4-ethyl-N-methylcyclohexan-1-amine | 252854-34-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-ethyl-N-methylcyclohexan-1-amine
• CAS: 252854-34-5
• 化学式: C₉H₁₉N
• mdl: MFCD09044903
• 分子量: 141.25
• InChiKey: QMMUYVTYTBICLS-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：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• Substituted Cyclohexylamine Compounds
  申请人：EPIZYME, INC.

  公开号：US20200123142A1

  公开（公告）日：2020-04-23

  The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2a , R 2b , R 3a , R 3b , R 4 , R 5 , and R 7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

  本公开提供具有化学式（I）的替代环己胺化合物及其药用可接受的盐和溶剂化合物，其中R1、R2a、R2b、R3a、R3b、R4、R5和R7如规范中所定义。本公开还涉及使用化合物I的方法来治疗对SMYD蛋白如SMYD3或SMYD2阻断产生反应的疾病。本公开的化合物特别适用于治疗癌症。
• [EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITOR AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE KINASE ET LEURS UTILISATIONS
  申请人：INTEGRAL BIOSCIENCES PVT LTD

  公开号：WO2021019514A1

  公开（公告）日：2021-02-04

  The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed.

  本公开涉及一般用于治疗与检查点激酶（CHK）相关疾病的化合物，特别是CHK-1酶。具体地，本发明揭示了式（IA）的化合物，该化合物对CHK-1酶具有抑制活性。公开了使用这些化合物治疗与CHK-1酶过度活性相关的疾病的方法。还公开了这些化合物的用途、制药组合物、试剂盒和合成方法。
• OXAZOLE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：BARTH Francis

  公开号：US20070043060A1

  公开（公告）日：2007-02-22

  This invention relates to compounds of formula (I): Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.

  本发明涉及式(I)化合物：其中R1、R2、R3、R4、R5、R6、R7和R8如本文所述。本发明还涉及其预防和治疗用途的方法。
• AROMATIC AMINE AR AND BET TARGETING PROTEIN DEGRADATION CHIMERA COMPOUND AND USE
  申请人：Hinova Pharmaceuticals Inc.

  公开号：EP3971176A1

  公开（公告）日：2022-03-23

  An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound and its use. Specifically provided is a compound represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide); the compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.

  一种芳香胺雄激素受体（AR）和BET靶向蛋白降解嵌合物化合物及其用途。具体提供的是由式I表示的化合物。实验结果表明，该化合物可以靶向降解AR和BRD4，并下调AR和BRD4蛋白的表达；该化合物可以抑制多种前列腺癌细胞的增殖；该化合物可以抑制过表达AR的前列腺癌细胞系LNCaP/AR的增殖，并且对一种对市售前列腺癌药物（恩扎鲁胺）具有耐药性的前列腺癌细胞系22RV1具有良好的抑制效果；该化合物还表现出良好的代谢稳定性，在制备AR和/或BET蛋白降解靶向嵌合物和治疗由AR和BET调控的相关疾病的药物方面具有良好的应用前景。
• [EN] NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS<br/>[FR] NOUVEAUX GLYCOPEPTIDES SEMI-SYNTHÉTIQUES COMME AGENTS ANTIBACTÉRIENS
  申请人：LEAD THERAPEUTICS INC

  公开号：WO2010065174A1

  公开（公告）日：2010-06-10

  Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi¬ synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

  本文介绍了具有抗菌活性的半合成糖肽，特别是在这里描述的半合成糖肽是通过化学修饰糖肽（化合物A、化合物B、化合物H或化合物C）或通过在酸性介质中水解母体糖肽的氨基酸-4的二糖基团，从而得到氨基酸-4单糖的方法制备的；将单糖转化为氨基糖衍生物；用特定的酰基基团对这些支架上氨基酸-4氨基取代糖基团上的氨基取代基进行酰化；并将这些支架上的大环环上的酸基团转化为某些取代酰胺。关键反应是用异氰酸酯处理适当保护的中间化合物。还提供了合成这些化合物的方法，含有这些化合物的制药组合物以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。