6-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-ylamino)naphthalene-2-carboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 6-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-ylamino)naphthalene-2-carboxylic acid
• 英文别名: 6-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphth-2-ylamino)naphthalene-2-carboxylic acid；6-[(5,5,8,8-Tetramethyl-6,7-dihydronaphthalen-2-yl)amino]naphthalene-2-carboxylic acid
• 化学式: C₂₅H₂₇NO₂
• 分子量: 373.495
• InChiKey: APVJFPPFKHOIOJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.4
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  三氟甲烷磺酸-6-溴-2-萘酯 在 palladium diacetate 、 四(三苯基膦)钯 1,3-双(二苯基膦)丙烷 、 potassium tert-butylate 作用下， 生成 6-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-ylamino)naphthalene-2-carboxylic acid
  参考文献：
  名称：

  Structural modifications of 6-naphthalene-2-carboxylate retinoids

  摘要：

  The keto linker of 2-naphthoate retinoid 1 has been found nonessential for RAR transactivation activity and can be replaced with heteroatoms such as S, O, N without significant reduction of the activity. On the other hand, substitutions on the aromatic rings of retinoids 1 and 2 resulted in analogs with reduced potentcy and RAR selectivity. Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/s0960-894x(96)00524-0

文献信息

• 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。
• PPAR receptor activator compounds for treating cutaneous disorders/afflictions
  申请人：——

  公开号：US20020049249A1

  公开（公告）日：2002-04-25

  Compounds of formula (I): 1 characteristically activators of receptors of PPAR type, are well suited for treating cutaneous disorders/afflictions, notably disorders of the barrier function of the skin, more particularly disorders of the secretion of epidermal lipids, photodermatoses or ulcers, and/or disorders of the metabolism of lipids.

  公式（I）的化合物：1是PPAR型受体的特征性激活剂，非常适合治疗皮肤疾病/痛苦，特别是皮肤屏障功能障碍，尤其是表皮脂质分泌障碍，光敏性皮肤病或溃疡，以及/或脂质代谢障碍。
• Methods of treating proteinuria
  申请人：Vaughan R. Michael

  公开号：US20050112123A1

  公开（公告）日：2005-05-26

  The present invention provides methods of treating proteinuria, and treating renal disorders associated with proteinuria, the methods generally involving administering to an individual having such a disorder an effective amount of retinoic acid receptor agonist or a retinoid X receptor agonist.

  本发明提供了治疗蛋白尿和与蛋白尿相关的肾脏疾病的方法，这些方法一般涉及向患有此类疾病的个体施用有效量的维甲酸受体激动剂或维A酸X受体激动剂。
• UTILISATION DE COMPOSES POLYCYCLIQUES AROMATIQUES EN TANT QU'ACTIVATEURS DES RECEPTEURS DE TYPE PPARs DANS UNE COMPOSITION COSMETIQUE OU PHARMACEUTIQUE
  申请人：Galderma Research & Development

  公开号：EP1223913B1

  公开（公告）日：2006-03-08
• US6506796B1
  申请人：——

  公开号：US6506796B1

  公开（公告）日：2003-01-14