1-(o-Iodphenyl)-2-propylamin | 21894-70-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(o-Iodphenyl)-2-propylamin
• 英文别名: 2-Iodoamphetamine；1-(2-iodophenyl)propan-2-amine
• CAS: 21894-70-2
• 化学式: C₉H₁₂IN
• 分子量: 261.105
• InChiKey: WSTDXRKNIDTRHW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  1-(2-iodophenyl)propan-2-one 在 甲酸 、 formamide 作用下， 反应 16.0h， 生成 1-(o-Iodphenyl)-2-propylamin
  参考文献：
  名称：

  Binovic,K.; Vrancea,S., Chimica Therapeutica, 1968, vol. 3, p. 313 - 320

  摘要：

  DOI：

文献信息

• [EN] TRP-M8 RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS<br/>[FR] LIGANDS DU RÉCEPTEUR TRP-M8 ET LEUR UTILISATION DANS DES TRAITEMENTS
  申请人：AMGEN INC

  公开号：WO2009073203A1

  公开（公告）日：2009-06-11

  Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintened pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

  公式（I）的四氢异喹啉化合物及含有它们的组合物，用于治疗急性、炎症性和神经性疼痛、牙痛、普通头痛、偏头痛、集群头痛、混合血管和非血管综合征、紧张性头痛、一般炎症、关节炎、风湿性疾病、骨关节炎、炎症性肠道疾病、炎症性眼部疾病、炎症性或不稳定的膀胱疾病、牛皮癣、带有炎症成分的皮肤疾病、慢性炎症症状、炎症性疼痛及相关的过敏性疼痛和触痛、神经性疼痛及相关的过敏性疼痛和触痛、糖尿病性神经病痛、烧灼性疼痛、交感神经维持性疼痛、感觉缺失综合征、哮喘、上皮组织损伤或功能障碍、单纯疱疹、呼吸、泌尿、消化或血管区域内脏运动障碍、伤口、烧伤、过敏性皮肤反应、瘙痒、白癜风、一般胃肠道疾病、胃溃疡、十二指肠溃疡、腹泻、坏死性剂引起的胃病变、毛发生长、血管运动性或过敏性鼻炎、支气管疾病或膀胱疾病。
• [EN] COMPOSITIONS COMPRISING ENZYME-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS DE TYPE AMPHÉTAMINE CLIVABLES PAR ENZYME ET LEURS INHIBITEURS
  申请人：PHARMACOFORE INC

  公开号：WO2011133348A1

  公开（公告）日：2011-10-27

  Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

  提供了药物组合物及其使用方法，其中药物组合物包括一种苯丙胺前药，该前药提供苯丙胺或苯丙胺类似物的酶控释放。该组合物还可以包括一种酶抑制剂，与介导苯丙胺前药中的苯丙胺或苯丙胺类似物的酶相互作用，以减轻苯丙胺前药的酶催化裂解。
• Method of preparing a chlorinated, brominated, radiobrominated, iodinated and/or radioiodinated, aromatic or heteroaromatic compound, as well as a kit for preparing a diagnostic composition on the basis of this compound
  申请人：MALLINCKRODT, INC.(a Missouri corporation)

  公开号：EP0165630A2

  公开（公告）日：1985-12-27

  The invention relates to a method of preparing a chlorinated, brominated, radiobrominated, iodinated and/or radio-iodinated aromatic or heteroaromatic compound, in which the (hetero)aromatic nucleus optionally comprises one or more additional substituents, by reacting the corresponding halogenated or diazonium-substituted compound in the presence of a water-soluble acid and of copper ions as a catalyst with a likewise water-soluble chloride, bromide radiobromide, iodide or radio-iodide, in which the reaction is carried out in the presence of one or more reduction agents, which are stable in acid medium, in a quantity exceeding the quantity of catalyst. The invention also relates to a composition suitable for diagnostic examination and to a kit for the preparation thereof. The invention further relates to a method and an equipment for the preparation of said composition.

  本发明涉及一种制备氯化、溴化、放射性溴化、碘化和/或放射性碘化芳香族或杂芳香族化合物的方法，其中（杂）芳香族核可选择地包括一个或多个附加取代基、在水溶性酸和作为催化剂的铜离子存在下，使相应的卤代或重氮代化合物与同样的水溶性氯化物、溴化物、放射性溴化物、碘化物或放射性碘化物反应，其中反应是在一种或多种在酸介质中稳定的还原剂存在下进行的，还原剂的数量超过催化剂的数量。本发明还涉及一种适用于诊断检查的组合物及其制备试剂盒。本发明还涉及制备上述组合物的方法和设备。
• CEREBRAL BLOOD FLOW QUANTIFICATION DEVICE, CEREBRAL BLOOD FLOW QUANTIFICATION METHOD AND PROGRAM
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：EP2249181A1

  公开（公告）日：2010-11-10

  A cerebral blood flow rate quantification device (10) comprises: a nuclear medicine image acquisition unit (12) for acquiring a nuclear medicine image of the head of a subject administered with a radiopharmaceutical; a count calculation unit (16) for calculating the number of counts obtained from a unit region indicating the same location in brain tissue in a plurality of nuclear medicine images of the head successively imaged between first time and second time; a cerebral blood flow rate calculation unit (24) for calculating, for each unit region, the value of a cerebral blood flow rate that makes the value of a function integrated from the first time to the second time equal to the number of counts, the function which, with cerebral blood flow rate and time elapsed from the administration of the radiopharmaceutical being as variables, expresses the concentration of the radiopharmaceutical in brain tissue; and a cerebral blood flow map generation unit (30) for generating a map showing cerebral blood flow based on the cerebral blood flow rate in each unit region. Consequently, the cerebral blood flow rate can be accurately quantified even at a relatively early stage after administration of a radiopharmaceutical.

  脑血流量定量装置（10）包括核医学影像采集单元（12），用于采集接受放射性药物治疗的受试者头部的核医学影像； 计数计算单元（16），用于计算在第一时间和第二时间之间连续成像的多个头部核医学影像中表示脑组织中相同位置的单位区域获得的计数数；脑血流率计算单元（24），用于为每个单元区域计算脑血流率值，使从第一时间到第二时间的函数积分值等于计数数，该函数以脑血流率和从施放放射性药物开始的时间为变量，表示放射性药物在脑组织中的浓度；脑血流图生成单元（30），用于根据每个单元区域的脑血流速率生成显示脑血流的地图。因此，即使在施用放射性药物后的较早阶段，也能准确量化脑血流量。
• 5-HT2C receptor agonists and compositions and methods of use
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US10272094B2

  公开（公告）日：2019-04-30

  Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.

  在一些实施方案中，提供了如本文所定义的式 A 化合物，其可调节 5-HT2C 受体的活性。在一些实施方案中还提供了一些方法，例如，用于体重管理、诱导饱腹感和减少食物摄入量，以及预防和治疗肥胖症、抗精神病药诱导的体重增加、2 型糖尿病、普拉德-威利综合征、烟草/尼古丁依赖、药物成瘾、酒精成瘾、病态赌博、奖赏缺乏综合征和性成瘾）、强迫症谱系障碍和冲动控制障碍（包括咬指甲和嗜睡）、睡眠障碍（包括失眠、睡眠结构破碎和慢波睡眠紊乱）、尿失禁、精神障碍（包括精神分裂症、神经性厌食症和神经性贪食症）、老年痴呆症、性功能障碍、勃起功能障碍、癫痫、运动障碍（包括帕金森病和抗精神病药物诱发的运动障碍）、高血压、血脂异常、非酒精性脂肪肝、肥胖相关性肾病和睡眠呼吸暂停。