4-(8-Trifluoromethyl-quinolin-4-ylamino)-thiophene-3-carboxylic acid 2,3-dihydroxy-propyl ester | 39978-17-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-(8-Trifluoromethyl-quinolin-4-ylamino)-thiophene-3-carboxylic acid 2,3-dihydroxy-propyl ester
• 英文别名: 2,3-Dihydroxypropyl 4-[[8-(trifluoromethyl)quinolin-4-yl]amino]thiophene-3-carboxylate
• CAS: 39978-17-1
• 化学式: C₁₈H₁₅F₃N₂O₄S
• 分子量: 412.389
• InChiKey: MLSDARYKQOGGFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  120
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• Pharmaceutical preparations containing a mollusc extract
  申请人：Mc Farlane, Stuart John

  公开号：EP0010061A1

  公开（公告）日：1980-04-16

  The invention concerns novel pharmaceutical preparations containing A) an extract of the mollusc Perna canaliculus, a mussel which is found on the shores of New Zealand, and B) a pharmaceutically active substance, especially medicaments having anti-phlogistic, antipyretic and/or analgetic action, which, when taken per se, may cause as a side effect irritation of the gastro-intestinal mucosae and possibly the formation of ulcers. The addition of a mollusc extract according to A) to the said medicaments has a gastro-protective action, in that the occurence of the said side effects is prevented or diminished. The component A) is preferably used as a dry powder of the whole of the flesh of the mollusc or a dry powder obtained from the gonads thereof. In a typical preparation according to the invention an extract of the gonads is e.g. combined with acetyl-salicylic acid. The preparations may contain the 2 components in one and the same dosage unit form, e.g. a capsule or in 2 different ones, e.g. a capsule and a tablet. The invention also includes a method for preventing, alleviating or a treating gastro-intestinal irritation or ulcer formation by administering an effective amount of the mollusc extract as defined under A.

  本发明涉及一种新型药物制剂，其中含有 A）新西兰海岸发现的一种软体动物 Perna canaliculus 的提取物和 B）一种药物活性物质，特别是具有抗咽喉炎、解热和/或镇痛作用的药物。在上述药物中添加 A)软体动物提取物具有胃肠道保护作用，可以防止或减少上述副作用的发生。A)成分最好是软体动物整个肉的干粉或从其生殖腺中提取的干粉。在本发明的典型制剂中，性腺提取物与乙酰水杨酸等成分结合使用。制剂可将这两种成分以一种相同的剂量单位形式（如胶囊）或两种不同的剂量单位形式（如胶囊和片剂）包含。 本发明还包括一种预防、减轻或治疗胃肠道刺激或溃疡形成的方法，通过服用有效量的软体动物提取物如A.
• US4455298A
  申请人：——

  公开号：US4455298A

  公开（公告）日：1984-06-19
• [EN] PHARMACEUTICAL PREPARATIONS
  申请人：——

  公开号：WO1980000661A1

  公开（公告）日：1980-04-17

  (EN) Novel pharmaceutical preparations containing A) an extract of the mollusc Perna canaliculus, a mussel which is found on the shores of New Zealand, and B) a pharmaceutically active substance, especially medicaments having anti-phlogistic, anti-pyretic and/or analgetic action, which, when taken per se, may cause as a side effect imitation of the gastro-intestinal mucosae and possibly the formation of ulcers. The addition of a mollusc extract according to A) to the said medicaments has a gastro-protective action, in that the occurrence of the said side effects is prevented or diminished. The component A) is preferably used as a dry powder of the whole of the flesh of the mollusc or a dry powder obtained from the gonads thereof. In a typical preparation according to the invention an extract of the gonads is e.g. combined with acetyl-salicylic acid. The preparations may contain the 2 components in one and the same dosage unit form, e.g. a capsule or in 2 different ones, e.g. a capsule and a tablet. The invention also includes a method for preventing, alleviating or treating gastro-intestinal imitation or ulcer formation by administering an effective amount of the mollusc extract as defined under A. (FR) Nouvelles preparations pharmaceutiques contenant A) un extrait du mollusque Perna canaliculus, une moule que l"on trouve sur les cotes de Nouvelle-Zelande, et B) une substance pharmaceutique active, specialement des medicaments ayant une activite antiphlogistique, antipyretique e/ou analgesique, qui, lorsqu"ils sont pris per se, peuvent entrainer un effet secondaire d"irritation de la muqueuse gastro-intestinale et eventuellement former des ulceres, L"addition d"un extrait de mollusques selon A) auxdits medicaments presente une action gastro-protectrice, dans le sens que lesdits effets secondaires sont elimines ou diminues. Le composant A) est utilise de preference sous forme d"une poudre seche de la totalite de la chair du mollusque ou sous forme d"une poudre seche obtenue a partir de ces gonades. Dans une preparation caracteristique selon l"invention, un extrait des gonades est par exemple combine avec de l"acide acetylsalicylique. Les preparations peuvent contenir les deux composants dans une meme et unique forme d"unite de dosage, p. ex. une capsule ou en deux formes differentes, p.ex. une capsule et un comprime. Methodes preventives, calmantes ou de traitement des irritations gastro-intestinales ou de formation d"ulceres en administrant une quantite effective de l"extrait de mollusques tel qu"il est defini sous A.