替氟朵 | 83386-35-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 中文名称: 替氟朵
• 英文名称: tifluadom
• 英文别名: 1-methyl-2-[(thiophene-3-carbonyl)-aminomethyl]-5-(2-fluorophenyl)-1H-2,3-dihydro-1,4-benzodiazepine；N-[[5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1,4-benzodiazepin-2-yl]methyl]thiophene-3-carboxamide
• CAS: 83386-35-0
• 化学式: C₂₂H₂₀FN₃OS
• 分子量: 393.485
• InChiKey: NPGABYHTDVGGJK-UHFFFAOYSA-N

物化性质

• 沸点：
  592.7±50.0 °C(Predicted)
• 密度：
  1.28

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  72.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  替氟朵 在 sodium cyanoborohydride 作用下， 以 水 、 溶剂黄146 为溶剂， 生成 1-methyl-2-(3-thiophenecarbonyl)aminomethyl-5-(2'-fluorophenyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine
  参考文献：
  名称：

  2-substituted-aminomethyl-1,4-benzodiazepines

  摘要：

  这篇文章介绍了一种新型的2-取代氨甲基-1,4-苯二氮平衍生物，发现其可以作为胆囊收缩素（CCK）功能的拮抗剂，同时介绍了这些化合物的制备方法，以及利用这些化合物拮抗CCK功能的用途。该拮抗作用可用于治疗和预防哺乳动物，尤其是人类的胃肠道、中枢神经系统和食欲调节系统的紊乱。

  公开号：

  US04724237A1

文献信息

• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Treatment of pain with combinations of nalbuphine and other kappa-opioid receptor agonists and opioid receptor antagonists
  申请人：The Regents of the University of California

  公开号：US20040180916A1

  公开（公告）日：2004-09-16

  Methods and compositions for treating, managing or ameliorating pain in a subject (preferably, a mammal, and more preferably, a human) comprising administration of a centrally acting (i.e., crosses the blood brain barrier) agonist of a &kgr;-opioid receptor and a centrally acting opioid antagonist such that the analgesia achieved by this administration is greater than with administration of either the &kgr;-opioid receptor agonist or the opioid antagonist alone. Preferably the &kgr;-opioid receptor is nalbuphine or a salt or prodrug of nalbuphine and the opioid antagonist is naloxone or a salt or prodrug of naloxone. Preferred methods of administration include mucosal (e.g. intranasal or pulmonary) and intravenous. Other &kgr;-opioid receptors include pentazocine and butorphanol.

  本发明涉及用于治疗、管理或缓解受体（优选为哺乳动物，更优选为人类）疼痛的方法和组合物，包括给予中枢作用（即穿过血脑屏障）的&kgr;-阿片受体激动剂和中枢作用阿片受体拮抗剂，使得通过此给予的镇痛作用大于单独给予&kgr;-阿片受体激动剂或阿片受体拮抗剂的镇痛作用。优选的&kgr;-阿片受体为纳布啡或纳布啡的盐或前药，而阿片受体拮抗剂为纳洛酮或纳洛酮的盐或前药。优选的给药方法包括黏膜（例如鼻内或肺部）和静脉注射。其他&kgr;-阿片受体包括哌替啶和丁丙诺啡。
• Hybrid Opioid Compounds and Compositions
  申请人：Holaday John W.

  公开号：US20110245287A1

  公开（公告）日：2011-10-06

  Disclosed are hybrid opioid compounds, mixed opioid salts, compositions comprising the hybrid opioid compounds and mixed opioid salts, and methods of use thereof. More particularly, in one aspect the hybrid opioid compound includes at least two opioid compounds that are covalently bonded to a linker moiety. In another aspect, the hybrid opioid compound relates to mixed opioid salts comprising at least two different opioid compounds or an opioid compound and a different active agent. Also disclosed are pharmaceutical compositions, as well as to methods of treating pain in humans using the hybrid compounds and mixed opioid salts.

  本发明涉及混合型阿片类化合物、混合型阿片盐、包括混合型阿片类化合物和混合型阿片盐的组合物以及其使用方法。更具体地，在一个方面，混合型阿片类化合物包括至少两种阿片类化合物，它们与连接物基团共价键合。在另一个方面，混合型阿片类化合物涉及至少两种不同的阿片类化合物或一种阿片类化合物和不同的活性剂组成的混合型阿片盐。还公开了制药组合物以及使用混合化合物和混合型阿片盐治疗人体疼痛的方法。
• Therapeutic Treatment
  申请人：Sears Douglas

  公开号：US20140100249A1

  公开（公告）日：2014-04-10

  This invention discloses a treatment for a patient receiving medication to treat an attention deficit disorder such as ADHD wherein the treatment results in a loss of appetite and impairment of the patient's attentiveness. The treatment combines a treatment for an attention deficit disorder with an appetite stimulant, wherein the appetite stimulant increases the caloric intake of a patient, which can increase the patient's attentiveness. The combination treatment can be given for an indefinite, including, without limitation, life-long, to allow a patient to maintain normal caloric intake during treatment for an attention deficit disorder.

  本发明揭示了一种治疗接受治疗注意力缺陷障碍（如ADHD）的患者的方法，其中治疗导致患者食欲下降和注意力受损。该治疗将注意力缺陷障碍的治疗与食欲刺激剂相结合，其中食欲刺激剂增加患者的热量摄入量，这可以增加患者的注意力。该组合治疗可以无限期地给予，包括但不限于终身，以使患者在接受注意力缺陷障碍治疗期间保持正常的热量摄入量。