1-ethyloctahydroazocine | 73676-23-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-ethyloctahydroazocine
• 英文别名: 1-ethylperhydroazocine；Octahydroazocine, 1-ethyl-；1-ethylazocane
• CAS: 73676-23-0
• 化学式: C₉H₁₉N
• 分子量: 141.257
• InChiKey: ZWPXCDPVWYPZKE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  N-[4-(chloromethyl)-phenyl]-7-(4-methylphenyl)-3,4-dihydronaphthalene-2-carboxamide 、 1-ethyloctahydroazocine 以 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 生成 1-ethyl-1-[4-[7-(4-methyl-phenyl)-3,4-dihydronaphthalene-2-carboxamido]benzyl]perhydroazocinium chloride
  参考文献：
  名称：

  US6166006

  摘要：

  公开号：
• 作为产物：
  描述：

  七亚甲基亚胺 、 乙醚 、 碘乙烷 在 potassium carbonate 作用下， 以 乙醇 为溶剂， 生成 1-ethyloctahydroazocine
  参考文献：
  名称：

  US6166006

  摘要：

  公开号：

文献信息

• [EN] THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER<br/>[FR] AGENTS THÉRAPEUTIQUES CIBLANT LA POLYPOSE ADÉNOMATEUSE COLIQUE (APC) MUTANTE POUR LE TRAITEMENT DU CANCER
  申请人：UNIV TEXAS

  公开号：WO2020117972A1

  公开（公告）日：2020-06-11

  The present disclosure reports an extensive medicinal chemistry evaluation of a large collection of Truncating APC-Selective Inhibitor (TASIN) compounds. The compounds were evaluated for activity against a series of colon cancer cell lines with and without truncating APC-mutations, as well as in an isogenic cell line pair reporting on the status of APC- dependent selectivity. A number of very potent and selective compounds were identified, including compounds with good metabolic stability and PK properties. The small molecules reported herein thus represent a first-in-class genotype-selective series that specifically target ape mutations present in the vast majority of CRC patients, and therefore serves as a translational platform towards a potential targeted therapy for colon cancer.

  本披露报告了对大量截断APC-选择性抑制剂（TASIN）化合物的广泛药物化学评估。这些化合物针对一系列结肠癌细胞系进行了活性评估，包括具有截断APC突变和不具有截断APC突变的细胞系，以及在报告APC依赖性选择性状况的同源细胞系对。鉴定了一些非常有效和选择性的化合物，包括具有良好代谢稳定性和药代动力学性质的化合物。因此，本文报道的小分子代表了一种首创的基因型选择性系列，专门针对存在于绝大多数结直肠癌患者中的猿类突变，因此可作为一个转化平台，朝着结肠癌的潜在靶向治疗迈进。
• BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
  申请人：Katayama Seiji

  公开号：US20130116227A1

  公开（公告）日：2013-05-09

  Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R 1 is a substitutable aminosulfonyl group, etc.; R 2 is a hydrogen atom, etc.; R 3 is a hydrogen atom, etc.; R 4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C 1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R 5a , R 5b and R 5c are each independently hydrogen atoms, etc.; R 6 is a halogen atom, a cyano group, etc.; R 7 and R 8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.)

  揭示了一种表示为公式（1）的新型联苯酰胺衍生物，具有与醛固酮受体的亲和力；还揭示了其药用可接受的盐。（在该公式中，A是由公式（a）表示的任何基团之一；L是—CONH—等；R1是可替代的氨基磺酰基等；R2是氢原子等；R3是氢原子等；R4是氢原子、卤原子、羟基、可替代的氨基基团、可替代的C1-6烷氧基、可替代的4-到7-成员环氨基基团等；R5a、R5b和R5c各自独立地是氢原子等；R6是卤原子、氰基等；R7和R8各自独立地是氢原子等；m是整数，例如0。）
• BICYCLIC COMPOUND, PRODUCTION AND USE THEREOF
  申请人：TOBIRA THERAPEUTICS, INC.

  公开号：US20160008326A1

  公开（公告）日：2016-01-14

  The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R 1 is a 5- to 6-membered ring group which may be substituted; X 1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X 2 is a bivalent group of 1 to 4 atom; Z 1 is a bivalent cyclic ring group or the like; Z 2 is a bond or the like; and R 2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

  本发明提供了一种具有CCR拮抗活性的新环化合物，特别是CCR5拮抗活性，以及其用途。本发明的化合物由以下公式表示：其中，R1是一个可能被取代的5至6成员环基团；X1是键或类似物；环A是一个可能被取代的5至6成员环基团；环B是一个可能被取代的8至10成员环基团；X2是1至4原子的二价基团；Z1是二价环状基团或类似物；Z2是键或类似物；R2是氨基、可能被取代的含氮杂环基团或类似物，或其盐。
• PROLYL HYDROXYLASE INHIBITORS
  申请人：Gardner Joseph H.

  公开号：US20110110961A1

  公开（公告）日：2011-05-12

  Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1α), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

  本文披露了一种可以稳定缺氧诱导因子-1α（HIF-1α）和缺氧诱导因子-2（HIF-2）的脯氨酸羟化酶抑制剂。本文还披露了包含所述化合物的一种或多种药物组合物。此外，还披露了一种用于刺激哺乳动物细胞免疫应答的方法，例如增加吞噬作用，延长吞噬细胞（包括角质细胞、中性粒细胞等）的寿命。因此，所披露的化合物提供了治疗与机体免疫应答相关疾病的方法。
• N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
  申请人：The Procter & Gamble Company

  公开号：US20040097560A1

  公开（公告）日：2004-05-20

  Compounds of Formula (I) 1 are effective in the treatment of a microbial infection.

  化合物式（I）1在治疗微生物感染方面具有良好的疗效。