3-哌啶-1-基喹唑啉-4-酮 | 89804-94-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 3-哌啶-1-基喹唑啉-4-酮
• 英文名称: 3-(Piperidin-1-yl)quinazolin-4(3H)-one
• 英文别名: 3-piperidin-1-ylquinazolin-4-one
• CAS: 89804-94-4
• 化学式: C₁₃H₁₅N₃O
• 分子量: 229.282
• InChiKey: ZTEHZCFAKPLXIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  35.9
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-氨基哌啶 、 alkaline earth salt of/the/ methylsulfuric acid 在 三乙胺 作用下， 以 吡啶 为溶剂， 反应 17.0h， 生成 3-哌啶-1-基喹唑啉-4-酮
  参考文献：
  名称：

  3-氨基-4（3 H）-喹唑啉酮类化合物的合成及其抗惊厥活性

  摘要：

  由邻氨基苯甲酰肼和原甲酸三乙酯或由等角酸酐，肼和原甲酸三乙酯制备了几种3-氨基-4（3 H）-喹唑啉酮。邻氨基苯甲酰肼中间体是通过使等角酸酐与肼反应而获得的。一些氨基喹唑啉酮在小鼠中表现出抗惊厥活性。

  DOI：

  10.1002/jhet.5570200623

文献信息

• Antisense modulation of microsomal triglyceride transfer protein expression
  申请人：——

  公开号：US20030086912A1

  公开（公告）日：2003-05-08

  Antisense compounds, compositions and methods are provided for modulating the expression of microsomal triglyceride transfer protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding microsomal triglyceride transfer protein. Methods of using these compounds for modulation of microsomal triglyceride transfer protein expression and for treatment of diseases associated with expression of microsomal triglyceride transfer protein are provided.

  提供了用于调节微粒体甘油三酯转移蛋白表达的反义化合物、组合物和方法。这些组合物包括针对编码微粒体甘油三酯转移蛋白的核酸的反义化合物，特别是反义寡核苷酸。提供了利用这些化合物调节微粒体甘油三酯转移蛋白表达和治疗与微粒体甘油三酯转移蛋白表达相关的疾病的方法。
• 3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
  申请人：Japan Tobacco Inc.

  公开号：EP0970954A1

  公开（公告）日：2000-01-12

  3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 4, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.

  提供了3-哌啶基-4-氧代喹唑啉衍生物，由式(I)表示： 其中 R 代表氨基或环状氨基，如二苯并氮杂卓，它们各自被取代或未被取代的芳基、取代或未被取代的杂芳基或类似基团取代，n 是 1 至 4 的整数，R3 和 R4 独立地代表氢原子、低级烷基或类似基团，或其药学上可接受的盐。本发明的化合物（I）具有优异的 MTP 抑制活性。因此，这些化合物不仅能抑制导致动脉硬化疾病的低密度脂蛋白的形成，还能调节血液中的总胆固醇、胆固醇和脂蛋白（如低密度脂蛋白），并通过调节 MTP 活性来调节细胞脂质。它们还可用作高脂血症或动脉硬化疾病的新型预防或治疗药物。此外，它们还可用作胰腺炎、肥胖症、高胆固醇血症和高甘油三酯血症的治疗或预防药物。
• 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。
• Solid formulation with improved solubility and stability, and method for producing said formulation
  申请人：Yamane Shogo

  公开号：US20060153913A1

  公开（公告）日：2006-07-13

  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一起形成固体分散体；(2) 形成固体分散体的水溶性高分子物质呈细小颗粒状；(3) 保持细小颗粒状的水溶性高分子物质吸附在和/或粘附在无机多孔物质表面。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。
• [EN] 3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME<br/>[FR] DERIVES DU 3-PIPERIDYL-4-OXOQUINAZOLINE ET COMPOSITIONS MEDICINALES LES CONTENANT
  申请人：JAPAN TOBACCO INC.

  公开号：WO1999031085A1

  公开（公告）日：1999-06-24

  (EN) 3-Piperidyl-4-oxoquinazoline derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein R represents amino substituted by optionally substituted aryl or optionally substituted heteroaryl, or cyclic amino such as dibenzazepine; n is an integer selected among 1 to 4; and R3 and R4 represent each hydrogen, lower alkyl, etc. Because of having an excellent MTP-inhibitory activity, these compounds (I) are expected as usable in inhibiting the formation of LDL causative of arteriosclerotic diseases and enabling the regulation of TG, cholesterol and lipoproteins such as LDL in the blood and cellular lipids via the regulation of the MTP activity. Owing to these effects, the above compounds are expected also as a novel type of remedies or preventives for hyper-lipemia or arteriosclerotic diseases and, moreover, as remedies or preventives for pancreatitis, obesity, hypercholesterolemia, hypertriglyceridemia, etc.(FR) L'invention concerne des dérivés de 3-pipéridyl-4-oxoquinazoline, pharmaceutiquement acceptables, représentés par la formule générale suivante (I), ou des sels de ceux-ci. Dans cette formule R représente un amino substitué par un aryle éventuellement substitué ou par un hétéroaryle éventuellement substitué, ou un amino cyclique comme une dibenzazepine; n est un entier allant de 1 à 4; R3 et R4 représentent chacun un hydrogène, un alkyle inférieur, etc. En raison de leur excellente activité comme inhibiteur de MTP, ces composés (I) peuvent s'utiliser pour l'inhibition de la formation de LDL responsables de maladies artérioscléreuses et permettre la régulation des TG, du cholestérol et des lipoprotéines comme les LDL dans le sans et les lipides cellulaires par la régulation de l'activité MTP. En raison de ces effets, les composés ci-dessus peuvent être considérés comme un nouveau type de remèdes ou d'agents prophylactiques pour les hyperlipémies ou les maladies artérioscléreuses et, de plus, comme remèdes ou agents prophylactiques pour les pancréatites, l'obésité, l'hyperchlolestérolémie, l'hypertriglycéridémie, etc.

  3-吡啶酰胺-4-氧quinazoline衍生物，代表一般式(I)或药学上可接受的其盐，其中R代表氨基酸，其氢或氨基上选自取代或未取代的算叶基或未取代或取代的算子基，或像二苯甲zipine环状的氨基；n是选取1到4之间的整数；R3和R4各自代表氢、低级烷基等。由于对MTP抑制活性的优异性能，这些化合物(I)也可期待用于防止LDL由动脉硬化的疾病导致，同时调节甘油三酯、胆固醇及脂蛋白等如LDL在血液和细胞内的脂质，通过调节MTP活性而发挥作用。由于这些效应显而易见，上述化合物也被期待作为一种新型类药物或预防药物用于高脂血症或动脉硬化的防治，而且也可以用作防治胰腺炎、肥胖、高胆固醇血症、高三角lycerid血症等疾病。