all-trans retinoic acid pinacyl ester | 730961-06-5

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: all-trans retinoic acid pinacyl ester
• 英文别名: (3-hydroxy-2,3-dimethylbutan-2-yl) (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoate
• CAS: 730961-06-5
• 化学式: C₂₆H₄₀O₃
• 分子量: 400.602
• InChiKey: JSZJPPNMQNYRGY-VVYUTNTRSA-N

物化性质

• 沸点：
  520.1±33.0 °C(Predicted)
• 密度：
  0.994±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  29
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  频哪醇 、 维A酸 在 草酰氯 、 吡啶 作用下， 以 乙醚 为溶剂， 反应 16.5h， 以47%的产率得到all-trans retinoic acid pinacyl ester
  参考文献：
  名称：

  [EN] METHOD OF REDUCING TOXICITY OF RETINOIDS
  [FR] PROCEDE DE REDUCTION DE LA TOXICITE DE RETINOIDES

  摘要：

  公开号：

  WO2004065358A3

文献信息

• Compounds, compositions, kits and methods of use to topically treat acne and other skin conditions by administering a 19-nor containing vitamin D analog.
  申请人：Wisconsin Alumni Research Foundation

  公开号：EP2591769A2

  公开（公告）日：2013-05-15

  Topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3'hydroxypropyl-1',2'-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and/or a solute thereof.

  外用药物组合物、试剂盒及其治疗方法，用于治疗各种皮肤疾病，包括痤疮、牛皮癣、鱼鳞病、光老化、光损伤皮肤和皮肤癌。作为活性药物成分的典型维生素 D 类似物包括 19-去甲-26,27-二亚甲基-20(S)-2-亚甲基-1α,25-二羟基维生素 D3、2-亚甲基-1α,25-二羟基-(17E)-17(20)-去甲-19-去甲维生素 D3、2-亚甲基-(20R,25S)-19,26-二去甲-1α,25-二羟基维生素 D3、2-亚甲基-23、2-亚甲基-(20R,25S)-19,26-二去甲-1α,25-二羟基维生素 D3、2-亚甲基-23,23-二氟-1α-羟基-19-去甲-双去甲孕钙化醇、（2-(3'羟丙基-1'、2'-亚烯）-19,23,24-三去甲-(20S)-1α-羟基维生素 D3、其立体异构体、其口服组合物中的原药、其盐和/或其溶质。
• A GROUP OF CHIMERIC ANTIGEN RECEPTORS (CARS)
  申请人：St. Anna Kinderkrebsforschung

  公开号：EP3632461A1

  公开（公告）日：2020-04-08

  Disclosed is a group of chimeric antigen receptors (CARs) consisting of two, three or four CAR molecules, wherein the members of the group of CARs can be different or identical in their amino acid sequences to one another, and wherein each of the CAR molecules of the group comprise at least a transmembrane domain and an ectodomain comprising either an antigen binding moiety or a binding site to which another polypeptide is able to bind, wherein the another polypeptide comprises an antigen binding moiety; wherein each CAR molecule of the group comprises at least one dimerization domain, wherein this dimerization of a pair of dimerization domains is either induced by a regulating molecule and optionally reduced by another regulating molecule, or occurs in the absence of a regulating molecule and is reduced by a regulating molecule, and wherein the ectodomain of each CAR molecule of the group in its prevalent conformation is free of cysteine amino acid moieties which are able to form intermolecular disulphide bonds with other CAR molecules of the group, respectively, and wherein the antigen binding moieties of the CAR molecules of the group and of the other polypeptides being able to bind to the CAR molecules of the group are either specific for one target antigen or for a non-covalent or a covalent complex of different target antigens.

  公开了一组嵌合抗原受体（CAR），由两个、三个或四个 CAR 分子组成、 其中，该组 CAR 成员的氨基酸序列可以彼此不同或相同，以及 其中该组的每个 CAR 分子至少包括一个跨膜结构域和一个外结构域，该结构域包括抗原结合分子或另一种多肽可与之结合的结合位点，其中另一种多肽包括抗原结合分子； 其中该组的每个 CAR 分子包括至少一个二聚化结构域，一对二聚化结构域的这种二聚化或者由调节分子诱导并可选地被另一个调节分子降低，或者在没有调节分子的情况下发生并被调节分子降低，以及 其中，该组每个 CAR 分子的外结构域在其盛行构象中不含半胱氨酸氨基酸分子，而半胱氨酸氨基酸分子可分别与该组其他 CAR 分子形成分子间二硫键，以及 其中，该组 CAR 分子和能与该组 CAR 分子结合的其他多肽的抗原结合分子对一种靶抗原或不同靶抗原的非共价或共价复合物具有特异性。
• Conditionally active heterodimeric polypeptides and methods of use thereof
  申请人：The Regents of the University of California

  公开号：US11136562B2

  公开（公告）日：2021-10-05

  The present disclosure provides conditionally active, heterodimeric polypeptides. The conditionally active, heterodimeric polypeptides are active in the presence of a dimerizing agent that induces dimerization of the polypeptides of the heterodimer. A conditionally active, heterodimeric polypeptide of the present disclosure is useful in a variety of research and treatment methods, which are also provided.

  本公开提供了具有条件活性的异源二聚体多肽。有条件活性的异源二聚体多肽在二聚化剂存在时具有活性，二聚化剂可诱导异源二聚体多肽的二聚化。本公开的具有条件活性的异源二聚体多肽可用于多种研究和治疗方法，这些方法也已提供。
• Modified retinoid compounds and their uses
  申请人：——

  公开号：US20040167215A1

  公开（公告）日：2004-08-26

  A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.

  本文描述了一种最大限度地降低或减少具有游离羧基的维甲酸毒性的方法，以及由此产生的改性维甲酸。该方法包括用高度立体受阻的化合物（最好是仲醇或叔醇）酯化维甲酸的羧基。由此产生的维甲酸酯的毒性比起始或母体维甲酸低得多。这种工艺可提供毒性更低的维甲酸酯类似物，因此口服给药时副作用最小，治疗窗口期更长。经修饰的维甲酸化合物可用于治疗和预防维甲酸化合物已被证明有效的所有疾病。
• Method of reducing toxicity of retinoids
  申请人：DeLuca F. Hector

  公开号：US20050085539A1

  公开（公告）日：2005-04-21

  A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group is described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably an alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window.

  本文描述了一种将具有游离羧基的维甲酸的毒性降至最低或减少的方法。该方法包括用一种高度立体受阻的化合物（最好是醇）酯化维甲酸的羧基。由此产生的维甲酸酯的毒性远远低于起始或母体维甲酸。这种工艺可提供毒性更低的维甲酸酯类似物，因此口服给药时副作用最小，治疗窗口期更长。