2,4-Bis-benzo[1,3]dioxol-5-yl-1,1-dioxo-1,2-dihydro-1λ6-benzo[e][1,2]thiazine-3-carboxylic acid | 182163-51-5

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: 2,4-Bis-benzo[1,3]dioxol-5-yl-1,1-dioxo-1,2-dihydro-1λ6-benzo[e][1,2]thiazine-3-carboxylic acid
• 英文别名: 2,4-Bis(1,3-benzodioxol-5-yl)-1,1-dioxo-1lambda6,2-benzothiazine-3-carboxylic acid；2,4-bis(1,3-benzodioxol-5-yl)-1,1-dioxo-1λ6,2-benzothiazine-3-carboxylic acid
• CAS: 182163-51-5
• 化学式: C₂₃H₁₅NO₈S
• 分子量: 465.44
• InChiKey: BATPIGLNLCBBQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  33
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  120
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• [EN] BENZOTHIAZINE DIOXIDES AS ENDOTHELIN ANTAGONISTS<br/>[FR] DIOXYDES DE BENZOTHIAZINE UTILISES COMME ANTAGONISTES DE L'ENDOTHELINE
  申请人：WARNER-LAMBERT COMPANY

  公开号：WO1996026195A1

  公开（公告）日：1996-08-29

  (EN) Novel benzothiazine dioxides which are antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation, and pharmaceutical compositions of the same, which are useful in treating elevated levels of endohelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.(FR) La présente invention concerne de nouveaux dioxydes de benzothiazine qui sont des antagonistes de l'endothéline, ainsi que de nouveaux intermédiaires utilisés pour leur préparation, des procédés de préparation et des compositions pharmaceutiques à base de ces nouveaux dioxydes de benzothiazine. Ces nouveaux dioxydes de benzothiazine sont utiles dans le traitement des niveaux élevés d'endothéline, de l'hypertension artérielle rénovasculaire et pulmonaire essentielle maligne, de l'infarctus cérébral, de l'insuffisance cardiaque congestive et de l'hémorragie sous-arachnoïdienne.

  描述了一种新的苯并噻唑二氧化物，它们是内皮素拮抗剂，以及用于它们的制备的新中间体，制备方法和相应的药物组成物，这些药物组成物在治疗内皮素水平升高、重要肾血管恶性和肺动脉高压、脑梗死、脑缺血、充血性心力衰竭和蛛网膜下腔出血方面有用。
• Herbicidal compositions
  申请人：MAKHTESHIM CHEMICAL WORKS LIMITED

  公开号：EP0254049A2

  公开（公告）日：1988-01-27

  Herbicidal compositions containing a compound of the formula: wherein R is hydrogen, a lower alkyl, lower alkoxy, amino, substituted amino, cycloalkyl, halogen, or nitro; Rʹ is selected from the group consisting of a haloalkylthio group containing l or 2 carbon atoms and at least two halogen sub­stituents; linear or branched alkyl and alkenyl group having from 2 to l0 carbon atoms, optionally substituted by halogen, hydroxy, lower alkoxy or haloalkyl; and cycloalkyl of 5 to l0 carbon atoms, optionally substituted by halogen, hydroxy, lower alkoxy, or haloalkyl; provided that at least one of Rʹ is a haloalkylthio group as defined; n is zero or an integer from l to 4; and X is oxygen or sulfur

  含有式化合物的除草组合物 其中R是氢、低级烷基、低级烷氧基、氨基、取代氨基、环烷基、卤素或硝基；Rʹ选自由含l或2个碳原子和至少两个卤素取代基的卤代硫代烷基；2至l0个碳原子的直链或支链烷基和烯基，可选择被卤素、羟基、低级烷氧基或卤代烷基取代；以及5至l0个碳原子的环烷基，可选择被卤素、羟基、低级烷氧基或卤代烷基取代；条件是Rʹ中至少有一个是所定义的卤代硫代烷基；n是零或l至4的整数；以及X是氧或硫。
• Combinations of an endothelin receptor antagonist and an antiepileptic compound having pain alleviating properties or analgesic
  申请人：——

  公开号：US20030232787A1

  公开（公告）日：2003-12-18

  The present invention is a novel combination effective for alleviating pain comprising a pain alleviating effective amount of an endothelin receptor antagonist or a pharmaceutically acceptable salt thereof and from 1 to 3 compounds independently selected from the group consisting of antiepileptic compounds having pain alleviating properties and analgesics, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising same. The administration of endothelin receptor antagonists in these novel combinations results in an improved reduction in the frequency and severity of pain. The incidence of unwanted side effects can be reduced by these novel combinations in comparison to using higher doses of a single agent treatment to achieve a similar therapeutic effect. The present invention is also directed to methods of using effective amounts of the novel combinations and pharmaceutical compositions thereof to treat pain in mammals, including a human.

  本发明是一种有效缓解疼痛的新型复方制剂，它包含缓解疼痛有效量的内皮素受体拮抗剂或其药学上可接受的盐，以及1至3种独立选自具有缓解疼痛特性的抗癫痫化合物和镇痛剂及其药学上可接受的盐组成的化合物，以及包含这些化合物的药物组合物。在这些新型组合物中施用内皮素受体拮抗剂，可有效降低疼痛的频率和严重程度。与使用较大剂量的单药治疗以达到类似的治疗效果相比，这些新型组合物可以降低不希望出现的副作用的发生率。本发明还涉及使用有效量的新型组合物及其药物组合物治疗哺乳动物（包括人类）疼痛的方法。
• Pesticidal 1-(2-pyridyl)pyrazoles
  申请人：RHONE-POULENC AGROCHIMIE

  公开号：EP0500209B1

  公开（公告）日：1997-09-17
• BENZOTHIAZINE DIOXIDES AS ENDOTHELIN ANTAGONISTS
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0811001A1

  公开（公告）日：1997-12-10