(2-氨基-苯基)-甲磺酸酰胺 | 344750-18-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (2-氨基-苯基)-甲磺酸酰胺
• 中文别名: (2-氨基苯基)甲磺酰胺
• 英文名称: (2-amino-phenyl)-methanesulfonic acid amide
• 英文别名: (2-Amino-phenyl)-methansulfonsaeure-amid；(2-Aminophenyl)methanesulfonamide
• CAS: 344750-18-1
• 化学式: C₇H₁₀N₂O₂S
• mdl: MFCD08436679
• 分子量: 186.235
• InChiKey: AESAOFCUDMECSQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  94.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (2-氨基-苯基)-甲磺酸酰胺 在 溴 作用下， 生成 7-bromo-3,5-dihydro-benzo[e][1,2,4]thiadiazepine-4,4-dioxide
  参考文献：
  名称：

  Synthesis of Derivatives of a New Heterocyclic Ring. 1,3-Dihydro-2,3,5-benzothiadiazepine 2,2-Dioxide

  摘要：

  DOI：

  10.1021/ja01527a044
• 作为产物：
  描述：

  2-nitrophenylmethanesulfonamide 在 palladium on activated charcoal 氢气 作用下， 以 乙醇 为溶剂， 40.0 ℃ 、413.68 kPa 条件下， 反应 8.0h， 生成 (2-氨基-苯基)-甲磺酸酰胺
  参考文献：
  名称：

  抗高血脂的N-苄基氨基磺酸盐，N-苄基氨基磺酸盐和苄基磺酰胺的结构活性研究

  摘要：

  已经制备了一系列芳基取代的N-苯甲酰基-和N-苄基氨基磺酸钠盐和苄基磺酰胺钠盐，并以20 mg / kg / d ip ip水平在雄性CF1小鼠中检测了16 d的降血脂活性。这些物质也接受了毒理学评估和化学稳定性研究。通常，氨基磺酸盐和磺酰胺都显着降低了小鼠的血清胆固醇和甘油三酸酯水平。该化合物是非致突变性的，在雄性小鼠中没有显示出急性毒性或肝或肾功能受损，并且在3.5-7.4的pH范围内，作为一水合物和水溶液都具有化学稳定性。虽然这一系列的氨基磺酸盐和磺酰胺盐都降低了血清胆固醇和甘油三酸酯的水平，

  DOI：

  10.1002/jps.2600730321

文献信息

• 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。
• Inhibitors of protein kinases
  申请人：Schauerte Heike

  公开号：US20080275063A1

  公开（公告）日：2008-11-06

  The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceutical compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

  本发明提供了新化合物。这些化合物可用作CDK5抑制剂，因此它们可以包含在药物组合物中，用于治疗任何类型的疼痛、炎症性疾病、免疫性疾病、增殖性疾病、传染病、心血管疾病和神经退行性疾病。
• Pyrazole-amides and -sulfonamides
  申请人：Atkinson N. Robert

  公开号：US20050049237A1

  公开（公告）日：2005-03-03

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazole-amides and -sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.

  本发明提供了一种通过抑制电压依赖性钠通道中的钠离子流来治疗疾病的化合物、组合物和方法。更具体地，本发明提供了吡唑酰胺和磺酰胺，以及其组合物和方法，这些化合物、组合物和方法对于治疗中枢或外周神经系统疾病特别是疼痛和慢性疼痛非常有用，通过阻止与所述疾病的发作或复发有关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制包括PN3亚基的通道中的离子流来治疗神经病理性或炎性疼痛。
• PYRAZOLE-AMIDES AND -SULFONAMIDES
  申请人：Atkinson N. Robert

  公开号：US20080064690A1

  公开（公告）日：2008-03-13

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazole-amides and -sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.

  本发明提供了一种通过抑制电压依赖性钠通道中的钠离子通量来治疗疾病的化合物、组合物和方法。更具体地，本发明提供了嘧唑酰胺和磺酰胺、组合物和方法，用于治疗中枢或外周神经系统障碍，特别是疼痛和慢性疼痛，通过阻断与指示条件的发生或复发有关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制包括PN3亚单位的通道中的离子通量来治疗神经病理性或炎症性疼痛。
• Antihyperlipidemic N-benzoylsulfamates, N-benzylsulfamates and benzylsulfonamides, a therapeutic composition containing same and a process for the production thereof
  申请人：Research Corporation

  公开号：EP0135927A2

  公开（公告）日：1985-04-03

  This invention relates to novel N-benzoylsulfamates, N-benzylsulfamates and benzylsulfonamides and pharmacologically acceptable salts thereof, a method for the production thereof and a therapeutic composition containing same. The new compounds are useful for lowering serum levels in mammals by administration of said compounds.

  本发明涉及新型 N-苯甲酰基氨基磺酸盐、N-苄基氨基磺酸盐和苄基氨基磺酸盐及其药理学上可接受的盐类、其生产方法和含有这些物质的治疗组合物。这些新化合物可通过给哺乳动物施用上述化合物来降低其血清水平。