Novel compositions

Patent metadata

Field	Value
Publication number	US-2025032439-A1
Application number	US-202218715405-A
Country	US
Kind code	A1
Filing date	Dec 5, 2022
Priority date	Dec 3, 2021
Publication date	Jan 30, 2025
Grant date	—

Abstract

The present invention relates to novel compositions comprising a retinoid mixture of cis and trans isomers of a retinyl ester, particularly retinyl acetate, with a cis/trans ratio of less than 0.03 as well as the use thereof for the treatment, prevention and lessening of the symptoms of diseases and conditions which can be treated with 5-HT2B serotonin receptor antagonists, including but not limited to diseases or conditions selected from migraine headaches, anxiety, ocular hypotension, heart valve disease, irritable bowel syndrome, and MDMA (commonly called “ecstasy”) abuse.

First claim

1 . A retinoid mixture comprising cis and trans isomers of retinyl ester, particularly cis and trans isomers of retinyl acetate, wherein the cis/trans ratio within said mixture is 1 to more than 33.33, wherein the ratio is calculated as wt % of cis-isomers compared to wt % of trans-isomers based on total retinoids in said mixture, particularly wherein the mixture comprises less than 0.5 wt % of cis retinyl esters, preferably cis-retinyl acetate, based on total retinoids.

2 . The retinoid mixture according to claim 1 , comprising cis- and trans isomers of retinyl acetate, with a ratio of 1:40, 1:45, 1:50, 1:55, 1:60, 1:65, 1:66.67, 1:70, 1:75, 1:80, 1:90, 1:95, 1:100, 1:101.01, 1:105.26, 1:110, 1:111.11, 1:115, 1:117.65, 1:120, 1:125, 1:130, 1:133.33, 1:135, 1:140, 1:142.86, 1:145, 1:150, 1:155, 1:160, 1:165, 1:166.67, 1:170, 1:175, 1:180, 1:181.82, 1:185, 1:190, 1:195, 1:200, 1:204.08, 1:205, 1:210, 1:215, 1:220, 1:222.22, 1:225, 1:230, 1:232.56, 1:235, 1:240, 1:245, 1:250, 1:255, 1:260, 1:265, 1:270, 1:275, 1:280, 1:285, 1:285.71, 1:290, 1:295, 1:300, 1:305, 1:310, 1:315, 1:320, 1:325, 1:330, 1:333.33, 1:335, 1:340, 1:345, 1:350, 1:355, 1:357.14, 1:360, 1:365, 1:370, 1:375, 1:380, 1:385, 1:390, 1:395 or 1:400, 1:405, 1:410, 1:420, 1:430, 1:440, 1:450 or 1:500, 1:1000 or less, more preferably ranges of 1:33 to 1:1000, 1:100 to 1:500, 1:100 to 1:1000, 1:125 to 1:1000, 1:200 to 1:1000, 1:200 to 1:500, 1:200 to 1:400.

3 . The retinoid mixture according to claim 2 , wherein the retinoid mixture comprising cis- and trans retinyl acetate with a ratio of about 1:400.

4 . The mixture according to claim 1 comprising 2 wt % or less retinol based on total retinoids.

5 . The mixture according to claim 1 comprising 1 wt % or less retinal based on total retinoids.

6 . The mixture according to claim 1 with a color value of L* being in the range of 50 to 100, a* being in the range of −25 to 10 and b* being in the range of 40 to 150.

7 . A pharmaceutical, food, feed or cosmetic composition comprising a biologically-derived mixture of claim 1 .

8 . The composition according to claim 7 , wherein the biologically-derived mixture is biologically produced through fermentation process.

9 . The composition according to claim 7 , wherein the mixture has an anthropogenic CO 2 emission profile of zero upon biodegradation.

10 . The composition according to claim 7 for use as serotonin 5-HT2B receptor antagonist.

11 . The composition according to claim 7 for use in preparation of a nutraceutical, dietary, pharmaceutical or cosmetic product, particularly preparation of a medicament, in the treatment, lessening or prevention of a condition selected from the group consisting of migraine, preferably migraine headache, anxiety, irritable bowel syndrome, ocular hypotension, heart valve disease, and addiction/abuse of a member of the phenethylamine family of stimulants.

12 . A nutraceutical, dietary, pharmaceutical or cosmetic product comprising a mixture or composition according to claim 1 .

13 . Composition or product according to claim 7 for treatment or prevention of migraine, anxiety, irritable bowel syndrome, ocular hypotension, heart valve disease, and addiction/abuse of a member of the phenethylamine family of stimulants.

14 . Method for prevention, treatment or lessening of symptoms associated with migraine, anxiety, irritable bowel syndrome, ocular hypotension, heart valve disease, and addiction/abuse of a member of the phenethylamine family of stimulants comprising administering a composition according to claim 7 .

Assignees

• Dsm Ip Assets Bv

Inventors

• Mendrok-Edinger Christine
• Jackson Eileen
• Wildermann Angela
• Houston Peter Louis

Classifications

• A61Q19/00

  Preparations for care of the skin · CPC title

• A61K2800/10

  General cosmetic use · CPC title

• A61K8/671

  Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal · CPC title

• A61K31/222 Primary

  with compounds having aromatic groups, e.g. dipivefrine, ibopamine · CPC title

• A61K2800/85

  Products or compounds obtained by fermentation, e.g. yoghurt, beer, wine · CPC title