2-fluoro-N-(1,3-thiazol-2-yl)benzamide | 319-38-0

• 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: 2-fluoro-N-(1,3-thiazol-2-yl)benzamide
• CAS: 319-38-0
• 化学式: C₁₀H₇FN₂OS
• mdl: MFCD00454557
• 分子量: 222.24
• InChiKey: PPEREJLLBYEIRE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Novel heterocyclic NF-kB inhibitors
  申请人：Leban Johann

  公开号：US20060069102A1

  公开（公告）日：2006-03-30

  The present invention relates to compounds of the general formula (1) and salts and physiologically functional derivatives thereof, wherein R 1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R 2 is independently —NR 3 R 4 , R 3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R 4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 5 is independently H, COR 6 , CO 2 R 6 , SOR 6 , SO 3 R 6 , alkyl, cycloalkyl, alkoxy, —NH 2 , alkylamine, —NR 7 COR 6 , halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 6 is independently H, alkyl, cycloalkyl, —NH 2 , alkylamine, aryl or heteroaryl; R 7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO 2 .

  本发明涉及一般式（1）的化合物及其盐和生理功能衍生物，其中R1独立地为氢；烷基，环烷基，羟基烷基，卤代烷基，卤代烷氧基，芳基，取代芳基，杂芳基，取代杂芳基，芳基烷基或取代芳基烷基；R2独立地为—NR3R4，R3独立地为烷基，环烷基，烷氧基，烷基胺，—OH，—SH，烷硫基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基，R4独立地为烷基，环烷基，烷氧基，烷基胺，烷硫基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基；R5独立地为H，COR6，CO2R6，SOR6，SO3R6，烷基，环烷基，烷氧基，—NH2，烷基胺，—NR7COR6，卤素，—OH，—SH，烷硫基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基；R6独立地为H，烷基，环烷基，—NH2，烷基胺，芳基或杂芳基；R7独立地为H，烷基，环烷基，烷氧基，—OH，—SH，烷硫基，羟基烷基，芳基或杂芳基；p为0或1；q为0或1；X为CO或SO2。
• [EN] THIOHYDANTOIN ANDROGEN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CANCER<br/>[FR] ANTAGONISTES DU RÉCEPTEUR DES ANDROGÈNES THIOHYDANTOÏNE POUR LE TRAITEMENT DU CANCER
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2018037342A1

  公开（公告）日：2018-03-01

  Disclosed are compounds, compositions and methods for treating and/ or ameliorating diseases, syndromes, disorders, or conditions associated with AR mutant receptors linked to castration-resistant prostate cancer, in a subject, including a mammal and/or human, in need thereof, who has demonstrated resistance to a first or second generation AR antagonist, comprising, consisting of, and/or consisting essentially of, administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I) Formula (I) wherein R1, G, R10, and R11 are defined herein.

  本发明涉及化合物、组合物和方法，用于治疗和/或改善与与去势抵抗性前列腺癌相关的AR突变受体相关的疾病、综合征、障碍或病况，包括哺乳动物和/或人类在内，需要对第一代或第二代AR拮抗剂表现出抵抗性的对象。该方法包括、由以下组成或基本组成：向需要治疗的对象投与治疗有效量的I式化合物，其中R1、G、R10和R11在此被定义。
• Novel Heterocyclic NF-kB Inhibitors
  申请人：LEBAN Johann

  公开号：US20100004258A1

  公开（公告）日：2010-01-07

  The present invention relates to compounds of the general formula (III): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.

  本发明涉及一般式（III）的化合物：或其与酸或碱的药学上可接受的盐，或药学上可接受的前药或其立体异构体。
• Novel Heterocyclic Nf-Kb Inhibitors
  申请人：Leban Johann

  公开号：US20080261971A1

  公开（公告）日：2008-10-23

  The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R 1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R 2 is independently —NR 3 R 4 , (II) or (III) R 3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R 4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 5 is independently H, COR 6 , CO 2 R 6 , SOR 6 , SO 2 R 6 , SO 3 R 6 , alkyl, cycloalkyl, alkoxy, —NH 2 , alkylamine, —NR 7 COR 6 , halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 6 is independently H, alkyl, cycloalkyl, —NH 2 , alkylamine, aryl or heteroaryl; R 7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO 2 .

  本发明涉及一般式(I)的化合物及其盐和生理功能衍生物，其中R1独立地为氢、烷基、环烷基、羟基烷基、卤代烷基、卤代烷氧基、芳基、取代芳基、杂环芳基、取代杂环芳基、芳基烷基或取代芳基烷基；R2独立地为—NR3R4、(II)或(III)，其中R3独立地为烷基、环烷基、烷氧基、烷基胺、—OH、—SH、烷硫基、羟基烷基、卤代烷基、卤代烷氧基、芳基或杂环芳基，R4独立地为烷基、环烷基、烷氧基、烷基胺、烷硫基、羟基烷基、卤代烷基、卤代烷氧基、芳基或杂环芳基；R5独立地为H、COR6、CO2R6、SOR6、SO2R6、SO3R6、烷基、环烷基、烷氧基、—NH2、烷基胺、—NR7COR6、卤素、—OH、—SH、烷硫基、羟基烷基、卤代烷基、卤代烷氧基、芳基或杂环芳基；R6独立地为H、烷基、环烷基、—NH2、烷基胺、芳基或杂环芳基；R7独立地为H、烷基、环烷基、烷氧基、—OH、—SH、烷硫基、羟基烷基、芳基或杂环芳基；p为0或1；q为0或1；X为CO或SO2。
• NOVEL HETEROCYCLIC NF-kB INHIBITORS
  申请人：Leban Johann

  公开号：US20100048574A1

  公开（公告）日：2010-02-25

  The present invention relates to compounds of the general formula (II): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.

  本发明涉及通式(II)的化合物或其与酸或碱的药物可接受盐，或药物可接受的前药，或其立体异构体。