舒马他莫 | 69217-67-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 舒马他莫
• 中文别名: 4-乙酰氨基-N-乙酰基-dl-蛋氨酸苯酯
• 英文名称: N-acetyl-para-aminophenyl N'-acetyl-D,L-methionate
• 英文别名: sumacetamol；(4-acetamidophenyl) 2-acetamido-4-methylsulfanylbutanoate
• CAS: 69217-67-0
• 化学式: C₁₅H₂₀N₂O₄S
• 分子量: 324.401
• InChiKey: GDRGOYFISYGSHQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  22
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  对乙酰氨基酚 以 水 为溶剂， 生成 舒马他莫
  参考文献：
  名称：

  Analgesic N-acetyl-para-aminophenyl N'-acetylaminothioalkanoates

  摘要：

  N-乙酰基对氨基苯基N'-乙酰氨基硫代烷酸酯I是一种新的镇痛化合物，与N-乙酰对氨基苯酚相比，当过量使用时具有大大降低的肝毒性效果。它们是通过将N-乙酰氨基硫代烷酸IV与反应性有机氯化物V反应形成混合酸酐II，然后将后者与N-乙酰对氨基苯酚反应制备而成。混合酸酐II是新的有用中间体。或者，可以通过将酸IV与双-(4-硝基苯基)亚磺酸酯反应形成对硝基苯基N-乙酰氨基硫代烷酸酯VIII，还原后者为对氨基苯基N-乙酰氨基硫代烷酸酯VII，并对该产物进行乙酰化来制备衍生物I。酯类VII和VIII是新的有用中间体。这两种反应都可以通过S-阻断中间体进行，这也是新的。揭示了含有衍生物I的制药组合物，以及使用它们的镇痛方法。

  公开号：

  US04181719A1

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。
• HEPATOPROTECTANT ACETAMINOPHEN MUTUAL PRODRUGS
  申请人：Muhammad Naweed

  公开号：US20110263545A1

  公开（公告）日：2011-10-27

  The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.

  本发明提供了肝保护醋氨酚共价偶联物，其含有醋氨酚基团与第二基团共价结合，第二基团可能作为肝保护剂对抗醋氨酚肝毒性。此外，醋氨酚共价偶联物可能具有改善的水溶性，相对于醋氨酚的给药方式，更适合于静脉和其他剂型的使用。本发明还提供了使用肝保护醋氨酚共价偶联物治疗对醋氨酚具有反应的疾病或病况的方法（如发热、疼痛和缺血性损伤），以及套装和单元剂量。
• Processes for preparing tablets by a modified 'wet-granulation' technique
  申请人：Rogerson, Alan George

  公开号：EP0100168A2

  公开（公告）日：1984-02-08

  The invention relates to a process for preparing a wet granulate suitable for use in manufacturing tablets by compression and compaction thereof. The process comprises first forming an intimate mixture of particulate-solid materials including pharmacologically or like active matter and tabletting aids. Then one predetermines a quantity of granulating fluid needed to convert the entire particulate-solid mixture into a desired moist, coherent, non-pasty mass as known per se but homogenizes part only of the particulate-solid materials, separately from the remainder thereof, with a chosen amount of granulating fluid, that chosen amount being at least 90% by weight of the aforesaid predetermined quantity of granulating fluid, so as to form a substantially-homogeneous slurry wherein the percentage by weight of solids in the slurry, namely: Total Solids, i.e. both dissolved and undissolved x 100 Total Slurry, i.e. fluids plus total solids is at least about 25% w/w. Thereafter, the remaining part of the particulate-solid material is moistened in the manner of «wet-granulation» as known per se but with the thus-prepared slurry (and then as necessary with the balance of the granulating fluid, if any) so as thus to form the desired substantially-uniform, moist, coherent, non-pasty mass ready for granulation.

  本发明涉及一种通过压缩和压实制备适用于片剂生产的湿颗粒的工艺。 该工艺包括首先形成颗粒-固体材料的亲密混合物，包括药理或类似活性物质和制片助剂。然后，预先确定将整个颗粒-固体混合物转化为所需的湿润、连贯、无呕吐物的颗粒-固体混合物所需的造粒液量，但只将颗粒-固体材料的一部分与其余部分分开，用选定量的造粒液进行均质，该选定量至少为上述预定量造粒液重量的 90%，以形成基本均质的浆料，其中浆料中固体的重量百分比，即： 总固体量，即： 总固体量，即： 总固体量，即： 总固体量，即： 总固体量，即： 总固体量： 总固体，即溶解的和未溶解的 x 100 淤浆总量，即流体加固体总量 至少约为 25% w/w。然后，按照已知的 "湿法造粒 "方式，将颗粒-固体材料的剩余部分用这样制备的泥浆（必要时再用剩余的造粒液（如果有的话））润湿，从而形成所需的基本均匀、湿润、连贯、无粘性的团块，以备造粒。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。