2-hydroxy-4-[3-hydroxy-3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-1-propynyl]-benzoic acid | 170099-89-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 2-hydroxy-4-[3-hydroxy-3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-1-propynyl]-benzoic acid
• 英文别名: 8Ubu25xlc8；2-hydroxy-4-[3-hydroxy-3-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)prop-1-ynyl]benzoic acid
• CAS: 170099-89-5
• 化学式: C₂₄H₂₆O₄
• 分子量: 378.468
• InChiKey: HLSHNXLMUMGCSV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  77.8
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-hydroxy-4-[3-hydroxy-3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-1-propynyl]-benzoic acid 生成 2-hydroxy-4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-1-propynyl]benzoic acid
  参考文献：
  名称：

  Propynyl or dienyl biaromatic compounds

  摘要：

  这项发明涉及具有一般式（I）##STR1##的新型丙炔基或二烯基双芳香化合物，以及这些化合物在用于人类或兽医药物（特别用于皮肤病、风湿病、呼吸系统疾病、心血管疾病和眼科疾病）的制剂中的使用，或者在化妆品制剂中的使用。

  公开号：

  US06046220A1

文献信息

• ANHYDROUS PETROLEUM JELLY/ELASTOMER-FREE DEPIGMENTING COMPOSITIONS COMPRISING A SOLUBILIZED PHENOLIC COMPOUND AND A RETINOID
  申请人：Mallard Claire

  公开号：US20110152372A1

  公开（公告）日：2011-06-23

  Novel dermatological depigmentation compositions, especially for topical application, contain as pharmaceutical active agents a dissolved phenolic compound and a retinoid, formulated as anhydrous compositions free of petroleum jelly and free of elastomer. The present invention relates to a novel depigmenting composition especially for topical application, comprising as pharmaceutical active agents a dissolved phenolic derivative and a retinoid, in the form of an anhydrous composition free of petroleum jelly and free of elastomer, to the process for preparing it and to its use in dermatology.

  新型皮肤美白组合物，特别适用于局部应用，包含作为药用活性剂的溶解酚类化合物和维生素A酸衍生物，制成无石蜡和无弹性体的无水配方。本发明涉及一种新型美白组合物，特别适用于局部应用，包括作为药用活性剂的溶解酚类衍生物和维生素A酸衍生物，以无石蜡和无弹性体的无水配方形式存在，以及其制备过程和在皮肤科中的使用。
• Use of a RAR-gamma-specific agonist ligand for increasing the rate of apoptosis
  申请人：——

  公开号：US20030092758A1

  公开（公告）日：2003-05-15

  The present invention relates to the use of at least one RAR receptor agonist ligand, particularly 6-[3-(adamantan-1-yl)-4-(prop-2-ynyloxy)phenyl]naphthalene-2-carboxylic acid or 5-[(E)-3-oxo-3-(5,5,8,8-tetrahydronaphthalene-2-yl)propenyl]thiophene-2-carboxylic acid, to prepare a pharmaceutical composition for increasing the rate of apoptosis in at least one cell population in which apoptosis may be induced by activating RAR-&ggr; receptors. The composition is particularly useful for treating a disease or disorder related to an insufficient rate of apoptosis in at least one cell population in which apoptosis may be induced by activating RAR-&ggr; receptors. The invention further relates to the use of at least one RAR receptor agonist ligand, particularly 6-[3-(adamantan-1-yl)-4-(prop-2-ynyloxy)phenyl]naphthalene-2-carboxylic acid or 5-[(E)-3-oxo-3-(5,5,8,8-tetrahydronaphthalene-2-yl)propenyl]thiophene-2-carboxylic acid, as the active ingredient in a pharmaceutical or cosmetic composition and the use of such RAR agonist ligands to treat various disorders associated with apoptosis, differentiation, and proliferation. The compositions of the present invention may be used to prevent and/or control photo-induced or chronological aging of the skin.

  本发明涉及使用至少一种RAR受体激动剂配体，特别是6-[3-(孔雀石-1-基)-4-(丙-2-炔氧基)苯基]萘-2-羧酸或5-[(E)-3-氧代-3-(5,5,8,8-四氢萘-2-基)丙烯基]噻吩-2-羧酸，用于制备一种药物组合物，以增加至少一种细胞群体中凋亡速率，其中通过激活RAR-γ受体可以诱导凋亡。该组合物特别适用于治疗与至少一种细胞群体中凋亡速率不足相关的疾病或紊乱，其中通过激活RAR-γ受体可以诱导凋亡。该发明还涉及使用至少一种RAR受体激动剂配体，特别是6-[3-(孔雀石-1-基)-4-(丙-2-炔氧基)苯基]萘-2-羧酸或5-[(E)-3-氧代-3-(5,5,8,8-四氢萘-2-基)丙烯基]噻吩-2-羧酸，作为药用或化妆品组合物中的活性成分，以及使用这些RAR激动剂配体治疗与凋亡、分化和增殖相关的各种紊乱。本发明的组合物可用于预防和/或控制皮肤的光致老化或年代老化。
• Nouveaux composés propynyl bi-aromatiques, compositions pharmaceutiques et cosmétiques les contenant et utilisations
  申请人：CENTRE INTERNATIONAL DE RECHERCHES DERMATOLOGIQUES GALDERMA, ( CIRD GALDERMA)

  公开号：EP0661258A1

  公开（公告）日：1995-07-05

  L'invention concerne de nouveaux composés bi-aromatiques présentant un motif propynyl de formule générale (I) : ainsi que l'utilisation de ces derniers dans des compositions pharmaceutiques destinées à un usage en médecine humaine ou vétérinaire (affections dermatologiques, rhumatismales, respiratoires, cardiovasculaires et ophtalmologiques notamment), ou bien encore dans des compositions cosmétiques.

  本发明涉及具有通式(I)丙炔基单元的新型双芳香族化合物： 以及后者在人类或兽类医药（尤其是皮肤病、风湿病、呼吸系统疾病、心血管疾病和眼科疾病）或化妆品组合物中的用途。
• Lipid nanocapsules comprising a retinoid, nanodispersion and composition containing the same, process for preparing the same and use thereof in dermatology
  申请人：GALDERMA RESEARCH & DEVELOPMENT

  公开号：US10702604B2

  公开（公告）日：2020-07-07

  Lipid nanocapsules are described that include at least one irritating active ingredient, and more specifically a retinoid in solubilized form. Also described, are nanodispersions and pharmaceutical compositions including the same and methods of producing the same. The use of the pharmaceutical compositions in the treatment of dermatological pathologies is also described.

  所述脂质纳米胶囊包括至少一种刺激性活性成分，更具体地说是一种溶解形式的维甲酸。此外，还介绍了纳米分散体、包括纳米分散体的药物组合物以及生产纳米分散体的方法。还描述了药物组合物在皮肤病治疗中的用途。
• Lipid microcapsules preferably comprising a retinoid, and composition containing same, method for the production thereof, and use of same in dermatology
  申请人：GALDERMA RESEARCH & DEVELOPMENT

  公开号：US10772807B2

  公开（公告）日：2020-09-15

  Lipid microcapsules are described that can include at least one irritant active substance, more specifically a retinoid, in a soluble form. Also described, are pharmaceutical compositions comprising the same, and methods for the production thereof. A method of using the composition to treat dermatological pathologies is also described.

  所述脂质微胶囊可包括至少一种可溶形式的刺激性活性物质，更具体地说是一种视黄醇。此外，还描述了包含上述物质的药物组合物及其生产方法。还描述了使用该组合物治疗皮肤病的方法。