Dexamethasone linoleate | 39026-39-6

• 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
• 英文名称: Dexamethasone linoleate
• 英文别名: [2-[(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] (9Z,12Z)-octadeca-9,12-dienoate
• CAS: 39026-39-6
• 化学式: C₄₀H₅₉FO₆
• 分子量: 654.9
• InChiKey: JCTITVWENFVLBV-SIVNAAEPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  9.3
• 重原子数：
  47
• 可旋转键数：
  18
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.72
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Liposomes containing steroid esters
  申请人：Aktiebolaget Draco

  公开号：EP0170642A2

  公开（公告）日：1986-02-05

  Pharmaceutical composition for administration primarily to the respiratory tract when treating and controlling anti-inflammatory conditions comprising liposomes in combination with a compound of the formula wherein Q is and R1 is a saturated or unsaturated, straight or branched alkyl group with 11-19 carbon atoms and R is H, -COCH3, -COC2H5, -CO(CH2)2CH3 or -CO(CH2)3CH3. The invention also refers to the compounds of the formula I per se processes for preparation of these compounds and to a method for the treatment of inflammatory conditions.

  在治疗和控制抗炎病症时主要用于呼吸道给药的药物组合物，该组合物由脂质体与一种式化合物结合而成 其中 Q 是 和 R1 是具有 11-19 个碳原子的饱和或不饱和、直链或支链烷基，R 是 H、-COCH3、-COC2H5、-CO(CH2)2CH3 或 -CO( )3CH3。 本发明还涉及式 I 化合物本身的制备工艺以及治疗炎症的方法。
• Use of combinations comprising a corticosteroid and a pyrimidopyrimidine in the treatment of inflammatory diseases
  申请人：Combinatorx, Incorporated

  公开号：EP2070550A1

  公开（公告）日：2009-06-17

  The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering to the patient a tetra-substituted pyrimidopyrimidine, either alone or in combination with one or more additional agents. The invention also features a composition containing a tetra-substituted pyrimidopyrimidine in combination with one or more additional agents.

  本发明的特点是通过向患者单独或与一种或多种附加制剂联合使用四取代嘧啶嘧啶，治疗被诊断患有或有可能患上免疫炎症性疾病的患者。本发明的另一个特点是含有四取代嘧啶嘧啶的组合物与一种或多种附加制剂的组合物。
• Methods, compositions, and kits for the treatment of ophthalmic disorders
  申请人：CombinatoRx, Inc.

  公开号：EP2218442A1

  公开（公告）日：2010-08-18

  The invention features methods, compositions and kits comprising a corticosteroid and a non-steroidal immunophilin-dependent immunosuppressant for treating an ophthalmic disorder in a patient, wherein at least one of said corticosteroid and said non-steroidal immunophilin-dependent immunosuppressant is present at a low concentration, in particular wherein said corticosteroid is prednisolone acetate and said non-steroidal immunophilin-dependent immunosuppressant is cyclosporine A.

  本发明的特征是包含皮质类固醇和非类固醇免疫嗜血素依赖性免疫抑制剂的方法、组合物和试剂盒，用于治疗患者的眼科疾病、其中，所述皮质类固醇和所述非类固醇免疫嗜血素依赖性免疫抑制剂中至少有一种以低浓度存在，特别是所述皮质类固醇为醋酸泼尼松龙，所述非类固醇免疫嗜血素依赖性免疫抑制剂为环孢素 A。
• POLYMORPHIC FORM OF FLUTICASONE PROPIONATE
  申请人：Nicox Ophthalmics, Inc.

  公开号：EP3517541A1

  公开（公告）日：2019-07-31

  The present invention provided nanocrystals of fluticasone propionate having an X-ray powder diffraction pattern including peaks at about 7.8, 15.7, 20.8, 23.7, 24.5, and 32.5 degrees 2θ further including peaks at about 9.9, 13.0, 14.6, 16.0, 16.9, 18.1, and 34.3 degrees 2θ, characterized in that :the nanocrystals are nanoplates having the [001] crystallographic axis substantially normal to the surfaces that define the thickness of the nanoplates,wherein said nanoplates have an average size between 100 and 1000 nm.

  本发明提供了丙酸氟替卡松的纳米晶体，其 X 射线粉末衍射图谱包括约 7.8、15.7、20.8、23.7、24.5 和 32.5 度 2θ处的峰，还包括约 9.9、13.0、14.6、16.0、16.9、18.1 和 34.3 度 2θ处的峰。3 度 2θ，其特征在于：纳米晶体是纳米板，其[001]结晶轴基本上与确定纳米板厚度的表面法线，其中所述纳米板的平均尺寸介于 100 和 1000 纳米之间。
• PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF
  申请人：Nicox Ophthalmics, Inc.

  公开号：EP3741772A1

  公开（公告）日：2020-11-25

  The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

  本发明进一步提供了制备疏水性治疗剂（如氟替卡松或曲安西龙）纳米晶体的方法、其药物组合物（如局部或鼻内组合物）以及治疗和/或预防诸如睑缘炎、睑板腺功能障碍或皮肤炎症或呼吸系统疾病（如哮喘）等疾病的症状和/或体征的方法。