIATED WITH VOLTAGE-GATED SODIUM CHANNELS<br/>[FR] FORMULATIONS PHARMACEUTIQUES POUR LE TRAITEMENT DE MALADIES ASSOCIÉES À DES CANAUX SODIQUES SENSIBLES À LA TENSION
  申请人：[en]XENON PHARMACEUTICALS INC.

  公开号：WO2022077094A1

  公开（公告）日：2022-04-21

  Provided herein are certain pharmaceutical compositions comprising (S)-4-(( 1 -benzylpyrrolidin-3 -yl)(methyl)amino)-2-fluoro-5-methyl-N-(thiazol-4-yl)benzenesulfonamide (Compound A), or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient. The pharmaceutical compositions can be present in form of an immediate release tablet, a granular formulation, a stable suspension oral dosage form or a multi-particulate sprinkle dosage form. Methods for the treatment of a disease or a condition associated with Naj4.6 activity, such as epilepsy, are described.
• [EN] USE OF THE NAVI.6 SODIUM CHANNEL BLOCKER (S)-4-((1-BENZYLPYRROLIDIN-3-YL)(METHYL)AMINO)-2-FLUORO-5-METHYL-N( THIAZOL-4-YL)BENZENESULFONAMIDE, TOGETHER WITH STRONG INDUCERS OF CYTOCHROME P450 3A4, IN THE TREATMENT OF CONDITIONS ASSOCIATED WITH NAV1.6 ACTIVITY<br/>[FR] UTILISATION DU BLOQUEUR DU CANAL SODIQUE NAV1.6, LE (S)-4-((1-BENZYLPYRROLIDIN-3-YL))(MÉTHYL) AMINO)-2-FLUORO-5-MÉTHYL-N(THIAZOL-4-YL) BENZÈNESULFONAMIDE, CONJOINTEMENT AVEC DES INDUCTEURS FORTS DU CYTOCHROME P450 3A4, DANS LE TRAITEMENT D'ÉTATS ASSOCIÉS À L'ACTIVITÉ NAV1.6
  申请人：[en]XENON PHARMACEUTICALS INC.

  公开号：WO2022077095A1

  公开（公告）日：2022-04-21

  Provided are methods for treating diseases or conditions associated with Nav1.6 activity in a patient, comprising administering to said patient (S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2-fluoro-5-methyl-N(thiazol-4-yl)benzenesulfonamide or a pharmaceutically acceptable salt thereof, wherein the patient is also being administered a strong inducer of cytochrome P450 3A4 (CYP3A4).