1-acetylpiperidine-3-carbaldehyde | 1082481-93-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-acetylpiperidine-3-carbaldehyde
• CAS: 1082481-93-3
• 化学式: C₈H₁₃NO₂
• mdl: MFCD11044202
• 分子量: 155.197
• InChiKey: SYUMWXVBQIRTKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-acetylpiperidine-3-carbaldehyde 在 溶剂黄146 作用下， 以 甲醇 为溶剂， 反应 20.0h， 生成
  参考文献：
  名称：

  Hit-to-Lead Studies for the Antimalarial Tetrahydroisoquinolone Carboxanilides

  摘要：

  Phenotypic whole-cell screening in erythrocytic cocultures of Plasmodium falciparum identified a series of dihydroisoquinolones that possessed potent antimalarial activity against multiple resistant strains of P. falciparum in vitro and show no cytotoxicity to mammalian cells. Systematic structure activity studies revealed relationships between potency and modifications at N-2, C-3, and C-4. Careful structure property relationship studies, coupled with studies of metabolism, addressed the poor aqueous solubility and metabolic vulnerability, as well as potential toxicological effects, inherent in the more potent primary screening hits such as 10b. Analogues 13h and 13i, with structural modifications at each site, were shown to possess excellent antimalarial activity in vivo. The (+)-(35,4S) enantiomer of 13i and similar analogues were identified as the more potent. On the basis of these studies, we have selected (+)-13i for further study as a preclinical candidate.

  DOI：

  10.1021/acs.jmedchem.6b00752

文献信息

• Piperidine derivative and use thereof
  申请人：Shirai Junya

  公开号：US20080275085A1

  公开（公告）日：2008-11-06

  The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula: wherein R 1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R 2 is methyl or cyclopropyl; R 3 is a hydrogen atom or methyl; R 4 is a chlorine atom or trifluoromethyl; R 5 is a chlorine atom or trifluoromethyl; and a group represented by the formula: is a group represented by the formula: wherein R 6 is a hydrogen atom, methyl, ethyl or isopropyl; R 7 is a hydrogen atom, methyl or a chlorine atom; and R 8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.

  本发明提供了一种新颖的哌啶衍生物和含有该衍生物的催吐肽受体拮抗剂，以及由下式表示的化合物： 其中R1为羰胺甲基、甲磺酰乙基羰基等；R2为甲基或环丙基；R3为氢原子或甲基；R4为氯原子或三氟甲基；R5为氯原子或三氟甲基；以及由下式表示的基团： 是由下式表示的基团： 其中R6为氢原子、甲基、乙基或异丙基；R7为氢原子、甲基或氯原子；R8为氢原子、氟原子、氯原子或甲基；或3-甲基噻吩-2-基，并且其盐。
• COMPOSITIONS IN THE FORM OF AN INJECTABLE AQUEOUS SOLUTION COMPRISING AMYLIN, AN AMYLIN RECEPTOR AGONIST OR AN AMYLIN ANALOGUE AND A CO-POLYAMINO ACID
  申请人：ADOCIA

  公开号：US20190275108A1

  公开（公告）日：2019-09-12

  A composition in the form of an injectable aqueous solution, the pH of which is comprised from 6.0 to 8.0, including at least: a) amylin, an amylin receptor agonist or an amylin analogue; b) a co-polyamino acid bearing carboxylate charges and hydrophobic radicals Hy, said co-polyamino acid being constituted of glutamic or aspartic units and said hydrophobic radicals Hy being according to formula I below: *GpR r GpA a GpC) p Formula I wherein the composition does not comprise a basal insulin the isoelectric point pI of which is comprised from 5.8 to 8.5. It also relates to a composition wherein it further includes prandial insulin.

  一种以可注射的水溶液形式的组合物，其pH值为6.0至8.0，包括至少：a) 胰淀粉样素、胰淀粉样素受体激动剂或胰淀粉样素类似物；b) 载有羧基电荷和疏水基团Hy的共聚氨基酸，所述共聚氨基酸由谷氨酸或天冬氨酸单元构成，所述疏水基团Hy按照下面的公式I：*GpRrGpAaGpC)p。其中，该组合物不包括等电点pI为5.8至8.5的基础胰岛素。还涉及一种组合物，其中还包括餐后胰岛素。
• Carbazole derivatives and their use as neuropeptide y5 receptor ligands
  申请人：——

  公开号：US20040067999A1

  公开（公告）日：2004-04-08

  Compounds of formula (I): are described wherein R 1 -R 6 and m are as defined within. Processes for their preparation and their use as NPY 5 inhibitors is described.

  描述了化学式（I）的化合物，其中R1-R6和m的定义如所述。描述了它们的制备过程以及它们作为NPY 5抑制剂的用途。
• N-TERMINUS MODIFIED ANALOGS OF LHRH
  申请人：Abbott Laboratories

  公开号：EP0738154A1

  公开（公告）日：1996-10-23
• EP0738154A4
  申请人：——

  公开号：EP0738154A4

  公开（公告）日：1996-04-12