5-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-yl)thiophene-2-carboxylic acid | 107430-70-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 蒽
• 英文名称: 5-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-yl)thiophene-2-carboxylic acid
• 英文别名: 5-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthracenyl)-2-thiophene carboxylic acid；5-(5,5,8,8-Tetramethyl-6,7-dihydroanthracen-2-yl)thiophene-2-carboxylic acid
• CAS: 107430-70-6
• 化学式: C₂₃H₂₄O₂S
• 分子量: 364.508
• InChiKey: KEQZAPJIJZMRKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.5
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  65.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  5,5,8,8-四甲基-5,6,7,8-四氢-2-萘甲醛 在 palladium diacetate 、 三氟甲磺酸三甲基硅酯 盐酸 、 sodium hydroxide 、 potassium carbonate 、 三苯基膦 作用下， 以 四氢呋喃 为溶剂， 反应 7.25h， 生成 5-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-yl)thiophene-2-carboxylic acid
  参考文献：
  名称：

  Aromatic retinoids (part 2): A short and convenient route to 5-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthracenyl)-2-furan and -2-thiophene carboxylic acids.

  摘要：

  DOI：

  10.1016/s0040-4039(00)80508-0

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。
• Methods for treating multiple osteochondroma (MO)
  申请人：Clementia Pharmaceuticals Inc.

  公开号：US10980778B2

  公开（公告）日：2021-04-20

  The invention features methods for inhibiting the formation, reducing the size, and slowing the growth of an osteochondroma in a subject with multiple osteochondroma (MO) by administering to the subject palovarotene (also known as R667), or a pharmaceutically acceptable salt thereof. The methods described herein can also ameliorate complications associated with osteochondroma formation and growth in a subject with MO.

  本发明的特点是通过向多发性骨软骨瘤（MO）患者施用帕罗伐汀（又称 R667）或其药学上可接受的盐，抑制骨软骨瘤的形成、减小其大小并减缓其生长。本文所述的方法还可以改善与MO患者骨软骨瘤形成和生长相关的并发症。
• 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。
• EUSTACHE, JACQUES;BERNARDON, JEAN-MICHEL;SHROOT, BRAHAM, TETRAHEDRON LETT., 29,(1988) N 35, C. 4409-4410
  作者：EUSTACHE, JACQUES、BERNARDON, JEAN-MICHEL、SHROOT, BRAHAM

  DOI：——

  日期：——
• Dérivés aromatiques polycycliques, leur procédé de préparation et leur application dans les domaines pharmaceutique et cosmetique
  申请人：CENTRE INTERNATIONAL DE RECHERCHES DERMATOLOGIQUES GALDERMA - CIRD GALDERMA

  公开号：EP0210929B1

  公开（公告）日：1992-06-03