POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF RETINOIDS AND RETINOID-LIKE COMPOUNDS WITH VERY HIGH SKIN PENETRATION RATES

Japanese Patent JP2019006795

A

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

YU CHONGXI

JP2018158141A

January 17, 2019

August 27, 2018

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YU CHONGXI

C07C403/20; A61K9/06; A61K9/08; A61K9/107; A61K9/70; A61K31/14; A61L15/44; A61P17/00; A61P17/04; A61P17/06; A61P17/10; A61P17/12; A61P17/14; A61P17/16

JPS63101347A	1988-05-06
JP2019065016A	2019-04-25
JPS6016925A	1985-01-28
JPH0912538A	1997-01-14

US3950418A	1976-04-13
US4326055A	1982-04-20
WO2004009538A1	2004-01-29

Shinichiro Tanaka
Disciple Maru Ken
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori

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