1-(3,5-dimethyl-4-propionylamino)benzoyl-4-(N-methyl-2-phenylethyl)aminopiperidine | 167626-17-7

• 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: 1-(3,5-dimethyl-4-propionylamino)benzoyl-4-(N-methyl-2-phenylethyl)aminopiperidine
• 英文别名: 4-[N-Methyl-N-(2-phenylethyl)amino]-1-(3,5-dimethyl-4-propionylaminobenzoyl)piperidine；N-[2,6-dimethyl-4-[4-[methyl(2-phenylethyl)amino]piperidine-1-carbonyl]phenyl]propanamide
• CAS: 167626-17-7
• 化学式: C₂₆H₃₅N₃O₂
• 分子量: 421.583
• InChiKey: BESKMDLUOAVUJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  52.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-氨基-3-甲基苯甲酸甲酯 在 镍 sodium hydroxide 、 N-氯代丁二酰亚胺 、 氢气 、 双(2-氧代-3-恶唑烷基)次磷酰氯 、 三乙胺 作用下， 以 甲醇 、 乙醇 、 二氯甲烷 为溶剂， 反应 14.5h， 生成 1-(3,5-dimethyl-4-propionylamino)benzoyl-4-(N-methyl-2-phenylethyl)aminopiperidine
  参考文献：
  名称：

  Novel Selective Hindlimb Vasodilators:  Synthesis and Biological Activity of 1-Acyl-4-aminopiperidine Derivatives

  摘要：

  A series of 6-(4-amino-1-piperidinyl)carbonyl-2(1H)-quinolinones, and their open form derivatives, were synthesized and evaluated for their ability to stimulate femoral artery blood flow (FBF) in the canine hindlimb. All members of this series stimulated FBF, and subsequent experiments revealed that selected members of this series produced minimal changes in coronary blood flow or systemic blood pressure. Compound 25 was the most promising agent in this respect, and clinical trials are now ongoing to evaluate the effectiveness of this drug as a novel treatment for intermittent claudication and Raynaud's phenomenon.

  DOI：

  10.1021/jm020597o

文献信息

• [EN] PERIPHERAL VASODILATING AGENT CONTAINING N-ACYLATED 4-AMINO PIPERIDINE DERIVATIVES AS ACTIVE INGREDIENTS<br/>[FR] AGENTS VASODILATATEURS PERIPHERIQUES COMPORTANT COMME PRINCIPE ACTIF DES DERIVES DE LA PIPERIDINE 4-AMINO N-ACYLEE
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：WO1994022826A1

  公开（公告）日：1994-10-13

  (EN) The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity. Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by general formula (1), wherein R, R1 and R2 are the same as defined above.(FR) Nouveaux agents dilatateurs périphériques contenant individuellement comme principe actif un dérivé de la pipéridine ou l'un de ses sels pharmaco-compatibles et présentant une excellente activité vasodilatatrice périphérique. Lesdits dérivés de la pipéridine ou leurs sels pharmaco-compatibles sont représentés par la formule générale (1) où R, R1 et R2 sont conformes à la définition ci-dessus.

  (EN) 本发明涉及一种新型周围血管扩张剂，其特征在于每种扩张剂均包含作为活性成分的哌啶衍生物或其药学上可接受的盐，具有出色的周围血管扩张活性。所述哌啶衍生物或其药学上可接受的盐由通式（1）表示，其中R，R1和R2与上述定义相同。 (FR) La présente invention concerne de nouveaux agents vasodilatateurs périphériques caractérisés chacun par la présence, en tant que principe actif, d'un dérivé de pipéridine ou de l'un de ses sels pharmaceutiquement acceptables présentant une excellente activité vasodilatatrice périphérique. Lesdits dérivés de pipéridine ou leurs sels pharmaceutiquement acceptables sont représentés par la formule générale (1), dans laquelle R, R1 et R2 sont tels que définis ci-dessus.
• GEL-FORMING COMPOSITION FOR MEDICAL USE, DEVICES FOR THE APPLICATION OF THE COMPOSITION, AND DRUG RELEASE CONTROLLING CARRIER
  申请人：Next21 K.K.

  公开号：EP1985283A1

  公开（公告）日：2008-10-29

  It is an object of the present invention to provide a gel-forming composition which permits on-site administration and can form a gel exhibiting prescribed strength and sustained drug release, devices for the administration thereof, and a kit for medical use. A gel-forming composition which is composed of the first composition comprising a drug, a first gelling agent represented by the general formula (I) and the like, and the first diluent and the second composition comprising the second gelling agent represented by the general formula (I) and the like and the second diluent; and application devices and kits for medical use, which can hold the gel-forming composition. X1 - (OCH2CH2)n - X2 (I) wherein X1 and X2 are each -R1COONHS (wherein R1 is C1-7 alkylene), -COR1COONHS, -NOCOR1-R2 (wherein R2 is maleimido), -R1NH2, -R1SH, or -CO2PhNO2, and n is an integer of 80 to 1000.

