尼克噻嗪 | 95058-70-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并硫氮卓类
• 中文名称: 尼克噻嗪
• 英文名称: Nictiazem
• 英文别名: [(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] pyridine-3-carboxylate
• CAS: 95058-70-1
• 化学式: C₂₆H₂₇N₃O₄S
• 分子量: 477.6
• InChiKey: DSYNMAGEJOOLTQ-RPWUZVMVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  97.3
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  去乙酰地尔硫卓 、 烟酰氯 生成 尼克噻嗪
  参考文献：
  名称：

  MAIORANA, S.;BROCCHETTI, D. G.;PIACENZA, G.;MANFREDI, A.

  摘要：

  DOI：

文献信息

• [EN] TOPICAL OPHTHALMIC COMPOSITIONS COMPRISING A COMBINATION OF CALCIUM ANTAGONISTS WITH KNOWN ANTIGLAUCOMA AGENTS<br/>[FR] COMPOSITIONS OPHTALMIQUES A USAGE LOCAL CONTENANT UNE COMBINAISON D'ANTAGONISTES DU CALCIUM ET D'AGENTS ANTIGLAUCOME
  申请人：ALCON LABORATORIES, INC.

  公开号：WO1993023082A1

  公开（公告）日：1993-11-25

  (EN) Calcium antagonists and compounds which lower intraocular pressure are combined in ophthalmic compositions to treat glaucoma. The calcium antagonists prevent or reduce the loss of visual field, while the intraocular pressure-lowering compounds maintain the intraocular pressure at normal levels.(FR) L'invention concerne des antagonistes du calcium et des composés abaissant la pression intraoculaire combinés dans des compositions ophtalmiques afin de traiter le glaucome. Les antagonistes du calcium empêchent au minimum la perte de champ visuel et les composés abaissant la pression intraoculaire maintiennent la pression intraoculaire à des niveaux normaux.

  （中文翻译）钙拮抗剂和降低眼内压的化合物被组合在眼科制剂中用于治疗青光眼。钙拮抗剂可以预防或减少视野损失，而降低眼内压的化合物可以维持眼内压在正常水平。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• 1,5-Benzothiazepines with cardiovascular utility, and pharmaceutical
  申请人：Schiapparelli Farmaceutici S.p.A.

  公开号：US04547495A1

  公开（公告）日：1985-10-15

  New 1,5-benzothiazepines of the following general formula ##STR1## wherein: R.sub.1 represents (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or a halogen atom; R.sub.2 is selected from: benzoyl independently substituted with 1 to 3 (C.sub.1-4)alkyl or (C.sub.1-4)alkoxy groups, or with halogen atoms; phenylcarbamoyl; phenylcarbamoyl independently substituted with 1 to 3 (C.sub.1-4) alkyl or (C.sub.1-4) alkoxy groups or with halogen atoms; the groups R.sub.5 -CO, in which R.sub.5 is the radical deriving from a heterocyclic ring optionally substituted by a (C.sub.1-4)alkyl or a (C.sub.1-4)alkoxy radical, or by a halogen atom; R.sub.3 and R.sub.4 independently represent (C.sub.1-4)alkyl groups; and salts therewith of pharmaceutically acceptable acids. The compounds of the invention possess cardiovascular utility.

  以下是通式为 ##STR1## 的新型1,5-苯并噻吩化合物，其中：R.sub.1代表(C.sub.1-4)烷基，(C.sub.1-4)烷氧基或卤素原子；R.sub.2选自：独立取代1至3个(C.sub.1-4)烷基或(C.sub.1-4)烷氧基，或卤素原子的苯甲酰基；苯基氨甲酰基；独立取代1至3个(C.sub.1-4)烷基或(C.sub.1-4)烷氧基，或卤素原子的苯基氨甲酰基；R.sub.5-CO基团，其中R.sub.5是从杂环环取代或未取代(C.sub.1-4)烷基或(C.sub.1-4)烷氧基基团，或卤素原子导出的基团；R.sub.3和R.sub.4独立表示(C.sub.1-4)烷基基团；以及与药学上可接受的酸形成的盐。该发明的化合物具有心血管效用。
• Use of an antidiarrheal for the manufacture of a medicament for the treatment of inflammatory conditions
  申请人：Adolor Corporation

  公开号：EP0937460A2

  公开（公告）日：1999-08-25

  The present invention provides the use of an antidiarrheal for the manufacture of a medicament for the treatment of a pathological condition mediated by TNF production in a mammal, wherein the pathologic condition is an inflammatory one.

  本发明提供了一种止泻药，用于制造治疗哺乳动物体内由 TNF 产生介导的病理状况的药物，其中的病理状况是一种炎症。
• PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS
  申请人：President and Fellows of Harvard College

  公开号：EP3485881A1

  公开（公告）日：2019-05-22

  The present invention relates to a composition, optionally a pharmaceutical composition, comprising cysteine-derived compounds as defined in Formula (XII). The compound may be used in a method for treating neurogenic inflammation in a human patient.

  本发明涉及一种组合物，也可以是一种药物组合物，其中包含如式（XII）所定义的半胱氨酸衍生化合物。该化合物可用于治疗人类患者神经源性炎症的方法中。