1-(5-methyl-[2]thienyl)-ethylamine | 603951-41-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-(5-methyl-[2]thienyl)-ethylamine
• 英文别名: 1-(5-Methyl-[2]thienyl)-aethylamin；1-(5-Methylthiophen-2-yl)ethan-1-amine；1-(5-methylthiophen-2-yl)ethanamine
• CAS: 603951-41-3
• 化学式: C₇H₁₁NS
• mdl: MFCD05215239
• 分子量: 141.237
• InChiKey: CODYMUAFGSPBNA-UHFFFAOYSA-N

物化性质

• 沸点：
  95-96 °C(Press: 17 Torr)
• 密度：
  1.066±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  54.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(5-methyl-[2]thienyl)-ethylamine 、 Lithium aluminium hydride 、 2-(1-Azidoethyl)-5-methylthiophene 、 乙酸乙酯 在 Brine 、 Sodium sulfate-III 、 methanol-dichloromethane 、 crude mixture 、 甲醇 、 氨 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 16.0h， 以to obtain the title compound as an oil (80 mg, 95%)的产率得到1-(5-methylthiophen-2-yl)ethan-1-ol
  参考文献：
  名称：

  6-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS

  摘要：

  本发明提供了式I的6-取代的2,3,4,5-四氢-1H-苯并氮烯作为选择性5-HT2C受体激动剂，用于治疗5-HT2C相关疾病，包括肥胖症、强迫症、抑郁症和焦虑症：其中：R6为-C≡C-R10，-O-R12，-S-R14或-NR24R25；其他取代基如规范中所定义。

  公开号：

  US20090099155A1
• 作为产物：
  描述：

  2-乙酰-5-甲基噻吩 在 sodium amalgam 、 羟胺 、 溶剂黄146 作用下， 生成 1-(5-methyl-[2]thienyl)-ethylamine
  参考文献：
  名称：

  Chabrier et al., Bulletin de la Societe Chimique de France, 1946, vol. <5>, p. 332,337

  摘要：

  DOI：

文献信息

• [EN] 6-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS<br/>[FR] 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES SUBSTITUES EN POSITION 6 EN TANT QU'AGONISTES DE RECEPTEUR 5-HT2C
  申请人：LILLY CO ELI

  公开号：WO2005082859A1

  公开（公告）日：2005-09-09

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: I where: R6 is -C=C-R10, -O-R12, -S-R14, or -NR24R25; and other substituents are as defined in the specification.

  本发明提供了公式I中的6-取代的2,3,4,5-四氢-1H-苯并[d]氮杂环庚烯作为选择性5-HT2C受体激动剂，用于治疗与5-HT2C相关的疾病，包括肥胖症、强迫症/强迫性障碍、抑郁症和焦虑症：I其中：R6为-C=C-R10，-O-R12，-S-R14或-NR24R25；其他取代基如规范中所定义。
• THIENO-IMINO ACID DERIVATIVES FOR USE AS MATRIX METALLOPROTEINASE INHIBITORS
  申请人：SCHUDOK Manfred

  公开号：US20070093482A1

  公开（公告）日：2007-04-26

  The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier. The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof. Furthermore the invention is directed to a method for preparing a compound of formula I.

  本发明涉及一种公式I的化合物，其中变量如此处所定义，或其立体异构体形式，立体异构体混合物，以任何比例，或其盐。另一个方面的本发明涉及一种制药组合物，该制药组合物包括根据权利要求1的公式I中的一个或多个化合物的药学有效量与药学可接受的载体混合。本发明还涉及一种用于预防和治疗退行性关节疾病，如骨关节炎、脊椎病、关节创伤后软骨丢失或关节固定期较长时间内的髁盖板或髌骨损伤或韧带断裂、结缔组织疾病如胶原病、牙周病、创伤愈合障碍和运动器官的慢性疾病，如炎症、免疫或代谢相关的急性和慢性关节炎、关节病、肌痛和骨代谢障碍的方法，用于溃疡、动脉粥样硬化和狭窄的治疗，以及用于炎症、癌症、肿瘤转移形成、消瘦、厌食、心力衰竭和脓毒性休克的治疗或预防心肌和脑梗死的方法，包括向患者施用根据权利要求1的公式I的药学有效量或其药学可接受的盐、溶剂或前药。此外，本发明还涉及一种制备公式I化合物的方法。
• 6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist
  申请人：ALLEN JOHN GORDON

  公开号：US20120028961A1

  公开（公告）日：2012-02-02

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is —S—R 14 ; and other substituents are as defined in the specification.

  本发明提供了公式I的6-取代的2,3,4,5-四氢-1H-苯并[d]氮杂环作为选择性5-HT2C受体激动剂，用于治疗5-HT2C相关疾病，包括肥胖症、强迫症、抑郁症和焦虑症：其中：R6为—S—R14；其他取代基如规范中所定义。
• 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines as 5-HT2C receptor agonists
  申请人：Eli Lilly and Company

  公开号：US08022062B2

  公开（公告）日：2011-09-20

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —C≡C—R10, —O—R12, —S—R14, or —NR24R25; and other substituents are as defined in the specification.

  本发明提供了式I的6-取代2,3,4,5-四氢-1H-苯并[d]氮杂环化合物，作为选择性5-HT2C受体激动剂，用于治疗与5-HT2C相关的疾病，包括肥胖症、强迫症、抑郁症和焦虑症：其中：R6是—C≡C—R10，—O—R12，—S—R14或—NR24R25; 其他取代基如规范中定义。
• 6 substituted 2, 3,4,5 tetrahydro-1H-benzo[d]azepines as 5-HT2C receptor agonist
  申请人：Allen John Gordon

  公开号：US08580780B2

  公开（公告）日：2013-11-12

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —S—R14; and other substituents are as defined in the specification.

  本发明提供了6-取代的2,3,4,5-四氢-1H-苯并[d]氮杂环化合物I的选择性5-HT2C受体激动剂，用于治疗与5-HT2C相关的疾病，包括肥胖症、强迫症、抑郁症和焦虑症：其中：R6为—S—R14;其他取代基如规范中所定义。