2-chloro-N-methylpyridine-3-sulfonamide | 38030-51-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-chloro-N-methylpyridine-3-sulfonamide
• 英文别名: N-Methyl-2-chlor-3-pyridinsulfonamid；2-chloro-pyridine-3-sulfonic acid methylamide
• CAS: 38030-51-2
• 化学式: C₆H₇ClN₂O₂S
• 分子量: 206.653
• InChiKey: TXPOXFGONQEPTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-chloro-N-methylpyridine-3-sulfonamide 以80%的产率得到
  参考文献：
  名称：

  THUNUS L.; LAPIERE C.-L., ANN. PHARM. FRANC. , 1975 (1976), 33, NO 12, 663-669

  摘要：

  DOI：
• 作为产物：
  描述：

  2-溴-3-氨基吡啶 在 盐酸 、 三乙胺 、 sodium nitrite 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 4.17h， 生成 2-chloro-N-methylpyridine-3-sulfonamide
  参考文献：
  名称：

  钯催化多米诺反应合成 3-氨基 1,2,4-苯并噻二嗪 1,1-二氧化物

  摘要：

  磺胺类药物在药物化学中无处不在。由于其多种生物活性，它们被广泛用作具有抗微生物、抗糖尿病、抗高血压或抗炎特性的畅销药物。1最常用的两种磺胺类药物是呋塞米 ( A ) 2和氯噻嗪 ( B )（方案 1）3，根据世界卫生组织 (WHO) 的规定，它们属于基本药物。4呋塞米 ( A ) 是一种袢利尿剂，而2氯噻嗪 ( B ) 是一种抗高血压和利尿剂。3除了在药物化学中的应用外，磺胺类药物还广泛用于作物保护，5以环丙磺酰胺 ( C )为例。5a、6 方案一 在图查看器中打开微软幻灯片软件 生物学相关磺胺类药物和磺内酰胺制备合成方法的示例。 在生物活性磺酰胺类化合物中，称为磺内酯的相应杂环化合物在新活性药物成分的开发中引起了特别的兴趣。7例子包括 1,2,4-苯并噻二嗪 1,1-二氧化物 氯噻嗪 ( B ) 或二氮嗪 ( D )，8两者均显示出多种药理活性。9同样，它们相关的 3-氨基取代衍生物E 10和F

  DOI：

  10.1002/adsc.202300875

文献信息

• [EN] BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS<br/>[FR] DERIVES DE BENZIMIDAZOLES ET UTILISATION DE CEUX-CI EN TANT QUE LIGANDS DU RECEPTEUR VANILLOIDE
  申请人：AMGEN INC

  公开号：WO2004035549A1

  公开（公告）日：2004-04-29

  Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.

  式（I）的化合物在治疗辣椒素受体介导的疾病方面很有用，如炎症性或神经病痛以及涉及感觉神经功能的疾病，如哮喘、类风湿性关节炎、骨关节炎、炎症性肠道疾病、尿失禁、偏头痛和牛皮癣。
• Vanilloid receptor ligands and their use in treatments
  申请人：Amgen Inc.

  公开号：US20040152690A1

  公开（公告）日：2004-08-05

  Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, bums, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

  治疗苯并咪唑和含有苯并咪唑的组合物，用于治疗急性、炎症性和神经痛、牙痛、普通头痛、偏头痛、集群头痛、混合血管和非血管综合症、紧张性头痛、一般炎症、关节炎、风湿病、骨关节炎、炎症性肠病、炎症性眼疾、炎症性或不稳定的膀胱疾病、牛皮癣、带有炎症成分的皮肤疾病、慢性炎症病状、炎症性疼痛及相关的高敏感性和痛觉过敏、神经痛及相关的高敏感性和痛觉过敏、糖尿病神经病疼痛、烧伤后疼痛、交感神经维持性疼痛、去神经症候群、哮喘、上皮组织损伤或功能障碍、单纯疱疹、呼吸、泌尿、胃肠或血管区域内脏运动障碍、伤口、烧伤、过敏性皮肤反应、瘙痒、白癜风、一般胃肠道疾病、胃溃疡、十二指肠溃疡、腹泻、由坏死性剂引起的胃病变、头发生长、血管运动或过敏性鼻炎、支气管疾病或膀胱疾病。
• HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS, IN PARTICULAR AS ANTI-ALZHEIMER AGENTS
  申请人：Marsais Francis

  公开号：US20090062279A1

  公开（公告）日：2009-03-05

  The invention is related to compound which comprises at least one radical C═Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C═Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

  本发明涉及一种化合物，其包含至少一个基团C═Y，其中Y为O或S，以及一个可氧化且不可质子化的氮原子N，其中在氧化时，基团C═Y的至少一个碳原子与氮原子之间的距离(d)在0.3至0.8纳米之间。本发明涉及由公式G定义的新杂环化合物及其制备方法，涉及包含它们的制药组合物以及它们在治疗神经退行性或阿尔茨海默病方面的用途。
• VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS
  申请人：Balan Chenera

  公开号：US20090143575A1

  公开（公告）日：2009-06-04

  Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

  治疗苯并咪唑及其含量物，用于急性、炎症性和神经痛、牙痛、一般头痛、偏头痛、集群性头痛、混合血管和非血管综合症、紧张型头痛、一般炎症、关节炎、风湿性疾病、骨关节炎、炎症性肠病、炎症性眼病、炎症性或不稳定的膀胱疾病、牛皮癣、有炎症成分的皮肤病、慢性炎症状况、炎症性疼痛和相关的高敏感性和触痛、神经痛和相关的高敏感性和触痛、糖尿病神经病疼痛、烧伤后疼痛、交感神经维持的疼痛、去感觉综合症、哮喘、上皮组织损伤或功能障碍、单纯疱疹、呼吸、泌尿、胃肠或血管区域内脏运动障碍、伤口、烧伤、过敏性皮肤反应、瘙痒、白癜风、一般胃肠疾病、胃溃疡、十二指肠溃疡、腹泻、坏死性剂引起的胃损伤、头发生长、血管运动或过敏性鼻炎、支气管疾病或膀胱疾病。
• New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents
  申请人：Institut National des Sciences Appliquees de Rouen (INSA)

  公开号：EP1731507A1

  公开（公告）日：2006-12-13

  The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

  本发明涉及由至少一个基团C=Y（Y为O或S）和一个可氧化且不可质子化的氮原子N组成的化合物，其中基团C=Y的至少一个碳原子与氮原子之间的距离（d）在氧化时介于0.3至0.8纳米之间。 本发明涉及由式 G 定义的新杂环化合物、 它们的制备、包含它们的药物组合物以及它们作为治疗剂的用途，特别是在治疗神经退行性疾病或阿尔茨海默病中的用途。