3-(二甲氨基)-2-羟基苯甲酸 | 67127-88-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 3-(二甲氨基)-2-羟基苯甲酸
• 英文名称: 3-dimethylaminosalicylic acid
• 英文别名: 3-(Dimethylamino)-2-hydroxybenzoic acid
• CAS: 67127-88-2
• 化学式: C₉H₁₁NO₃
• 分子量: 181.191
• InChiKey: MCTTXFMIBVXKKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  60.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(二甲氨基)-2-羟基苯甲酸 、 isobutyric acid (3S,6S,7R,8R)-3-amino-8-benzyl-6-methyl-4,9-dioxo-[1,5]dioxonane-7-yl ester 在 吡啶 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 四氢呋喃 为溶剂， 以27%的产率得到Isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-(3-dimethylamino-2-hydroxy-benzoylamino)-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester
  参考文献：
  名称：

  Semi-synthesis and biological evaluation of analogues of UK-2A, a novel antifungal antibiotic from Streptomyces sp. 517-02

  摘要：

  Several analogues of UK-2A, a novel antifungal antibiotic isolated from Streptomyces sp. 517-02, were semi-synthesized for structure-activity studies. In vitro antifungal activities of these compounds against Saccharomyces cerevisiae IFO 0203 were evaluated by the conventional paper disk method. Several derivatives exhibited growth inhibitory activity similar to UK-2A. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.02.065
• 作为产物：
  描述：

  3-氨基水杨酸 在 palladium on charcoal catalyst 聚合甲醛 、 氨 作用下， 以 盐酸 、 溶剂黄146 为溶剂， 生成 3-(二甲氨基)-2-羟基苯甲酸
  参考文献：
  名称：

  Benzamide derivatives

  摘要：

  苯甲酰胺衍生物的化学式为：- ##STR1## 其中R.sup.1代表氟、氯或溴原子，或烷基、烷氧基、烷硫基、烷磺酰基、烷酰胺基、烷基胺基或烷基磺酰胺基，每个这样的基团含有1至6个碳原子，双烷基磺酰胺基、双烷基胺基或双烷基氨基甲酰基（其中两个烷基可能相同或不同，每个含有1至4个碳原子），含有2至6个碳原子的烷酰基、烷氧羰基、烷氧羰胺基或烷基氨基甲酰基，或羟基、甲酰基、硝基、三氟甲基、芳基、苄氧羰胺基、氨基、磺酰胺基、氰基、四唑-5-基、羧基、氨基甲酰基或芳酰基，n代表整数1、2或3，是具有药理特性的新化合物，特别是在治疗由组织固定抗体与特定抗原相互作用所表现出的呼吸系统疾病的治疗中具有价值的特性。

  公开号：

  US04146631A1

文献信息

• Compounds and their salts specific to the PPAR receptors and the EGF receptors and their use in the medical field
  申请人：Naccari Giancarlo

  公开号：US20090118357A1

  公开（公告）日：2009-05-07

  Therefore the present invention relates specifically to the compounds of general formula (I), in which R 1 and R 2 , which may be identical or different, are selected from the group comprising H, —C n H 2n-1 , a linear or branched alkyl group having from 1 to 6 carbon atoms, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R 3 is selected from —CO—CH 3 , —NHOH, —OH, —OR 6 in which R 6 is a linear or branched alkyl group having from 1 to 6 carbon atoms; R 4 is selected from H, a linear or branched alkyl group having from 1 to 6 carbon atoms, phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl or allyl; R 5 , R 7 , R 8 are hydrogen atoms; or R 3 and R 4 , R 4 and R 5 , or R 7 and R 8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.

  因此，本发明特别涉及具有通用公式（I）的化合物，其中R1和R2，可以相同或不同，选自包括H，—CnH2n-1，具有1到6个碳原子的直链或支链烷基，或者共同形成一个含有5或6个原子的芳香族或脂肪族环；R3选自—CO—CH3，—NHOH，—OH，—OR6，其中R6是一个具有1到6个碳原子的直链或支链烷基；R4选自H，具有1到6个碳原子的直链或支链烷基，苯基，苄基，—CF3或—CF2CF3，乙烯基或烯丙基；R5，R7，R8是氢原子；或者R3和R4，R4和R5，或R7和R8共同形成一个环，与苯环，芳香族或脂肪族环融合，含有5或6个原子，并包括1到2个独立选自N，O的杂原子，及其在医疗领域的应用。
• [EN] METHODS OF TREATING HAIR RELATED CONDITIONS<br/>[FR] PROCÉDÉS DE TRAITEMENT DE TROUBLES LIÉS AU SYSTÈME PILEUX
  申请人：NOGRA PHARMA LTD

