(哌啶-4-氧基)-乙酸甲酯盐酸盐 | 146117-95-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: (哌啶-4-氧基)-乙酸甲酯盐酸盐
• 中文别名: 4-基氧哌啶乙酸甲酯盐酸盐
• 英文名称: methyl 2-(piperidin-4-yloxy)acetate hydrochloride salt
• 英文别名: methyl (piperidin-4-yl-oxy)acetate hydrochloride；methyl 4-piperidinyloxy-acetate hydrochloride；methyl 4-piperidinoxyacetate hydrochloride；(Piperidin-4-yloxy)-acetic acid methyl ester hydrochloride；methyl 2-piperidin-4-yloxyacetate;hydrochloride
• CAS: 146117-95-5
• 化学式: C₈H₁₅NO₃*ClH
• 分子量: 209.673
• InChiKey: XQDBZKHPFFODOD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.35
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  47.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (哌啶-4-氧基)-乙酸甲酯盐酸盐 在 tris-(dibenzylideneacetone)dipalladium(0) 、 caesium carbonate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 、 N,N-二异丙基乙胺 作用下， 以 N-甲基吡咯烷酮 、 甲苯 为溶剂， 反应 8.0h， 生成 methyl [(1-{5-fluoro-6-[(4-[3-fluoro-5-(trifluoromethyl)phenyl]-5-{[(2R)-2-methylpyrrolidin-1-yl]methyl}-1,3-thiazol-2-yl)amino]pyrimidin-4-yl}piperidin-4-yl)oxy]acetate
  参考文献：
  名称：

  2-AMINOTHIAZOLE DERIVATIVES OR SALT THEREOF AS MUSCARINIC M3 LIGANDS FOR THE TREATMENT OF BLADDER DISEASES

  摘要：

  公开号：

  EP3196200B1
• 作为产物：
  描述：

  2-氯-5-硝基烟酸乙酯 在 ethereal hydrochloric acid 作用下， 以 甲醇 为溶剂， 生成 (哌啶-4-氧基)-乙酸甲酯盐酸盐
  参考文献：
  名称：

  Piperazine derivatives, pharmaceutical compositions containing these

  摘要：

  吡嗪衍生物在治疗或预防炎症、骨质疏松、血栓形成和肿瘤转移方面具有用处。示例物种包括：(a) \x9b4-反式-\x9b3-\x9b4-(4-吡啶基)-哌嗪-1-基丙酰氨基-环己烷羧酸，(b) 3-\x9b4-反式-\x9b4-(4-吡啶基)-哌嗪-1-基甲酰氨基-环己基丙酸，(c) 3-\x9b4-反式-\x9b4-(4-吡啶基)-哌嗪-1-基马酰氨基环己基羧酸，(d) 甲基\x9b4-反式-\x9b3-\x9b4-(4-吡啶基)-哌嗪-1-基丙酰氨基环己烷羧酸酯，(e) 甲基3-\x9b4-反式-\x9b4-(4-吡啶基)-哌嗪-1-基甲酰氨基环己基丙酸酯，(f) 甲基\x9b4-反式-\x9b4-(4-吡啶基)-哌嗪-1-基马酰氨基环己基羧酸酯，(g) 环己基\x9b4-反式-\x9b\x9b4-(4-吡啶基)-哌嗪-1-基乙酰氨基环己烷羧酸酯，和(h) 异丁基\x9b4-反式-\x9b\x9b4-(4-吡啶基)-哌嗪-1-基乙酰氨基环己烷羧酸酯。

  公开号：

  US05700801A1

文献信息

• Piperazine derivatives, medicaments comprising these compounds, their
  申请人：Dr. Karl Thomae GmbH

  公开号：US05922717A1

  公开（公告）日：1999-07-13

  The present invention relates to piperazine derivatives of the general formula ##STR1## in which R.sub.a, Y.sub.1 to Y.sub.3 and E are defined herein, tautomers thereof, stereoisomers thereof, including their mixtures, and salts thereof, and in particular physiologically tolerated salts thereof with inorganic or organic acids or bases. These compounds have valuable pharmacological properties, such as aggregation-inhibiting activity. This invention also relates to medicaments comprising these compounds and to processes for the preparation of these compounds.

  本发明涉及一般式##STR1##的哌嗪衍生物，其中R.sub.a，Y.sub.1至Y.sub.3和E在此定义，其互变异构体，立体异构体，包括它们的混合物，以及其盐，特别是与无机或有机酸或碱的生理耐受盐。这些化合物具有有价值的药理特性，如抑制聚集活性。本发明还涉及包含这些化合物的药物和制备这些化合物的方法。
• Prodrugs of Compounds that Enhance Antifungal Activity and Compositions of Said Prodrugs
  申请人：MethylGene Inc.

  公开号：US20150203517A1

  公开（公告）日：2015-07-23

  The invention relates to prodrugs for use in the inhibition of histone deacetylase. The prodrugs of the present invention have good aqueous solubility and good aqueous stability. The prodrugs of the invention advantageously are metabolized to the active ingredient in plasma or in the blood stream of a warm-blooded animal. The invention also provides compositions and, and methods for making the prodrugs, and methods for using the prodrugs to treat fungal infections.

  该发明涉及用于抑制组蛋白去乙酰化酶的前药。本发明的前药具有良好的水溶性和良好的水稳定性。本发明的前药有利地在温血动物的血浆或血液中代谢成活性成分。该发明还提供了制备前药的组合物和方法，以及使用前药治疗真菌感染的方法。
• Amino acid derivatives
  申请人：Hoffmann-La Roche Inc

  公开号：US05378712A1

  公开（公告）日：1995-01-03

  N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or control of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.

  式为##STR1##的N-酰基-.alpha.-氨基羧酸衍生物，其中L、R'至R" "和Q具有描述中给出的含义，可用于治疗或控制由粘附蛋白结合到血小板和血小板聚集和细胞-细胞黏附引起的疾病。
• 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도
  申请人：주식회사 유빅스테라퓨틱스

  公开号：KR20230053600A

  公开（公告）日：2023-04-21

  본 개시는 안드로겐 수용체(androgen receptor; AR)를 분해하는 활성을 갖는 특정 화학구조의 화합물 또는 이의 약학적으로 허용 가능한 염을 제공한다. 본 개시는 또한 이러한 화합물 또는 이의 약학적으로 허용 가능한 염을 포함하는 조성물을 제공한다. 본 개시는 또한 본 개시에 따른 화합물, 이의 염 및 이들을 포함하는 조성물의 AR 관련 질환의 치료 또는 예방용 의약 용도를 제공한다. 본 개시는 또한 본 개시에 따른 화합물, 이의 염 또는 이들을 포함하는 조성물의 유효한 양을 치료가 필요한 개체에게 투여하는 것을 포함하는 AR 관련 질환의 치료 또는 예방 방법을 제공한다.

  本发明提供了一种具有分解雄性激素受体（androgen receptor; AR）活性的特定化学结构的化合物，或其药学上可接受的盐。本发明还提供了一种包含这些化合物或其药学上可接受的盐的组合物。本发明还涉及根据本发明的化合物、其盐及包含它们的组合物在治疗或预防与AR相关的疾病中的医药用途。此外，本发明还提供了一种治疗或预防与AR相关的方法，该方法包括向有需要的个体给药上述化合物、其盐或包含它们的组合物的有效量。
• US5378712A
  申请人：——

  公开号：US5378712A

  公开（公告）日：1995-01-03