可米松 | 35135-68-3

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 中文名称: 可米松
• 中文别名: (9R,11S,14S,16R,17R)-6,6,9-三氟-11,17-二羟基-17-(2-羟基乙酰基)-10,13,16-三甲基-8,11,12,14,15,16-六氢-7H-环戊二烯并[a]菲-3-酮
• 英文名称: Cormethasone
• 英文别名: (8S,9R,10S,11S,13S,14S,16R,17R)-6,6,9-trifluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-8,11,12,14,15,16-hexahydro-7H-cyclopenta[a]phenanthren-3-one
• CAS: 35135-68-3
• 化学式: C₂₂H₂₇F₃O₅
• 分子量: 428.4
• InChiKey: QVTPFMPYKMLGGK-QPZANWORSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  94.8
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• 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。
• 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。
• Rinse-off compositions and uses thereof for delivery of active agents
  申请人：CRESCITA THERAPEUTICS INC.

  公开号：US10945952B2

  公开（公告）日：2021-03-16

  The present application relates to a rinse-off composition comprising an oil phase and an aqueous surfactant matrix, wherein one or more active agents are dissolved in one or more non-polar, water-immiscible solvents, and the oil phase is dispersed in the aqueous surfactant matrix. The present application also relates to methods of delivering the active agent(s) to a subject in need thereof topically, for example to the skin, the hair, and scalp. The present application also relates to use of the rinse-off compositions to treat and/or prevent topical conditions such as dermatitis and psoriasis. In some embodiments, the rinse-off compositions of the present application are shampoo compositions.

  本申请涉及一种包含油相和水性表面活性剂基质的冲洗组合物，其中一种或多种活性剂溶解在一种或多种非极性、水不溶性溶剂中，油相分散在水性表面活性剂基质中。 本申请还涉及向有需要的受试者局部递送活性剂的方法，例如递送至皮肤、头发和头皮。 本申请还涉及使用冲洗组合物治疗和/或预防皮炎和牛皮癣等局部病症。 在某些实施方案中，本申请的冲洗组合物是洗发水组合物。
• [EN] LIPOSOMIC DRUG-DELIVERY VEHICLES<br/>[FR] VÉHICULES LIPOSOMAUX POUR L'ADMINISTRATION DE MÉDICAMENTS
  申请人：YEDA RES & DEV

  公开号：WO2018150429A9

  公开（公告）日：2018-09-13