Cholesterin

• 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: Cholesterin
• 英文别名: cholesterol；(3S,10R,13R)-10,13-dimethyl-17-(6-methylheptan-2-yl)-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
• 化学式: C₂₇H₄₆O
• 分子量: 386.662
• InChiKey: HVYWMOMLDIMFJA-XGKKJYDTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.7
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  Cholesterin 在 4-二甲氨基吡啶 、 水 、 溶剂黄146 、 N,N'-二环己基碳二亚胺 、 锌 作用下， 以 四氢呋喃 、 苯 为溶剂， 反应 6.5h， 生成 5-cholesten-3β-ol 3-(3-carboxypropanoate)
  参考文献：
  名称：

  New preparation of steroidal 3-hemisuccinates

  摘要：

  3-羟基琥珀酸酯（3-(3-羧基丙酸酯)) XI-XV，源自胆固醇（I），(20R)-3β-羟基-21-去甲胆甾-5,22-二烯-24 20-酮（II），雌二醇（III），(20E)-21-甲氧羰基-3β-羟基孕烯-5,20-二烯（IV）和地高辛（V），通过醇类I-V和三氯乙醇（3-[4-(2,2,2-三氯乙氧基)-4-氧代丁酸酯] VI-X）的混合琥珀酸酯制备而成。在吡啶中用琥珀酸酐对II和IV进行常规酰化失败。

  DOI：

  10.1135/cccc19840306

文献信息

• Process for oxidation of steroidal compounds having allylic groups
  申请人：Merck & Co., Inc.

  公开号：US06369247B1

  公开（公告）日：2002-04-09

  The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.

  这项即时发明涉及一种氧化含有烯丙基团的化合物的过程，即那些含有烯丙基氢或烯丙醇基团的化合物，使用基于钌的催化剂在过氧化氢的存在下将其氧化为相应的烯酮。特别地，Δ-5类固醇烯烃可以被氧化为相应的Δ-5-7酮烯烃。
• RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (SINA)
  申请人：SIRNA THERAPEUTICS, INC.

  公开号：US20160076034A1

  公开（公告）日：2016-03-17

  The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of HBV gene expression and/or activity, and/or modulate a HBV gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against HBV gene expression.

  本发明涉及化合物、组合物和方法，用于研究、诊断和治疗对HBV基因表达和/或活性调控有反应的特征、疾病和病况，以及/或调节HBV基因表达途径。具体地，本发明涉及包括小核酸分子在内的双链核酸分子，如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）和短发夹RNA（shRNA）分子，这些分子能够介导或介导RNA干扰（RNAi）对抗HBV基因表达。
• LIPID NANOPARTICLE BASED COMPOSITIONS AND METHODS FOR THE DELIVERY OF BIOLOGICALLY ACTIVE MOLECULES
  申请人：Chen Tongqian

  公开号：US20080188675A1

  公开（公告）日：2008-08-07

  The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

  本发明涉及新型阳离子脂质体、转染剂、微粒、纳米粒子和短干扰核酸（siNA）分子。本发明还涉及用于研究、诊断和治疗对基因表达和/或活性调节有反应的特征、疾病和状况的组合物和使用方法。具体而言，本发明涉及新型阳离子脂质体、微粒、纳米粒子和转染剂，它们能有效地转染或传递生物活性分子，例如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶性核酸、反义核酸、三股形成寡核苷酸、2,5-A嵌合体、dsRNA、等位酶、适配体、诱饵和类似物以及小核酸分子，例如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）和短发夹RNA（shRNA）分子，传递到相关的细胞和/或组织中，例如在主体或生物体中。这些新型阳离子脂质体、微粒、纳米粒子和转染剂在提供组合物以预防、抑制或治疗细胞、主体或生物体的疾病、状况或特征方面是有用的。本文所描述的组合物通常被称为配制的分子组合物（FMC）或脂质纳米粒子（LNP）。
• Inhibitors of caspases
  申请人：Wannamaker Marion W.

  公开号：US20090048226A1

  公开（公告）日：2009-02-19

  The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

  本发明涉及一类新型化合物，它们是caspase抑制剂，特别是白细胞介素-1β转化酶（“ICE”）抑制剂。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制caspase活性，并因此可以作为对白细胞介素-1（“IL-1”）、凋亡、干扰素-γ诱导因子（IGIF）或干扰素-γ（“IFN-γ”）介导的疾病，包括炎症性疾病、自身免疫性疾病、破坏性骨疾病、增生性疾病、传染性疾病和退行性疾病的药剂。本发明还涉及抑制caspase活性、减少IGIF生成和IFN-γ生成的方法以及使用本发明的化合物和组合物治疗白细胞介素-1、凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。
• Lipid Nanoparticle Based Compositions and Methods for the Delivery of Biologically Active Molecules
  申请人：Chen Tongqian

  公开号：US20090048197A1

  公开（公告）日：2009-02-19

  The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), short hairpin RNA (shRNA), and RNAi inhibitor molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).

  本发明涉及新型阳离子脂质、转染剂、微粒、纳米粒子和短干扰核酸（siNA）分子。本发明还涉及组合物和使用方法，用于研究、诊断和治疗对基因表达和/或活性调节有反应的个体或生物的特征、疾病和状况。具体而言，本发明涉及新型阳离子脂质、微粒、纳米粒子和转染剂，可以有效地转染或传递生物活性分子，如抗体（例如单克隆、嵌合、人源化等）、胆固醇、激素、抗病毒药物、肽、蛋白质、化学治疗药物、小分子、维生素、辅因子、核苷、核苷酸、寡核苷酸、酶性核酸、反义核酸、三链体寡核苷酸、2,5-A嵌合体、dsRNA、异构酶、aptamers、诱饵和其类似物，以及小的核酸分子，如短干扰核酸（siNA）、短干扰RNA（siRNA）、双链RNA（dsRNA）、微RNA（miRNA）、短发夹RNA（shRNA）和RNAi抑制分子，传递到相关的细胞和/或组织中，例如在个体或生物中。这种新型阳离子脂质、微粒、纳米粒子和转染剂在提供组合物以预防、抑制或治疗细胞、个体或生物的疾病、状况或特征方面是有用的。本文所描述的组合物通常称为配方分子组合物（FMC）或脂质纳米粒子（LNP）。