Prophylactic and/or Therapeutic Drug for Diabetic Nephropathy

• US 20190314339A1
• Filed: 04/02/2019
• Published: 10/17/2019
• Est. Priority Date: 04/02/2018
• Status: Active Grant

• Current Assignee: FUSO Pharmaceutical Industries Limited, Hubit Genomix Incorporated
• Original Assignee: Hubit Genomix Incorporated
• Inventors: Doi, Toshio, Tominaga, Tatsuya, Fujita, Yui
• Granted Patent: US 10,828,279 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 13/12 of the kidneys

Abstract

The present invention provides a drug capable of preventing or treating diabetic nephropathy.

The present invention relates to a prophylactic and/or therapeutic drug for diabetic nephropathy, comprising a RARγ agonist as an active ingredient. The present invention also provides a prophylactic and/or therapeutic drug for renal anemia; a drug inhibiting the expression of type IV collagen in mesangial cells; a drug inhibiting the expression of BMP4 in mesangial cells; and a drug inhibiting fibrosis in the renal tubulointerstitium.

Claims

1. (canceled)

4. (canceled)

5. (canceled)

7. (canceled)

9. (canceled)

14. A method of treating diabetic nephropathy in a subject in need thereof, comprising

administering an effective amount of an RARγ

agonist to the subject.

2. The method according to claim 14, wherein the RARγ

agonist is at least one compound selected from the group consisting of palovarotene, 3-fluoro-4-(2-hydroxy-2-(5,5,8,8-tetramethyl-5,6,7,8,-tetrahydronaphthalen-2-yl)acetamido)benzoic acid, 4-[7-(1-adamantyl)-6-hydroxynaphthalen-2-yl]benzoic acid, esters thereof and salts thereof.

3. The method according to claim 14, wherein diabetic nephropathy is derived from type 2 diabetes.

13. The method according to claim 14, which is to be administered orally or parenterally.

15. A method of treating renal anemia in a subject in need thereof, comprising

administering an effective amount of an RARγ

agonist to the subject.

16. A method of suppressing expression of type IV collagen in mesangial cells, comprising

contacting an RARγ

agonist with the mesangial cells.

6. The method according to claim 16, wherein the RARγ

agonist is at least one compound selected from the group consisting of palovarotene, 4-[7-(1-adamantyl)-6-hydroxynaphthalen-2-yl]benzoic acid esters thereof and salts thereof.

17. A method of suppressing expression of BMP4 in mesangial cells, comprising

contacting an RARγ

agonist with the mesangial cells.

8. The method according to claim 17, wherein the RARγ

agonist is at least one compound selected from the group consisting of palovarotene, 3-fluoro-4-(2-hydroxy-2-(5,5,8,8-tetramethyl-5,6,7,8,-tetrahydronaphthalen-2-yl)acetamido)benzoic acid, esters thereof and salts thereof.

18. A method of suppressing fibrosis in renal tubulointerstitium, comprising

contacting an RARγ

agonist with the renal tubulointerstitium.

10. The method according to claim 18, wherein the RARγ

agonist is at least one compound selected from palovarotene, esters thereof and salts thereof.

11. The method according to claim 18, which inhibits the expression of pSmad2/3 in the renal tubulointerstitial cells.

12. The method according to claim 18, wherein fibrosis in the renal tubulointerstitium is derived from diabetic nephropathy.