吡卡他胺 | 76732-75-7

• 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
• 中文名称: 吡卡他胺
• 中文别名: 吡硫酰胺
• 英文名称: N-methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide
• 英文别名: N-methyl-2-(pyrid-2-yl)tetrahydrothiophene-2-carbothioamide；picartamide；N-methyl-2-pyridin-2-ylthiolane-2-carbothioamide
• CAS: 76732-75-7
• 化学式: C₁₁H₁₄N₂S₂
• 分子量: 238.378
• InChiKey: ITNLONMDUMHEOK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  82.3
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090

反应信息

• 作为产物：
  描述：

  2-(四氢-2-噻吩基)吡啶 在 正丁基锂 作用下， 以 乙醇 为溶剂， 反应 0.5h， 生成 吡卡他胺
  参考文献：
  名称：

  Synthesis and antisecretory and antiulcer activities of derivatives and analogs of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide

  摘要：

  New thioamide derivatives of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (29) and related compounds (in which the tetrahydrothiophene ring was replaced by tetrahydrothiopyran, tetrahydrofuran, 1,3-dithiane, or 1,3-oxathiane and where the pyridine ring was replaced by other nitrogen heterocycles) were synthesized and tested for their antisecretory and antiulcer activities. These thioamides were prepared according to one of the following methods: reaction of an isothiocyanate with the carbanion of the corresponding cyclic precursor (for secondary thioamides); reaction of ammonia or an amine with the dithio ester prepared from the same precursor (for primary, secondary, and tertiary thioamides). These thioamides were evaluated by the Shay method to measure their antisecretory activity and by the stress-induced-ulcer method to test their antiulcer activity. Structure-activity relationships are discussed. N-Methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (R.P. 40749, 30) exhibited activities that were at least 10 times higher than those reported for cimetidine.

  DOI：

  10.1021/jm00384a004

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• 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。
• 2-(Pyrid-2-yl)tetrahydrothiophene derivatives
  申请人：Rhone-Poulenc Industries

  公开号：US04272534A1

  公开（公告）日：1981-06-09

  Compounds of the formula: ##STR1## wherein R represents hydrogen or alkyl of 1 through 4 carbon atoms, and R.sub.1 and R.sub.2 represent hydrogen or alkyl of 1 through 15 carbon atoms, or alkyl of 1 through 15 carbon atoms substituted by one substituent selected from (i) hydroxy, (ii) alkylamino in which the alkyl radical is of 1 through 4 carbon atoms, (iii) dialkylamino in which the alkyl radicals are of 1 through 4 carbon atoms, (iv) phenyl, (v) carboxy, and (vi) alkoxycarbonyl in which the alkoxy radical is of 1 through 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached represent a five- or six-membered heterocyclic radical, are new compounds. They possess pharmacological properties and are particularly useful in the treatment of gastro-intestinal ulcers.

  式为：##STR1## 其中R代表氢或1到4个碳原子的烷基，R.sub.1和R.sub.2代表氢或1到15个碳原子的烷基，或者1到15个碳原子的烷基被以下一种取代的基团所取代：(i)羟基，(ii)烷基胺，其中烷基基团为1到4个碳原子，(iii)二烷基胺，其中烷基基团为1到4个碳原子，(iv)苯基，(v)羧基，以及(vi)醇酸酯基，其中醇酸酯基团为1到4个碳原子的新化合物。它们具有药理学特性，特别适用于治疗胃肠溃疡。R.sub.1和R.sub.2连同它们所附着的氮原子可以代表一个五元或六元杂环基团。
• KIT, DEVICE AND METHOD FOR DETECTING PROSTATE CANCER
  申请人：Toray Industries, Inc.

  公开号：EP3835434A1

  公开（公告）日：2021-06-16

  This invention provides a kit or device for detection of prostate cancer and a method for detecting prostate cancer. This invention provides a kit or device for detection of prostate cancer comprising a nucleic acid capable of specifically binding to an miRNA in a sample from a subject or a complementary strand thereof and a method for detecting prostate cancer comprising measuring the miRNA in vitro.

  本发明提供了一种检测前列腺癌的试剂盒或装置以及一种检测前列腺癌的方法。本发明提供了一种用于检测前列腺癌的试剂盒或装置，该试剂盒或装置包括一种能与受试者样本中的 miRNA 或其互补链特异性结合的核酸，以及一种检测前列腺癌的方法，该方法包括体外测量 miRNA。
• KIT, DEVICE, AND METHOD FOR DETECTING UTERINE LEIOMYOSARCOMA
  申请人：Toray Industries, Inc.

  公开号：EP3936614A1

  公开（公告）日：2022-01-12

  This invention provides a kit and device for detection of uterine leiomyosarcoma, and a method for detecting uterine leiomyosarcoma. This invention provides a kit and device for detection of uterine leiomyosarcoma containing a nucleic acid capable of specifically binding to a miRNA in a sample from a subject or a complementary strand thereof and a method for detecting uterine leiomyosarcoma including measuring the miRNA in vitro.

  本发明提供了一种检测子宫细肌瘤的试剂盒和装置，以及一种检测子宫细肌瘤的方法。本发明提供了一种检测子宫细肌瘤的试剂盒和装置，其中含有一种能与受试者样本中的 miRNA 或其互补链特异性结合的核酸，以及一种检测子宫细肌瘤的方法，包括体外测量 miRNA。