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

Title:

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

Document Type and Number:

Japanese Patent JP2015221830

Kind Code:

A

Abstract:

PROBLEM TO BE SOLVED: To design and synthesize novel positively charged prodrugs of retinoids or retinoid-like compounds in a general formula (31), 'structure 31'.SOLUTION: The positively charged amino groups of the prodrugs not only largely increase the solubility of the drugs in water, but also bond to the negative charge on a phosphate head group of membranes. This bonding disturbs the membrane a little bit and may make some room for the lipophilic portion of the prodrug. When the molecules of membrane move, the membrane may 'crack' a little bit due to the bonding of the prodrug. This causes the prodrug to insert into the membrane. The prodrugs can be used medicinally in treating any retinoids or retinoid-like compounds-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments and avoid most of the side effects of retinoids or retinoid-like compounds.

More Like This:

JPH01128953	CATECHOL CARBOXYLIC ACID DERIVATIVE
JPS60243045	SUBSTITUTED PHENOXYPHENYLACETIC ACID OR THIOACETIC ACID DERIVATIVE AND HERBICIDE CONTAINING THE SAME
JPS51125245	PHENYL ACETIC ACID DERIVATIVES AND HYPERLIPIDEMIA TREATING AGENT CONTAINING SAME AS EFFECTIVE COMPONENT

Inventors:

YU CHONGXI

Application Number:

JP2015167104A

Publication Date:

December 10, 2015

Filing Date:

August 26, 2015

Export Citation:

Click for automatic bibliography generation Help

Assignee:

YU CHONGXI

International Classes:

C07C219/10; A61K31/192; A61K31/202; A61K31/203; A61K47/18; A61K47/48; A61P17/00; A61P17/06; A61P17/14; A61P35/00; A61P43/00; C07C213/00; C07C213/06; C07C219/14; C07C227/02; C07C229/12

Domestic Patent References:

JPS6016925A

1985-01-28

Foreign References:

WO2004018001A1	2004-03-04
US5972323A	1999-10-26
US3950418A	1976-04-13

Other References:

ＣＨＥＭ．ＰＨＡＲＭ．ＢＵＬＬ．, vol. ５２（５）, JPN6016017370, 2004, pages 501 - 506, ISSN: 0003314458

Attorney, Agent or Firm:

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

Previous Patent: RON BINDING CONSTRUCTS AND METHODS OF USE THEREOF

Next Patent: BIGLYCAN MUTANTS AND RELATED THERAPEUTICS AND METHODS OF USE