Title:
POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF RETINOIDS AND RETINOID-LIKE COMPOUNDS WITH VERY HIGH SKIN PENETRATION RATES
Document Type and Number:
Japanese Patent JP2017160261
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To design and synthesize novel positively charged prodrugs of retinoids or retinoid-like compounds of the general formula (31), 'structure 31'.SOLUTION: The positively charged amino groups of the prodrugs not only greatly increase the solubility of the drugs in water, but also bond to the negative charge on phosphate headgroups of a membrane. This bonding disturbs the membrane a little bit and may make some room for a lipophilic portion of the prodrug. When the molecules of the membrane move, the membrane 'cracks' a little bit because of the bonding of the prodrug. Thereby the prodrug is inserted into the membrane. The prodrugs can be used pharmaceutically in treating any retinoid or retinoid-like compound-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments and can avoid most of side effects of retinoids or retinoid-like compounds.SELECTED DRAWING: Figure 2
Inventors:
YU CHONGXI
Application Number:
JP2017115143A
Publication Date:
September 14, 2017
Filing Date:
June 12, 2017
Export Citation:
Assignee:
YU CHONGXI
International Classes:
C07C219/14; A61K9/70; A61K31/223; A61K31/232; A61K31/235; A61P17/00; A61P17/04; A61P17/06; A61P17/10; A61P17/12; A61P17/14; A61P17/16; A61P35/00; C07C213/06; C07C403/12; C07C403/20
Domestic Patent References:
| JPS6122047A | 1986-01-30 |
Foreign References:
| US20060034904A1 | 2006-02-16 | |||
| WO1997004766A1 | 1997-02-13 |
Attorney, Agent or Firm:
Shinichiro Tanaka
Disciple Maru Ken
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori
Disciple Maru Ken
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori