夹次苷 | 1182-87-2

• 物质功能分类: 生物化工 - 中草药成分
• 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: 夹次苷
• 中文别名: 黄夹次苷
• 英文名称: peruvoside
• 英文别名: (3S,5R,8R,9S,10R,13R,14S,17R)-3-[(2R,3S,4R,5S,6S)-3,5-dihydroxy-4-methoxy-6-methyloxan-2-yl]oxy-14-hydroxy-13-methyl-17-(5-oxo-2H-furan-3-yl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-10-carbaldehyde
• CAS: 1182-87-2
• 化学式: C₃₀H₄₄O₉
• 分子量: 548.674
• InChiKey: PMTSPAGBAFCORP-HBUONDEYSA-N

物化性质

• 熔点：
  161-164°C
• 比旋光度：
  D22 -71.7° (c = 1.54 in methanol)
• 沸点：
  540.83°C (rough estimate)
• 密度：
  1.1277 (rough estimate)
• 溶解度：
  可溶于氯仿（少许）、DMSO（少许）、甲醇（少许）
• 碰撞截面：
  239.4 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  39
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.87
• 拓扑面积：
  132
• 氢给体数：
  3
• 氢受体数：
  9

安全信息

• 危险品标志：
  T
• 安全说明：
  S36/37/39,S45
• 危险类别码：
  R23/24/25
• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  夹次苷 在 氢氧化钾 作用下， 生成 (20S,21S)-14,21-epoxy-19-oxo-3β-α-L-thevetopyranosyloxy-5β,14β-cardanolide
  参考文献：
  名称：

  Rangaswami; Rao, Journal of Scientific & Industrial Research, 1958, vol. 17 B, p. 331

  摘要：

  DOI：
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 strophanthobiose-substance 作用下， 生成 夹次苷
  参考文献：
  名称：

  Cerberosid（Thevetin B），Thevetin A和Peruvosid的组成。糖苷和糖苷配基，第213部分

  摘要：

  描述了通过分配色谱法将粗制的维汀类药物分离为纯成分小ber苷（维汀B）和维汀A的过程。cerberoside的构成我从转换与真菌淀粉酶或来自种子发酵一个制备thevebioside和neriifolin（V）如下Cerbera odollam。芥子油苷酶A（III）通过频闪霉素酶或上述来自Cerbera odollam的发酵制剂的作用被转化为普鲁佛苷（VIII）。后者代表血管生成素的α-L-vevetoside，通过与1，3-丙二酚反应生成环状硫代缩酮VII，然后通过RANEY镍催化脱硫将其转化为neriifolin（V）。

  DOI：

  10.1002/hlca.19600430306

文献信息

• COMPOSITIONS AND METHODS FOR ENHANCING CELLULAR UPTAKE AND INTRACELLULAR DELIVERY OF LIPID PARTICLES
  申请人：Lin Paulo J.C.

  公开号：US20120264810A1

  公开（公告）日：2012-10-18

  Compositions, methods and compounds useful for enhancing the uptake of a lipid particle b\ a cell are described In particular embodiments, the methods of the invention include contacting a cell with a lipid particle and a compound that binds a Na+/K+ ATPase to enhance uptake of the lipid particle b\ the cell Related compositions useful in practicing methods include lipid particles comprising a conjugated compound that enhances uptake of the lipid particles b\ the cell The methods and compositions are useful in delivering a therapeutic agent to a cell, e g for the treatment of a disease or disorder in a subject

  描述了用于增强细胞对脂质粒的摄取的组成物、方法和化合物。在特定的实施例中，发明的方法包括将细胞与脂质粒和一种与Na+/K+ ATPase结合的化合物接触，以增强细胞对脂质粒的摄取。在实践方法中使用的相关组成物包括包含一种共轭化合物的脂质粒，该共轭化合物增强细胞对脂质粒的摄取。这些方法和组成物可用于将治疗剂递送到细胞中，例如用于治疗主体中的疾病或失调。
• [EN] PYRAZOLO [4, 3-D] PYRIMIDINES USEFUL AS KINASE INHIBITORS<br/>[FR] PYRAZOLO[4,3-D]PYRIMIDINES UTILES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143144A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
• [EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143143A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
• Topical and oral formulations of cardiac glycosides for treating skin diseases
  申请人：Streeper Robert

  公开号：US20060205679A1

  公开（公告）日：2006-09-14

  The present invention provides method, preparation and use of a variety of pharmaceutical compositions containing at least one digitalis glycoside such as oleandrin, odoroside-A, neriifolin, proscillaridin-A, methyl-proscillaridin-A, digitoxin, digoxin alone or at least one digitalis glycoside complexed with cyclodextrins. In another aspect, the present invention provides an effective method to treat diseases in mammals. In yet another aspect, the present invention provides an effective method for treating skin diseases in a human or non-human animal.

  本发明提供了一种方法、制备和使用多种含有至少一种毛地黄苷类药物成分的药物组合物，例如奥利安定、奥多罗苷A、内里福林、普罗斯西拉里丁A、甲基普罗斯西拉里丁A、地高辛、地高辛或至少一种毛地黄苷类与环糊精络合的药物。另一方面，本发明提供了一种有效的方法来治疗哺乳动物的疾病。另一方面，本发明提供了一种有效的方法来治疗人类或非人类动物的皮肤疾病。
• CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS FOR PROLONGED EFFECT
  申请人：Hemmingsen Pernille Hoyrup

  公开号：US20100239667A1

  公开（公告）日：2010-09-23

  Layered pharmaceutical composition suitable for oral use in the treatment of diseases where absorption takes place over a large part of the gastrointestinal tract. The composition comprising A) a solid inner layer comprising i) an active substance, and ii) one or more disintegrants/exploding agents, one of more effervescent agents or a mixture thereof. the solid inner layer being sandwiched between two outer layers B1) and B2), each outer layer comprising iii) a substantially water soluble and/or crystalline polymer or a mixture of substantially water soluble and/or crystalline polymers, the polymer being a polyglycol in the form of one of a) a homopolymer having a MW of at least about 100,000 daltons, and b) a copolymer having a MW of at least about 2,000 daltons, or a mixture thereof, and iv) an active substance, which is the same as in said solid inner layer A), and layer A being different from layer B, the layered composition being coated with a coating C) that has at least one opening exposing at least one surface of said outer layer, the coating being substantially insoluble in and impermeable to fluids and comprising a polymer, and the composition having a cylindrical form optionally with one or more tapered ends, wherein the ratio between the surface area of one end surface of the cylinder and the length of the cylinder is in a range of from 0.02 to 45 mm.

  分层制药组合物，适用于口服治疗吸收发生在胃肠道大部分的疾病。该组合物包括A) 一个固体内层，其中包括i) 一种活性物质，和ii) 一种或多种分散剂/爆炸剂，一种或多种泡腾剂或其混合物。该固体内层被夹在两个外层B1)和B2)之间，每个外层包括iii) 一种或多种水溶性和/或结晶聚合物，或者水溶性和/或结晶聚合物的混合物，聚合物为聚乙二醇，形式为a) 分子量至少为约100,000道尔顿的同聚物，和b) 分子量至少为约2,000道尔顿的共聚物，或其混合物，和iv) 一种活性物质，其与所述固体内层A)中的活性物质相同，且层A与层B不同，该分层组合物被涂覆有一种涂层C)，该涂层具有至少一个开口，暴露出至少一个外层的表面，该涂层在液体中具有相当的不溶性和不透性，包括一种聚合物，该组合物具有圆柱形状，可选地具有一个或多个锥形端部，其中圆柱体的一个端面的表面积与圆柱体的长度之比在0.02至45毫米的范围内。