N,N-Dimethyl-N-(1-ethylcyclohexyl)-amin | 99863-03-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N,N-Dimethyl-N-(1-ethylcyclohexyl)-amin
• 英文别名: (1-ethyl-cyclohexyl)-dimethyl-amine；(1-Aethyl-cyclohexyl)-dimethyl-amin；1-ethyl-N,N-dimethylcyclohexan-1-amine
• CAS: 99863-03-3
• 化学式: C₁₀H₂₁N
• 分子量: 155.283
• InChiKey: JJSPISROASWDLZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  11
• 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：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• [EN] NEW PYRROLIDINE-2-CARBOXYLIC ACID DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS<br/>[FR] NOUVEAUX DÉRIVÉS D'ACIDE PYRROLIDINE-2-CARBOXYLIQUE POUR LE TRAITEMENT DE LA DOULEUR ET D'ÉTATS PATHOLOGIQUES ASSOCIÉS À LA DOULEUR
  申请人：ESTEVE PHARMACEUTICALS SA

  公开号：WO2020120606A1

  公开（公告）日：2020-06-18

  The present invention relates to new compounds that show pharmacological activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the µ-opiod receptor (MOR or mu-opioid). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments (formula (I)).

  本发明涉及对电压门控钙通道（VGCC）的亚单位α2δ，特别是对电压门控钙通道的α2δ-1亚单位或对电压门控钙通道（VGCC）的亚单位α2δ表现出药理活性的新化合物，特别是对电压门控钙通道的α2δ-1亚单位，以及与µ-阿片受体（MOR或μ-阿片）具有双重活性。该发明还涉及所述化合物的制备方法，以及包含它们的组合物，以及它们作为药物的用途（公式（I））。
• Norvaline Derivative and Method for Preparation Thereof
  申请人：Harada Naoyuki

  公开号：US20080076769A1

  公开（公告）日：2008-03-27

  Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2). [wherein X is —CH 2 —, —O—, —S— or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R 1 and R 2 are (i) each is hydrogen or lower alkyl; (ii) R 1 and R 2 are combined to form lower alkylene; or (iii) R 1 is hydrogen or lower alkyl and R 2 is combined with R 4 or R 6 to form lower alkylene; R 3 and R 4 are (i) each is hydrogen or lower alkyl; (ii) R 3 and R 4 are combined to form lower alkylene; or (iii) R 3 is hydrogen or lower alkyl and R 4 is combined with R 2 or R 6 to form lower alkylene; R is or —OR 7 ; R 5 and R 6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R 5 and R 6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R 5 is optionally substituted lower alkyl or hydrogen and R 6 is combined with R 2 or R 4 to form lower alkylene; R 7 is lower alkyl.

  Norvaline衍生物的化学式[I]或其药学上可接受的盐，制备方法，含有该化合物的药物组合物，以及用于抑制甘氨酸转运体2型（GlyT2）的转运活性的用途。[其中X为-CH2-，-O-，-S-或单键；Ar为可选取代芳基或较低的环烷基；n为0至2；R1和R2为（i）氢或较低的烷基；（ii）R1和R2结合形成较低的烷基；或（iii）R1为氢或较低的烷基，R2与R4或R6结合形成较低的烷基；R3和R4为（i）氢或较低的烷基；（ii）R3和R4结合形成较低的烷基；或（iii）R3为氢或较低的烷基，R4与R2或R6结合形成较低的烷基；R为-OH或-OR7；R5和R6为（i）可选取代的较低烷基或氢；（ii）R5和R6结合形成脂肪族5-至6-成员杂环基；或（iii）R5为可选取代的较低烷基或氢，R6与R2或R4结合形成较低的烷基；R7为较低烷基。
• Pyrrole Derivative or Salt Thereof
  申请人：Seo Ryushi

  公开号：US20090036421A1

  公开（公告）日：2009-02-05

  [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

  [问题] 提供一种可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病，特别是治疗肠易激综合征（IBS）的化合物。 [解决方案] 发现一种吡咯衍生物，在其3位具有胍基甲酰基基团或酰胺基团作为取代基团，或其药学上可接受的盐，具有对5-HT2B受体和5-HT7受体的强拮抗作用。此外，与仅使用对其中一种受体选择性拮抗剂相比，具有对两种受体拮抗活性的本发明化合物显示出良好的药理作用。基于上述，本发明化合物对于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病，特别是治疗肠易激综合征（IBS）是有用的。
• 2-AMINOBENZAMIDE DERIVATIVE
  申请人：Kuramochi Takahiro

  公开号：US20090233900A1

  公开（公告）日：2009-09-17

  To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

  本发明提供了一种基于对辣椒素受体VR1激活的抑制作用的新型优良药剂，用于治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等疾病。本发明通过确认一种苯甲酰胺衍生物，其特征在于其苯环上的单环在酰胺基氮原子上被紧缩，其低烷基氨基或邻位于酰胺基的环基取代的氨基具有对VR1激活的强抑制作用和优良的药理作用，从而发现它可以成为治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等VR1相关疾病的优良药剂。
• AMIDE DERIVATIVE OR SALT THEREOF
  申请人：Kaku Hidetaka

  公开号：US20090062363A1

  公开（公告）日：2009-03-05

  [Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

  [问题] 提供一种可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法] 发现一种具有含氮双环杂环（例如吲哚或类似物）的酰胺衍生物或其药学上可接受的盐具有强烈的5-HT2B受体和5-HT7受体的拮抗作用。此外，本发明的化合物具有对两种受体的拮抗活性，与仅使用选择性拮抗剂相比，表现出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病，特别是用于治疗肠易激综合征（IBS）。