Title:
NSAIA PRODRUG HAVING VERY FAST SKIN- AND FILM-INFILTRATION RATE, AND NEW USE THEREOF AS MEDICINE
Document Type and Number:
Japanese Patent JP2020147604
Kind Code:
A
Abstract:
To design and synthesize a new NSAIA prodrug that is positively charged and can be administered transdermally.SOLUTION: A positively-charged NSAIA prodrug is designed and synthesized which has a chemical structure 1, 2a, 2b, 2c, or 2d. A positively-charged amino group of the prodrug greatly increases the solubility in water of the medicine, and thus bonds to a negative charge in a phosphate head group of a film. This bonding destabilizes the film a little and can make a little room in a lipophilic moiety of the prodrug, and in some cases, a slight crack may occur by the bonding of the prodrug. As a result, the prodrug comes to enter the film inside. At pH 7.4, about 99% of the amino groups are protonated. When the amino group is not protonated, the bonding between the amino group of the prodrug and the phosphate head group of the film dissociates, and hence the prodrug enters the film completely.SELECTED DRAWING: Figure 1
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Inventors:
YU CHONGXI
XU LINA
XU LINA
Application Number:
JP2020104475A
Publication Date:
September 17, 2020
Filing Date:
June 17, 2020
Export Citation:
Assignee:
TECHFIELDS INC
YU CHONGXI
YU CHONGXI
International Classes:
C07D211/22; A61K31/192; A61K31/196; A61K31/335; A61K31/38; A61K31/40; A61K31/405; A61K31/407; A61K31/415; A61K31/5415; A61K31/616; A61K47/54; A61P1/04; A61P1/16; A61P3/06; A61P3/10; A61P5/14; A61P5/40; A61P7/06; A61P9/00; A61P9/14; A61P11/10; A61P13/12; A61P15/08; A61P15/18; A61P17/00; A61P17/06; A61P19/02; A61P21/00; A61P25/02; A61P25/28; A61P27/16; A61P29/00; A61P35/00; A61P35/02; A61P37/02; C07D207/337; C07D209/28; C07D231/12; C07D277/30; C07D279/02; C07D295/08; C07D313/14; C07D337/14; C07D417/12; C07D491/052
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| JP2015000561A | 2015-01-05 | |||
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SHANBHAG,V.R. ET AL.: "Ester and amide prodrugs of ibuprofen and naproxen: synthesis, anti-inflammatory activity, and gastr", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 81, no. 2, JPN6012058137, 1992, pages 149 - 154, XP000248778, ISSN: 0004527501, DOI: 10.1002/jps.2600810210
Attorney, Agent or Firm:
Shinichiro Tanaka
Hiroyuki Suda
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori
Shimura
Hiroyuki Suda
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori
Shimura