5-(2-chloro-α-cyclopropylcarbonylbenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 英文名称: 5-(2-chloro-α-cyclopropylcarbonylbenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
• 英文别名: 5-(α-cyclopropylcarbonyl-2-chlorobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin；2-(2-chlorophenyl)-1-cyclopropyl-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)ethanone
• 化学式: C₁₈H₁₈ClNOS
• 分子量: 331.866
• InChiKey: HHESGXNOEGCXBR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  48.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• MEDICINAL COMPOSITION
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1319399A1

  公开（公告）日：2003-06-18

  A pharmaceutical composition containing a drug (A), a waxy substance (B), and synthetic aluminum silicate and/or hydrous silicon dioxide (C). The invention provides a granular pharmaceutical composition suitable for providing a pharmaceutical characterized in that adhesion of granules thereof onto a granulation apparatus during granulation is minimized and caking of the granules is suppressed.

  一种药物组合物，包含药物（A）、蜡状物质（B）和合成氧化铝硅和/或水合二氧化硅（C）。该发明提供了一种颗粒状药物组合物，适用于提供一种药物，其特点在于在制粒过程中减少颗粒粘附到制粒设备上，并抑制颗粒结块。
• Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof and their preparation and uses for inhibiting blood platelet aggregation
  申请人：Sankyo Company Limited

  公开号：EP0542411A2

  公开（公告）日：1993-05-19

  Compounds of formula (I): in which: R¹ is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulphonyl, haloalkanesulphonyl or sulphamoyl; R² is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R³ is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is -NH- or oxygen or sulphur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.

  式(I)化合物： 其中R¹ 是氢、烷基、卤素、卤代烷基、羟基、烷氧基、卤代烷氧基、烷硫基、卤代烷硫基、氨基、烷酰基、卤代烷酰基、羧基、烷氧羰基、氨基甲酰基、氰基、硝基、烷磺酰基、卤代烷磺酰基或磺酰基；R² 是任选取代的烷酰基、任选取代的烯酰基、任选取代的环烷基羰基、取代的苯甲酰基或 5,6-二氢-1,4,2-二恶嗪-3-基；R³ 是氢、羟基、任选取代的烷氧基、烷氧基、烷甲氧基、烯甲氧基、环烷基羰基氧基、芳基羰基氧基、烷氧基羰基氧基、烷氧基羰基氧基、酞酰氧基、(5-甲基-2-氧代-1,3-二氧戊烯-4-基)甲氧基、(5-苯基-2-氧代-1,3-二氧戊烯-4-基)甲氧基、任选取代的氨基或硝基；Y 是-NH-或氧或硫；n 是 1 至 5；所述式（I）化合物的同系物和盐具有抑制血小板聚集的能力，因此可用于血栓和栓塞的治疗和预防。
• MEDICINAL COMPOSITIONS
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1161956A1

  公开（公告）日：2001-12-12

  The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.

  本发明涉及一种颗粒状药物组合物，该组合物由具有异味的药物、蜡和糖醇组成；一种制备该组合物的方法；以及一种包含该颗粒状组合物的口服药物。该产品能很好地掩盖药物的异味，并在口服时提供良好的感觉，因此即使是老人、儿童和吞咽困难患者也很容易摄入。此外，该产品还适合使用软管给药。
• Tastemasked pharmaceutical compositions
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP2275141A1

  公开（公告）日：2011-01-19

  A granular pharmaceutical composition, comprising (A) a drug having disagreeable taste; (B) one or more of waxy substances selected from the group consisting of hydrogenated castor oil, hydrogenated soybean oil, hydrogenated rape seed oil, hydrogenated cotton seed oil, camauba wax, white bees wax, beef tallow, stearyl alcohol, cetanol, polyethylene glycol, stearic acid, parmitic acid, mono-fatty acid glycerin ester, tri-fatty acid glycerin ester and fatty acid sucrose ester; and (C) erythritol, characterized in that the composition thereof does not cohere in water and has a dosage form of a granule, powder or capsule.

  一种颗粒状药物组合物，包括 (A) 有异味的药物；(B) 一种或多种蜡质物质，选自氢化蓖麻油、氢化大豆油、氢化菜籽油、氢化棉籽油、卡玛巴蜡、白蜂蜡、牛脂、硬脂醇、鲸蜡醇、聚乙二醇、硬脂酸、帕米特酸、单脂肪酸甘油酯、三脂肪酸甘油酯和脂肪酸蔗糖酯组成的组；(C) 赤藓糖醇，其特点是其成分在水中不凝聚，剂型为颗粒、粉末或胶囊。
• Medicinal composition
  申请人：——

  公开号：US20040022848A1

  公开（公告）日：2004-02-05

  A pharmaceutical composition containing a drug (A), a waxy substance (B), and synthetic aluminum silicate and/or hydrous silicon dioxide (C). The invention provides a granular pharmaceutical composition suitable for providing a pharmaceutical characterized in that adhesion of granules thereof onto a granulation apparatus during granulation is minimized and caking of the granules is suppressed.

  一种含有药物（A）、蜡状物质（B）和合成硅酸铝和/或水合二氧化硅（C）的药物组合物。本发明提供了一种适用于提供药物的颗粒状药物组合物，其特点是在制粒过程中将颗粒在制粒设备上的附着减至最小，并抑制颗粒的结块。