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desonide sodium phosphate

中文名称
——
中文别名
——
英文名称
desonide sodium phosphate
英文别名
Locapred°;Tridesilon;Prenacid;desonate;desonide;Desowen;verdeso;11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
desonide sodium phosphate化学式
CAS
——
化学式
C24H32O6
mdl
——
分子量
416.514
InChiKey
WBGKWQHBNHJJPZ-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    2.7
  • 重原子数:
    30
  • 可旋转键数:
    2
  • 环数:
    5.0
  • sp3杂化的碳原子比例:
    0.75
  • 拓扑面积:
    93.1
  • 氢给体数:
    2
  • 氢受体数:
    6

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用总结:地索奈德在母乳喂养期间尚未进行研究。由于只有大量应用最强效的皮质类固醇可能会对母亲产生系统性影响,因此短期应用局部皮质类固醇不太可能通过进入母乳而对哺乳婴儿构成风险。然而,尽量使用最弱效的药物,并尽可能在最小的皮肤区域使用是谨慎的做法。特别是要确保婴儿的皮肤不直接接触已涂抹药物的区域。应仅在溶性乳膏或凝胶产品上涂抹在乳房上,因为软膏可能会使婴儿通过舔食接触到高平的矿物石蜡。地索奈德乳膏或泡沫可用于乳头。如果局部皮质类固醇应用于乳房或乳头区域,应在哺乳前彻底擦除。 ◉ 对哺乳婴儿的影响:将具有相对较高盐皮质激素活性的皮质类固醇异氟泼尼松醋酸酯)涂在母亲的乳头上,导致她的2个月大的哺乳婴儿出现QT间期延长、库欣样外观、严重高血压、生长减缓和电解质异常。这位母亲从婴儿出生时起就因乳头疼痛而使用该乳膏。 ◉ 对泌乳和母乳的影响:截至修订日期,未找到相关已发布信息。
◉ Summary of Use during Lactation:Desonide has not been studied during breastfeeding. Since only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking. Desonide cream or foam are acceptable to use on the nipple. Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area. ◉ Effects in Breastfed Infants:Topical application of a corticosteroid with relatively high mineralocorticoid activity (isofluprednone acetate) to the mother's nipples resulted in prolonged QT interval, cushingoid appearance, severe hypertension, decreased growth and electrolyte abnormalities in her 2-month-old breastfed infant. The mother had used the cream since birth for painful nipples. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
来源:Drugs and Lactation Database (LactMed)

反应信息

  • 作为产物:
    描述:
    12-Bromo-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one 在 偶氮二异丁腈次磷酸三乙胺 作用下, 以 异丙醇 为溶剂, 以75.2%的产率得到desonide sodium phosphate
    参考文献:
    名称:
    9-卤代甾体化合物的脱卤方法及应用
    摘要:
    本发明提供了一种9‑卤代甾体化合物的脱卤方法及应用,涉及化学合成技术领域。9‑卤代甾体化合物的脱卤方法,包括如下步骤:化合物I与氢供体和偶氮类自由基引发剂反应,得到9‑卤代甾体化合物的9位脱卤产物化合物II。本发明提供的9‑卤代甾体化合物的脱卤方法,氢供体采用次磷酸及次磷酸盐、甲酸及甲酸盐、有机硅氢化物、肼类化合物或环己烯中的一种或几种的组合,引发剂采用偶氮类自由基引发剂,反应中未使用铬、二价铬盐、三价铬盐或氢化三丁基锡等毒性较大,对环境造成严重污染的试剂,绿色环保,合成工艺简便易行,提高了生产适用性。
    公开号:
    CN112142813A
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文献信息

  • Oligomer-Corticosteroid Conjugates
    申请人:Zhang Wen
    公开号:US20100286107A1
    公开(公告)日:2010-11-11
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
  • OLIGOMER-CORTICOSTEROID CONJUGATES
    申请人:NAKTAR THERAPEUTICS
    公开号:US20140309398A1
    公开(公告)日:2014-10-16
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits different properties compared to the properties of the corticosteroid not attached to the water-soluble oligomer.
  • US8796248B2
    申请人:——
    公开号:US8796248B2
    公开(公告)日:2014-08-05
  • [EN] OLIGOMER-CORTICOSTEROID CONJUGATES<br/>[FR] CONJUGUÉS D'OLIGOMÈRES ET CORTICOSTÉROÏDES
    申请人:NEKTAR THERAPEUTICS AL CORP
    公开号:WO2009045539A2
    公开(公告)日:2009-04-09
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
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