2-methyl-2-(pyridin-4-yl)propan-1-amine | 1060815-29-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-methyl-2-(pyridin-4-yl)propan-1-amine
• 英文别名: 2-methyl-2-pyridin-4-ylpropan-1-amine
• CAS: 1060815-29-3
• 化学式: C₉H₁₄N₂
• mdl: MFCD11898942
• 分子量: 150.224
• InChiKey: OJQCYAVJFWTLBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.444
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 危险等级：
  IRRITANT

反应信息

• 作为反应物：
  描述：

  1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)piperidine-4-carboxylic acid 、 2-methyl-2-(pyridin-4-yl)propan-1-amine 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 0.17h， 以23%的产率得到1-(1-(4-chlorobenzyl)-1H-indole-2-carbonyl)-N-(2-methyl-2-(pyridin-4-yl)propyl)piperidine-4-carboxamide
  参考文献：
  名称：

  Optimization of Novel Indole-2-carboxamide Inhibitors of Neurotropic Alphavirus Replication

  摘要：

  Neurotropic alphaviruses, which include western equine encephalitis virus (WEEV) and Fort Morgan virus, are mosquito-borne pathogens that infect the central nervous system causing acute and potentially fatal encephalitis. We previously reported a novel series of indole-2-carboxamides as alphavirus replication inhibitors, one of which conferred protection against neuroadapted Sindbis virus infection in mice. We describe here further development of this series, resulting in 10-fold improvement in potency in a WEEV repliton assay and up to 40-fold increases in half-lives in mouse liver microsomes. Using a rhodamine123 uptake assay in MDR1-MDCKII cells, we were able to identify structural modifications that markedly reduce recognition by P-glycoprotein, the key efflux transporter at the blood brain barrier. In a preliminary mouse PK study, we were able to demonstrate that two new analogues could achieve higher and/or longer plasma drug exposures than our previous lead and that one compound achieved measurable drug levels in the brain.

  DOI：

  10.1021/jm401330r

文献信息

• [EN] DERIVATIVES OF beta , beta -DIMETHYL-4-PIPERIDINEETHANAMINE AS INHIBITORS OF THE CHOLESTEROL BIOSYNTHESIS<br/>[FR] DERIVES DE BETA, BETA-DIMETHYL-4-PIPERIDINEETHANAMINE COMME INHIBITEURS DE LA BIOSYNTHESE DU CHOLESTEROL
  申请人：FOURNIER INDUSTRIE ET SANTE

  公开号：WO1994026713A1

  公开（公告）日：1994-11-24

  (EN) The present invention relates to $g(b),$g(b)-dimethyl-4-piperidineethanamine having the formula (I), wherein the groups R1 to R3 are defined as indicated in the description. It also relates to the method for preparing and using them in therapy as inhibitor agents to inhibit the cholesterol biosynthesis, particularly of epoxysqualene cyclase, useful as hypocholesterolemic agents, hypolipemic agents, antiatheromatous agents and antifongic agents.(FR) La présente invention concerne les $g(b),$g(b)-diméthyl-4-pipéridine-éthanamine de formule (I) (où les groupes R1 à R3 sont définis comme indiqué dans la description). Elle concerne également leur procédé de préparation et leur utilisation en thérapeutique en tant qu'agents inhibiteurs de la biosynthèse du cholestérol, notamment de l'époxysqualène cyclase, utiles comme hypocholestéroléminants, hypolipémiants, antiathéromateux et antifongiques.

  本发明涉及具有式(I)的$g(b),$g(b)-二甲基-4-哌啶乙胺，其中R1至R3基团如说明中所示。它还涉及制备和使用它们作为抑制胆固醇生物合成的抑制剂，特别是抑制环氧齐墩烯环化酶，有用作为降胆固醇剂、降脂剂、抗动脉粥样硬化剂和抗真菌剂的治疗药物。
• 1,3,4-OXADIAZOLONE COMPOUND AND MEDICINE
  申请人：Nippon Shinyaku Co., Ltd.

  公开号：EP3882239A1

  公开（公告）日：2021-09-22

  The purpose of the present invention is to provide a compound having PIM inhibitory activity. Examples of the present invention include 1,3,4-oxadiazolone compounds represented by the following formula [1], and pharmaceutically acceptable salts, and solvates thereof. The compounds of the present invention have PIM inhibitory activity. In addition, since the compounds of the present invention have PIM inhibitory activity, the compounds of the present invention are useful as therapeutic agents for systemic lupus erythematosus, lupus nephritis, etc.

  本发明的目的是提供一种具有 PIM 抑制活性的化合物。 本发明的实例包括下式[1]代表的 1，3，4-噁二唑酮化合物及其药学上可接受的盐和溶液。 本发明的化合物具有 PIM 抑制活性。此外，由于本发明的化合物具有 PIM 抑制活性，因此本发明的化合物可用作系统性红斑狼疮、狼疮肾炎等的治疗剂。
• EP3882239
  申请人：——

  公开号：——

  公开（公告）日：——
• DERIVES DE BETA, BETA-DIMETHYL-4-PIPERIDINEETHANAMINE COMME INHIBITEURS DE LA BIOSYNTHESE DU CHOLESTEROL
  申请人：FOURNIER INDUSTRIE ET SANTE

  公开号：EP0699187A1

  公开（公告）日：1996-03-06
• DERIVES DE BETA,BETA-DIMETHYL-4-PIPERIDINEETHANAMINE COMME INHIBITEURS DE LA BIOSYNTHESE DU CHOLESTEROL
  申请人：FOURNIER INDUSTRIE ET SANTE

  公开号：EP0699187B1

  公开（公告）日：1997-01-22