  本发明的目的是提供一种允许现场给药并能形成具有规定强度和持续释药的凝胶的凝胶形成组合物、其给药装置和医疗用试剂盒。一种凝胶形成组合物，它由包含药物、通式（I）代表的第一胶凝剂和类似物以及第一稀释剂的第一组合物和包含通式（I）代表的第二胶凝剂和类似物以及第二稀释剂的第二组合物组成；以及可容纳凝胶形成组合物的施用装置和医疗用试剂盒。X1-(OCH2CH2)n-X2(I) 其中X1和X2各自为-R1COONHS(其中R1为C1-7亚烷基)、-COR1COONHS、-NOCOR1-R2(其中R2为马来酰亚胺基)、-R1NH2、-R1SH或-CO2PhNO2，且n为80至1000的整数。
• PROCESS FOR PRODUCING BONE GRAFTING MATERIAL, BONE GRAFTING MATERIAL, THREE-DIMENSIONAL SUPPORT FOR CELL CULTURE, AND SEPARATION SUPPORT FOR CHROMATOGRAPHY
  申请人：The University of Tokyo

  公开号：EP1985318A1

  公开（公告）日：2008-10-29

  A novel method for producing a bone filling material is provided. The method comprises the steps of: (a) kneading ingredient comprising calcium-based material and material comprising binder; (b) molding a predetermined shape of the mixture obtained in step (a) with an injection molding machine having a mold; (c) removing the binder contained in the mold formed in step (b) (i.e., degreasing) to obtain a degreased body; (d) and heating and sintering the degreased body obtained in step (c) to obtain a sintered body.

  提供了一种生产骨填充材料的新方法。该方法包括以下步骤(a) 揉捏包含钙基材料的配料和包含粘合剂的材料；(b) 用具有模具的注塑机将步骤(a)中获得的混合物模塑成预定形状；(c) 去除步骤(b)中形成的模具中包含的粘合剂（即脱脂），以获得脱脂体；(d) 对步骤(c)中获得的脱脂体进行加热和烧结，以获得烧结体。
• BONE MODEL, BONE FILLER AND PROCESS FOR PRODUCING BONE FILLER
  申请人：Next21 K.K.

  公开号：EP2055268A1

  公开（公告）日：2009-05-06

  A method for producing a bone filler basically comprising: a bone model producing step (step 1) for producing a bone model; a figure forming material filling step (step 2) for filling a figure forming material into a bone defect site of the bone model obtained in the bone model producing step; and a bone filler producing step (step 3) for producing a bone filler which is to be filled in a bone defect site based on the figure forming material filled in the bone defect site of the bone model in the figure forming material filling step.

  一种生产骨填充物的方法，主要包括：骨模型制作步骤（步骤 1），用于制作骨模型；人物造型材料填充步骤（步骤 2），用于将人物造型材料填充到骨模型制作步骤中获得的骨模型的骨缺损部位；以及骨填充物制作步骤（步骤 3），用于根据人物造型材料填充步骤中填充到骨模型骨缺损部位的人物造型材料，制作将填充到骨缺损部位的骨填充物。
• BONE DEFECT FILLER, RELEASE-CONTROLLED CARRIER, AND THEIR PRODUCTION METHODS
  申请人：The University of Tokyo

  公开号：EP2082754A1

  公开（公告）日：2009-07-29

  A bone filling material having controlled release of a pharmaceutical agent such as a growth factor, and a drug release controlling carrier having controlled release of a pharmaceutical agent is provided by inactivating a functional group which can strongly bind to the pharmaceutical agent of the bone filling material with a blocking agent. The bone filling material and the drug release controlling carrier of the present invention comprises: a calcium-based material such as hydroxyapatite, carbonate apatite, fluorapatite, chlorapatite, β-TCP, and α-TCP; a blocking agent of the calcium-based material such as serine and dextran; and a pharmaceutical agent.

  本发明通过使用阻断剂使能与骨填充材料的药剂强结合的官能团失活，提供了一种可控制药剂（如生长因子）释放的骨填充材料和一种可控制药剂释放的药物释放控制载体。本发明的骨填充材料和药物释放控制载体包括：羟基磷灰石、碳酸盐磷灰石、氟磷灰石、氯磷灰石、β-TCP 和 α-TCP 等钙基材料；丝氨酸和葡聚糖等钙基材料的阻断剂；以及药剂。