4,4-Di-2-thienyl-3-buten-2-amine | 857725-50-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 杂芳族化合物
• 英文名称: 4,4-Di-2-thienyl-3-buten-2-amine
• 英文别名: 4,4-dithiophen-2-ylbut-3-en-2-amine
• CAS: 857725-50-9
• 化学式: C₁₂H₁₃NS₂
• 分子量: 235.4
• InChiKey: MPMSDAJIMMQXKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  82.5
• 氢给体数：
  1
• 氢受体数：
  3

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。
• ABUSE-DETERRENT PHARMACEUTICAL COMPOSITION
  申请人：G.L. Pharma GmbH

  公开号：EP3210596A1

  公开（公告）日：2017-08-30

  Disclosed is an abuse-deterrent pharmaceutical composition comprising a drug with an enzyme-reactive functional group, wherein the drug has an abuse potential, and an enzyme capable of reacting with the enzyme-reactive functional group (a drug-processing enzyme), wherein the drug with the enzyme-reactive functional group is contained in the pharmaceutical composition in a storage stable, enzyme-reactive state and under conditions wherein no enzymatic activity acts on the drug.

  本发明公开了一种抑制滥用的药物组合物，该药物组合物包含具有酶反应官能团的药物（其中该药物具有滥用潜力）和能够与酶反应官能团发生反应的酶（药物加工酶），其中具有酶反应官能团的药物以贮存稳定、酶反应状态包含在药物组合物中，并且在没有酶活性作用于该药物的条件下。
• Compositions and methods for reducing overdose
  申请人：Odidi Isa

  公开号：US10293046B2

  公开（公告）日：2019-05-21

  Drug delivery formulations, uses thereof and methods of making same are provided in order to reduce the potential for abuse, misuse or improper administration of an addictive substance or any active substance and to prevent, reduce, inhibit, or delay purposeful or accidental overdose of an active substance by ingesting too many dosage forms at once, for example.

  提供给药制剂、其用途和制作方法是为了减少滥用、误用或不当使用成瘾物质或任何活性物质的可能性，并防止、减少、抑制或延缓因一次摄入过多剂型的活性物质而有目的或意外地过量使用。
• Pharmaceutical composition having reduced abuse potential
  申请人：INTELLIPHARMACEUTICS CORP.

  公开号：US10632205B2

  公开（公告）日：2020-04-28

  A pharmaceutical paste composition comprising an active ingredient such as an addictive substance, a controlled release agent, and a pharmaceutically suitable aqueous or non-aqueous carrier. The composition may comprise one or more of a clay, or an oily, waxy, or fatty substance. The composition may be filled into a capsule or other dispensing device. The composition may reduce dose dumping of an active ingredient. Methods of making and using the composition are also described.

  一种药用膏状组合物，包含一种活性成分（如成瘾物质）、一种控释剂和一种药用水性或非水性载体。该组合物可包含一种或多种粘土，或油性、蜡性或脂肪性物质。组合物可装入胶囊或其他配药装置中。该组合物可以减少活性成分的剂量倾倒。此外，还介绍了该组合物的制造和使用方法。
• Abuse and alcohol resistant drug composition
  申请人：Odidi Isa

  公开号：US10960077B2

  公开（公告）日：2021-03-30

  A liquid or semi-solid matrix or magma or paste which is non-newtonian, thixotropic and pseudoplastic and composed of one or more controlled release agent, and/or one or more clays such as bentonite and/or one or more fillers in a non aqueous vehicle, and optionally materials selected from disintegrants, humectants, surfactants and stabilizers. The composition and physicochemical properties makes it harder or prevents dose dumping of narcotic analgesics in the presence of alcohol and harder to abuse opiod agonists or narcotic analgesics and discourages drug abuse via crushing, milling or grinding the dosage form to powder or heating the dosage form to vapour and snorting or inhalation by the nasal route or dissolving to abuse via the parenteral route.

  一种液态或半固态基质或岩浆或糊状物，具有非牛顿性、触变性和假塑性，由一种或多种控释剂和/或一种或多种粘土（如膨润土）和/或一种或多种非水性载体中的填料，以及从崩解剂、保湿剂、表面活性剂和稳定剂中选择的材料组成。这种成分和理化特性使麻醉性镇痛剂在酒精存在的情况下更难或更难防止剂量倾倒，也更难滥用阿片类受体激动剂或麻醉性镇痛剂，并阻止通过将剂型压碎、碾碎或研磨成粉末，或将剂型加热成蒸汽并吸入，或通过鼻腔途径吸入，或通过肠外途径溶解滥用药物。