美布噻嗪甲丁噻嗪 | 3568-00-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 中文名称: 美布噻嗪甲丁噻嗪
• 中文别名: 美布噻嗪；己氯噻嗪
• 英文名称: mebutizide
• 英文别名: 6-Chlor-3-<1,2-dimethyl-butyl>-7-sulfamoyl-3,4-dihydro-<1,2,4>-benzothiadiazin-1,1-dioxid；6-chloro-3-(1,2-dimethyl-butyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ⁶-benzo[1,2,4]thiadiazine-7-sulfonic acid amide；6-chloro-3-(3-methylpentan-2-yl)-1,1-dioxo-3,4-dihydro-2H-1λ6,2,4-benzothiadiazine-7-sulfonamide
• CAS: 3568-00-1
• 化学式: C₁₃H₂₀ClN₃O₄S₂
• 分子量: 381.904
• InChiKey: KJLLKLRVCJAFRY-UHFFFAOYSA-N

物化性质

• 熔点：
  >188°C (dec.)
• 溶解度：
  DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  135
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2,3-dimethylpentan-1-amine 、 4-amino-2-chloro-5-iodobenzenesulfonamide 在 双(二氧化硫)-1,4-二氮杂双环[2.2.2]辛烷加合物 、 氧气 、 palladium diacetate 、 caesium carbonate 作用下， 以 二甲基亚砜 为溶剂， 以70 %的产率得到美布噻嗪甲丁噻嗪
  参考文献：
  名称：

  钯催化插入二氧化硫的邻碘苯胺氨基磺酰化合成 3,4-二氢苯并噻二嗪 1,1-二氧化物

  摘要：

  开发了一种简单高效的 Pd 催化氧化环化系统，用于化学和区域选择性合成 3,4-二氢苯并噻二嗪 1,1-二氧化物，该化合物是通过邻碘苯胺与 SO 2 的氨基磺酰化形成的。DABSO用作SO 2源，有机化合物O 2用作氧化剂。这种直接的 C-S、S-N 和 C-N 官能化非常有效，并且观察到广泛的官能团耐受性，从而产生中等至优异的 3,4-二氢-苯并噻二嗪 1,1-二氧化物。此外，该方法适合克级合成。

  DOI：

  10.1021/acs.orglett.3c02683

文献信息

• Nitrosated and nitrosylated diuretic compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20050059655A1

  公开（公告）日：2005-03-17

  The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; and (l) treating nephropathy.

  该发明描述了新颖的亚硝基化和/或亚硝酰化利尿化合物或其药用盐，以及包含至少一种亚硝基化和/或亚硝酰化利尿化合物的新型组合物，以及可选地至少一种一氧化氮供体和/或至少一种治疗剂。该发明还提供了包含该发明中至少一种利尿化合物的新型组合物和试剂盒，该利尿化合物可选择地亚硝基化和/或亚硝酰化，并且可选地至少一种一氧化氮供体化合物和/或至少一种治疗剂。该发明还提供了用于(a)治疗由于过多水分和/或电解贮留引起的疾病；(b)治疗心血管疾病；(c)治疗肾血管疾病；(d)治疗糖尿病；(e)治疗由氧化应激引起的疾病；(f)治疗内皮功能障碍；(g)治疗由内皮功能障碍引起的疾病；(h)治疗肝硬化；(j)治疗子痫前期；(k)治疗骨质疏松症；和(l)治疗肾病的方法。
• Nitric oxide enhancing diuretic compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20060189603A1

  公开（公告）日：2006-08-24

  The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

  该发明描述了包含至少一种增强一氧化氮利尿化合物或其药用盐的新型组合物和试剂盒，以及可选地，至少一种增强一氧化氮化合物和/或至少一种治疗剂的试剂盒。该发明还提供了以下方法：(a)治疗由过多水分和/或电解贮留引起的症状；(b)治疗心血管疾病；(c)治疗肾血管疾病；(d)治疗糖尿病；(e)治疗由氧化应激引起的疾病；(f)治疗内皮功能障碍；(g)治疗由内皮功能障碍引起的疾病；(h)治疗肝硬化；(j)治疗子痫前期；(k)治疗骨质疏松症；(l)治疗肾病；(m)治疗外周血管疾病；(n)治疗门静脉高压；(o)治疗中枢神经系统疾病；(p)治疗代谢综合征；(q)治疗性功能障碍；以及(r)高脂血症。增强一氧化氮利尿化合物包括至少一种增强一氧化氮基团，通过碳、氧和/或氮等一个或多个位点与利尿化合物连接，连接通过不能水解的键或基团。
• AMIDE INHIBITORS OF RENIN
  申请人：Gant Thomas G.

  公开号：US20100124550A1

  公开（公告）日：2010-05-20

  The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof

  本发明涉及新的肾素酶抑制剂酰胺、其药物组成以及使用方法。
• [EN] NITRIC OXIDE RELEASING AMINO ACID ESTER COMPOUND, COMPOSITION AND METHOD OF USE<br/>[FR] COMPOSÉ D'ESTER D'ACIDE AMINÉ LIBÉRANT UN OXYDE NITRIQUE, COMPOSITION ET  PROCÉDÉ D'UTILISATION
  申请人：ORAL DELIVERY TECHNOLOGY LTD

  公开号：WO2010034118A1

  公开（公告）日：2010-04-01

  There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.

  提供的氨基酸酯化合物包括至少一个释放一氧化氮基团的化合物，其药学上可接受的盐和组合物。这些化合物涉及氨基酸侧链或其衍生物以及释放一氧化氮基团，如下面的结构所示：其中R1是乙基或氨基酸侧链基团或其衍生物，R2是氨基酸侧链基团或其衍生物，n是从1到10的整数。
• Nitric oxide enhancing angiotensin II antagonist compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20070032533A1

  公开（公告）日：2007-02-08

  The invention describes compositions and kits comprising at least one nitric oxide enhancing angiotensin II antagonist compound, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitric oxide enhancing angiotensin II antagonist compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (o) treating central nervous system disorders; (p) treating metabolic syndrome; and (q) treating hyperlipidemia. The nitric oxide enhancing angiotensin II antagonist compounds comprise at least one nitric oxide enhancing group linked to the angiotensin II antagonist compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

  该发明描述了包含至少一种一氧化氮增强的血管紧张素II拮抗剂化合物或其药用盐的组合物和试剂盒，以及包含至少一种一氧化氮增强的血管紧张素II拮抗剂化合物的新型组合物，还可以包含至少一种一氧化氮增强化合物和/或至少一种治疗剂。该发明还提供了用于(a)治疗心血管疾病；(b)治疗肾血管疾病；(c)治疗糖尿病；(d)治疗由氧化应激导致的疾病；(e)治疗内皮功能障碍；(f)治疗由内皮功能障碍引起的疾病；(g)治疗肝硬化；(h)治疗子痫前症；(j)治疗骨质疏松症；(k)治疗肾病；(l)治疗外周血管疾病；(m)治疗门静脉高压症；(o)治疗中枢神经系统疾病；(p)治疗代谢综合征；和(q)治疗高脂血症的方法。一氧化氮增强的血管紧张素II拮抗剂化合物包括至少一种一氧化氮增强基团，通过碳、氧和/或氮等一个或多个位点与血管紧张素II拮抗剂化合物连接，连接方式是通过一种不能水解的键或基团。