  公开号：WO2014041140A1

  公开（公告）日：2014-03-20

  Provided herein are methods for enhancing epidermal regeneration in a patient in need thereof, comprising topically administering to said patient a pharmaceutically acceptable composition comprising N-acetyl- 3-(4-aminophenyl)-2-methoxypropionic acid or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient. For example, provided are methods for treating or ameliorating cicatricial alopecia, comprising topically administering to a patient in need thereof a pharmaceutically acceptable composition comprising the disclosed compounds. Also provided are methods for protecting hair follicle progenitor cells and compositions comprising same using the disclosed compounds.

  本文提供了一种增强患者表皮再生的方法，包括向该患者局部施用含有N-乙酰基-3-(4-氨基苯基)-2-甲氧基丙酸或其药学上可接受的盐或立体异构体和药学上可接受的赋形剂的药学上可接受的组合物。例如，本文提供了治疗或改善瘢痕性脱发的方法，包括向需要该药物的患者局部施用含有上述化合物的药学上可接受的组合物。此外，本文还提供了使用上述化合物保护毛囊祖细胞和含有这些化合物的组合物的方法。
• [EN] METHODS OF INHIBITING HAIR GROWTH<br/>[FR] PROCÉDÉS D'INHIBITION DE LA CROISSANCE PILEUSE
  申请人：NOGRA PHARMA LTD

  公开号：WO2014041141A1

  公开（公告）日：2014-03-20

  Provided herein are methods for reducing mammalian hair growth using the disclosed compounds. Also provided herein are methods of inhibiting hair growth after hair removal of an area of mammalian skin of a mammal using the disclosed compounds.

  本文提供了使用披露的化合物减少哺乳动物毛发生长的方法。本文还提供了使用披露的化合物抑制哺乳动物皮肤区域脱毛后毛发生长的方法。
• Compounds and their Salts Specific to the PPAR Receptors and the EGF Receptors and their Use in the Medical Field
  申请人：Naccari Giancarlo

  公开号：US20120316230A1

  公开（公告）日：2012-12-13

  The present invention relates to compounds of formula (I), where R 1 and R 2 , which may be identical or different, are selected from the group comprising H, C n H 2n-1 , a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R 3 is —CO—CH 3 , —NHOH, —OH, or —OR 6 where R 6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF 3 or CF 2 CF 3 , vinyl or allyl; R 5 , R 7 , R 8 are hydrogen atoms; or R 3 and R 4 , R 4 and R 5 , or R 7 and R 8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.

  本发明涉及式（I）的化合物，其中R1和R2，可以相同也可以不同，选择自H，CnH2n-1，具有1至6个碳的线性或支链烷基团，或者共同形成一个具有5或6个原子的芳香或脂肪环；R3为—CO—CH3，—NHOH，—OH或—OR6，其中R6为具有1至6个碳的线性或支链烷基团；R4为H，具有1至6个原子的线性或支链烷基团，苯基，苄基，—CF3或CF2CF3，乙烯基或丙烯基；R5，R7，R8为氢原子；或者R3和R4，R4和R5，或R7和R8共同形成一个环，与苯环，芳香或脂肪环共同构成一个具有1至2个杂原子的环，独立选择自N，O的群组；以及在医药领域中的应用。
• METHODS OF TREATING HAIR RELATED CONDITIONS
  申请人：NOGRA PHARMA LIMITED

  公开号：US20150250749A1

  公开（公告）日：2015-09-10

  Provided herein are methods for enhancing epidermal regeneration in a patient in need thereof, comprising topically administering to said patient a pharmaceutically acceptable composition comprising N-acetyl-3-(4-aminophenyl)-2-methoxypropionic acid or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient. For example, provided are methods for treating or ameliorating cicatricial alopecia, comprising topically administering to a patient in need thereof a pharmaceutically acceptable composition comprising the disclosed compounds. Also provided are methods for protecting hair follicle progenitor cells and compositions comprising same using the disclosed compounds.

  本文提供了一种增强病人表皮再生的方法，包括将一种药学上可接受的组合物局部施用于该病人，所述组合物包括N-乙酰基-3-(4-氨基苯基)-2-甲氧基丙酸或其药学上可接受的盐或立体异构体，以及药学上可接受的赋形剂。例如，本文提供了治疗或改善瘢痕性脱发的方法，包括将所述化合物的药学上可接受的组合物局部施用于需要治疗的病人。同时，本文还提供了使用所述化合物保护毛囊祖细胞的方法和组合物。