奴氯美酮 | 86017-21-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 奴氯美酮
• 中文别名: 核美酮
• 英文名称: 6-p-chlorobenzyl-5H-2,3,6,7-tetrahydro-5,7-dioxothiazolo[3,2-a]pyrimidine
• 英文别名: Nuclomedone；6-[(4-chlorophenyl)methyl]-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidine-5,7-dione
• CAS: 86017-21-2；75963-52-9
• 化学式: C₁₃H₁₁ClN₂O₂S
• 分子量: 294.762
• InChiKey: QSKVYHYMQQQAFS-UHFFFAOYSA-N

物化性质

• 沸点：
  438.7±37.0 °C(Predicted)
• 密度：
  1.54±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  75
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  奴氯美酮 生成 6-[(4-chlorophenyl)methyl]-7-ethoxy-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-5-one
  参考文献：
  名称：

  SAKAUTI, SEHJ;OBA, SAJO;YU, KEHN;OKAMURA, KEHMMEHJ

  摘要：

  DOI：
• 作为产物：
  描述：

  2-氨基-2-噻唑啉 生成 奴氯美酮
  参考文献：
  名称：

  OBA, TAKEO;BANNAI, KIYOSHI;TANAKA, TOSHIO;WATANABE, KENZO;NARUCHI, TATSUY+

  摘要：

  DOI：

文献信息

• Derivative of thiazolo[3,2-a]pyrimidine and a process for the
  申请人：Teijin Limited

  公开号：US04383996A1

  公开（公告）日：1983-05-17

  A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.

  一种由式（I）表示的噻唑并[3,2-a]嘧啶衍生物##STR1##（其中R表示苯基或苄基，其具有卤原子、较低烷基或较低烷氧基作为取代基，脂环基或芳基乙基基团），以及制备式（I）化合物的方法，包括通过加热使式（II）表示的化合物环化##STR2##（其中R的定义与式（I）情况下给出的相同，R'表示卤原子或较低烷氧基）。包含该化合物作为活性成分的药物对治疗类风湿性关节炎、肾炎等自身免疫疾病有用。
• 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。
• Nasally administrable compositions
  申请人：DOTT RESEARCH LABORATORY

  公开号：EP0681833A2

  公开（公告）日：1995-11-15

  A nasally administrable composition having a physiologically active substance dispersed homogeneously in and adsorbed homogeneously onto a unique carrier. The nasally administrable composition contains a physiologically effective amount of the physiologically active substance having a molecular weight of not more than 40,000, dispersed homogeneously in and adsorbed homogeneously onto physiologically acceptable powdery or crystalline polyvalence metal compound carrier. The metal compound carrier is selected from aluminum compound, calcium compound, magnesium compound, silicon compound, iron compound and zinc compound. The composition is nasally administrable in powdery form.

  一种可经鼻腔给药的组合物，其生理活性物质均匀地分散在一种独特的载体中并被均匀地吸附在载体上。鼻腔给药组合物含有生理有效量的生理活性物质，其分子量不超过 40 000，均匀地分散在生理上可接受的粉末状或结晶状多价金属化合物载体上。 金属化合物载体选自铝化合物、钙化合物、镁化合物、硅化合物、铁化合物和锌化合物。 组合物可以粉末状鼻腔给药。
• 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。