Compounds and methods for inhibiting CYP26 enzymes

Patent metadata

Field	Value
Publication number	US-11358933-B2
Application number	US-202017084071-A
Country	US
Kind code	B2
Filing date	Oct 29, 2020
Priority date	Dec 12, 2017
Publication date	Jun 14, 2022
Grant date	Jun 14, 2022

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 method of treating a disease or condition in a mammal, comprising administering a compound of the following formula:

wherein the administering is sufficient for treating the disease or condition in the mammal, and the disease or condition is ectopic bone formation.

2. The method of claim 1 , wherein the ectopic bone formation comprises cardiovascular calcification or muscle tissue calcification.

3. The method of claim 1 , wherein the compound 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.

4. The method of claim 1 , wherein the compound is included in a medicament for systemic administration in a formulation comprising between 0.01 and 5 mg per kg body weight per day.

5. The method of claim 1 , 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.

6. The method of claim 5 , wherein the combination is provided in a tablet, capsule, injectable, or topical formulation.

7. The method of claim 1 , wherein the mammal is a human.

8. The method of claim 2 , wherein the ectopic bone formation is cardiovascular calcification.

9. The method of claim 2 , wherein the ectopic bone formation is muscle tissue calcification.

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

• C07D307/79

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

• C07C59/84 Primary

  containing six membered aromatic rings · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · 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