CP 346086

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: CP 346086
• 英文别名: 4'-trifluoromethyl-biphenyl-2-carboxylic acid [2-(1H-[1,2,4]triazol-3-ylmethyl)-1,2,3,4-tetrahydro-isoquinolin-6-yl]-amide；N-[2-(1H-1,2,4-triazol-5-ylmethyl)-3,4-dihydro-1H-isoquinolin-6-yl]-2-[4-(trifluoromethyl)phenyl]benzamide
• 化学式: C₂₆H₂₂F₃N₅O
• 分子量: 477.489
• InChiKey: WNDIAFXQKOHFLV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  35
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  73.9
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4'-trifluoromethylbiphenyl-2-carbonyl chloride 、 6-amino-2-<2H-<1,2,4>triazol-3-ylmethyl>-1,2,3,4-tetrahydro-isoquinoline 在 4'-trifluoromethylbiphenyl-2-carbonyl chloride 作用下， 生成 CP 346086
  参考文献：
  名称：

  Process and intermediates for preparing

  摘要：

  公开了一种制备式（1）化合物的方法。 ##STR1## 起始物质是N-三唑基甲基-6-氨基异喹啉和4-联苯-2-羧酸衍生物。

  公开号：

  US05998623A1

文献信息

• Combination of MTP inhibitors or apoB-secretion inhibitors with fibrates for use as pharmaceuticals
  申请人：Boehringer Ingelheim Pharma KG

  公开号：US20030162788A1

  公开（公告）日：2003-08-28

  The invention relates to the use of fibrates for lowering the liver toxicity of MTP inhibitors as well as pharmaceutical compositions containing an MTP inhibitor and a fibrate.

  本发明涉及使用纤维酸衍生物来降低MTP抑制剂对肝脏的毒性，以及包含MTP抑制剂和纤维酸衍生物的药物组合物。
• ELEVATION OF THE PLASMA HDL-CHOLESTEROL LEVEL
  申请人：Hermansen Kjeld

  公开号：US20110038827A1

  公开（公告）日：2011-02-17

  The present invention relates to the use of isosteviol, steviol, and related compounds for elevating the plasma HDL-cholesterol level. The invention furthermore relates to the use of these compounds for reducing the body weight of a subject and/or lowering the plasma triglyceride level of a subject, including a concomitant elevation of the plasma HDL-cholesterol level. Preferably the compounds used are isosteviol and/or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. The compounds may furthermore be administered in combination with one or more further active compounds, such as e.g. LDL-cholesterol lowering agents. The invention furthermore relates to a method for elevating the plasma HDL-cholesterol level in a subject by administering to a subject in need of such treatment a plasma HDL-cholesterol level elevating amount of the compounds, described herein.

  本发明涉及使用异甘草酸甙、甘草酸甙和相关化合物来提高血浆高密度脂蛋白胆固醇水平。此外，本发明还涉及使用这些化合物来减轻受试者的体重和/或降低受试者的血浆甘油三酯水平，包括同时提高血浆高密度脂蛋白胆固醇水平。优选使用的化合物是异甘草酸甙和/或甘草酸甙，或其药学上可接受的盐、溶剂合物或前药。这些化合物还可以与一个或多个其他活性化合物联合给药，例如降低低密度脂蛋白胆固醇的药物。此外，本发明还涉及一种通过向需要此类治疗的受试者给予所述化合物的血浆高密度脂蛋白胆固醇水平升高量的方法，以提高受试者的血浆高密度脂蛋白胆固醇水平。
• Substituted quinoline compounds
  申请人：Bertinato Peter

  公开号：US20050234099A1

  公开（公告）日：2005-10-20

  This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R 1 -R 7 , X 1 , m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

  本发明涉及公式（I）中的MTP / Apo-B分泌抑制剂，其中R1-R7，X1，m和n如规范中所定义，以及包含该化合物的制药组合物，以及该化合物和组合物的使用方法。本发明的化合物在治疗肥胖和相关疾病，状况或障碍方面是有用的。
• 4-Amino Substituted-2-Substituted-1,2,3,4-tetrahydroquinoline Compounds
  申请人：Ruggeri B. Roger

  公开号：US20060247272A1

  公开（公告）日：2006-11-02

  4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  4-氨基取代的2-取代的1,2,3,4-四氢喹啉化合物，含有此类化合物的制药组合物以及使用此类化合物以提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低某些其他血浆脂质水平，如低密度脂蛋白胆固醇和三酰甘油，因此治疗由低水平的高密度脂蛋白胆固醇和/或高水平的低密度脂蛋白胆固醇和三酰甘油加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物中，包括人类。
• SOLID MEDICINAL PREPARATION IMPROVED IN SOLUBILITY AND STABILITY AND PROCESS FOR PRODUCING THE SAME
  申请人：Japan Tobacco, Inc.

  公开号：EP1806149A1

  公开（公告）日：2007-07-11

  The present invention relates to a solid formulation with improved solubility and maintained stability including a chemical substance poorly soluble in water as a pharmaceutically active ingredient formulated in an improved manner. More specifically, the present invention relates to a solid formulation having improved water-solubility which comprises a chemical substance poorly soluble in water as a pharmaceutically active ingredient, a water-soluble polymer substance and an inorganic porous substance, characterized in that (1) the chemical substance poorly soluble in water forms a solid dispersion together with the water-soluble polymer substance, (2) the water-soluble polymer substance forming the solid dispersion is in the form of fine pieces, and (3) the water-soluble polymer substance is in the form of fine pieces is maintained to be adsorbed on and/or adhered to the surface of the inorganic porous substance. The solid formulation can be produced by stirring and mixing a solution obtained by dissolving a chemical substance poorly soluble in water as a pharmaceutically active ingredient and a water-soluble polymer substance in an organic solvent with an inorganic porous substance and then granulating and drying the mixture.

  本发明涉及一种固体制剂，它具有更好的溶解性和稳定性，包括以改进方式配制的一种难溶于水的化学物质作为药物活性成分。 更具体地说，本发明涉及一种具有更好水溶性的固体制剂，它包括一种作为药物活性成分的难溶于水的化学物质、一种水溶性聚合物物质和一种无机多孔物质，其特征在于 (1) 难溶于水的化学物质与水溶性高分子物质形成固体分散体、 (2) 形成固体分散体的水溶性高分子物质呈细小块状，以及 (3) 细粒形式的水溶性高分子物质被吸附和/或附着在无机多孔物质的表面。 固体制剂可通过将溶于水的化学物质（作为药物活性成分）和水溶性高分子物质溶解在有机溶剂中得到的溶液与无机多孔物质搅拌混合，然后将混合物造粒和干燥而制成。