Desisobutyryl-ciclesonide

• 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: Desisobutyryl-ciclesonide
• 英文别名: (1S,2S,4S,6R,8S,9S,11S,12S,13R)-6-cyclohexyl-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
• 化学式: C₂₈H₃₈O₆
• 分子量: 470.6
• InChiKey: OXPLANUPKBHPMS-FYSAVPLMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  34
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  93.1
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Crystalline Ciclesonide Methanol Solvate Form C
  申请人：Cipla Limited

  公开号：EP2392584A1

  公开（公告）日：2011-12-07

  The present invention relates to crystalline ciclesonide methanol solvate Form C, processes for its preparation, its use in the synthesis of crystalline ciclesonide Form A and its use in medicine.

  本发明涉及结晶环索地酮甲醇溶剂 Form C，其制备方法，其在合成结晶环索地酮 Form A 中的应用以及其在医学上的应用。
• PROCESSES FOR THE PREPARATION OF CICLESONIDE AND ITS CRYSTAL MODIFICATION
  申请人：Phull Manjinder Singh

  公开号：US20100222572A1

  公开（公告）日：2010-09-02

  Improved processes for the synthesis of ciclesonide, chemically termed as [11β,16α(R)]-16,17-[(cyclohexylmethylene)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione and its crystal modification.

  改进的合成环索尼德的过程，化学术语为[11β,16α(R)]-16,17-[(环己基亚甲基)双（氧基）]-11-羟基-21-(2-甲基-1-氧代丙氧基)孕-1,4-二烯-3,20-二酮及其晶体修饰。
• [EN] PROCESS FOR R-EPIMER ENRICHMENT OF 16,17-ACETAL DERIVATIVES OF 21-ACYLOXY PREGAN-1,4-DIEN-11.BETA.,16.ALPHA.,17.ALPHA.-TRIOL-3,20-DIONE DERIVATIVES<br/>[FR] PROCEDE D'ENRICHISSEMENT EN R-EPIMERES DE DERIVES 16,17-ACETAL DE DERIVES DE 21-ACYLOXY PREGAN-1,4-DIEN-11-BETA.,16.ALPHA.,17.ALPHA.-TRIOL-3,20 DIONE
  申请人：BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH

  公开号：WO1998009982A1

  公开（公告）日：1998-03-12

  (EN) The invention describes a process for epimer enrichment of compounds of formula (I) where R11 and R2 are as defined in the description, by fractional crystallization.(FR) L'invention a pour objet un procédé pour l'enrichissement en épimère de composés de la formule (I), par cristallisation fractionnée. Dans cette formule, R1 et R2 sont tels que définis dans le descriptif.

  该发明描述了一种通过分数结晶对式(I)中R11和R2如描述中所定义的化合物进行对映异构体富集的过程。(式(I)如下) 同时，该发明还涉及了一种用于该过程的方法。
• [EN] PROCESS FOR THE PRODUCTION OF 16,17-[(CYCLOHEXYLMETHYLEN)BIS(OXY)]-11,21-DIHYDROXY-PREGNA-1,4-DIEN-3,20-DION OR ITS 21-ISOBUTYRAT BY TRANSKETALISATION<br/>[FR] PROCEDE DE PRODUCTION DU 16,17-[(CYCLOHEXYLMETHYLENE)BIS(OXY)]-11,21-DIHYDROXY-PREGNA-1,4-DIENE-3,20-DIOE OU SON 21-ISOBUTYRATE PAR TRANSCETALISATION
  申请人：BYK GULDEN LOMBERG CHEM FAB

  公开号：WO2002038584A1

  公开（公告）日：2002-05-16

  The invention relates to a process for the preparation of 16,17-[(cyclohexylmethylene)bis(oxy)]-11,21-dihydroxypregna-1,4-diene-3,20-dione[11β,16α(R)] and similar compounds, by reaction of an appropri-ate 16,17-ketal with cyclohexanealdehyde.

  本发明涉及一种制备16,17-[(环己基亚甲基)双(氧)]-11,21-双羟基孕-1,4-二烯-3,20-二酮[11β,16α(R)]及类似化合物的方法，通过将适当的16,17-环缩酮与环己醛反应制备。
• Substituted Phenylphosphates as Mutual Prodrugs of Steroids and ß-Agonists for the Treatment of Title Pulmonary Inflammation and Bronchoconstriction
  申请人：Baker William

  公开号：US20100209508A1

  公开（公告）日：2010-08-19

  A mutual prodrug of a corticosteroid and a substituted phenylphosphate (β-agonist derivative) for formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 μL) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract inflammation and bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5μ, produced by nebulization or by dry powder inhaler.

  本文描述了一种皮质类固醇和取代苯基磷酸酯（β-激动剂衍生物）的相互前药，用于制剂通过气溶胶化途径送达，以抑制肺部炎症和支气管收缩。该相互前药最好以小体积溶液（10-500μL）的形式制剂，溶于pH在5.0至7.0之间的四分之一的生理盐水中，通过雾化或干粉吸入器产生主要介于1至5μ之间的质量平均直径的气溶胶治疗呼吸道炎症和支气管收缩。