Compounds and methods for inhibiting CYP26 enzymes

Patent metadata

Field	Value
Publication number	US-11795148-B2
Application number	US-201816771255-A
Country	US
Kind code	B2
Filing date	Dec 12, 2018
Priority date	Dec 12, 2017
Publication date	Oct 24, 2023
Grant date	Oct 24, 2023

Abstract

Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolism, act as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.

First claim

We claim:

1. A compound having formula

2. A pharmaceutical composition comprising the compound of claim 1 .

3. The pharmaceutical composition of claim 2 , further comprising an excipient.

4. The pharmaceutical composition of claim 2 , wherein the pharmaceutical composition is administered as a powder, spray, pill, tablet, syrup, elixir, solution or suspension capable of being administered by injection, suppository, extended release formulation for deposit under the skin or intramuscular injection.

5. The pharmaceutical composition of claim 2 , wherein the compound is included in a medicament for topical application.

6. The pharmaceutical composition of claim 5 , wherein the compound is present in a formulation comprising between 0.01 milligrams and 1 mg per mL of the compound.

7. The pharmaceutical composition of claim 2 , wherein the compound is in a medicament for systemic administration in a formulation comprising between 0.01 and 5 mg per kg body weight per day.

8. The pharmaceutical composition of claim 2 , wherein the compound is given in combination with a retinoid or a retinoid precursor selected from retinol, retinaldehyde, RA, or other natural or synthetic retinoids, or a combination thereof.

9. The pharmaceutical composition of claim 8 , wherein the combination is provided in a tablet, capsule, injectable, or topical formulation.

Assignees

• Univ Kingston

Inventors

• Cameron Donald Andrew
• Petkovich Martin
• Saha Uttam

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• C07D209/08 Primary

  with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring · CPC title

• A61P17/10

  Anti-acne agents · CPC title

• C07C59/84 Primary

  containing six membered aromatic rings · CPC title

• C07D307/79

  with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring · CPC title