Treatment of neuropathy

• US 20030162782A1
• Filed: 07/26/2002
• Published: 08/28/2003
• Est. Priority Date: 10/21/1999
• Status: Abandoned Application

• Current Assignee: Eric B. Grossman, Nandan P. Koppiker, Steven B. Leichter
• Original Assignee: Eric B. Grossman, Nandan P. Koppiker, Steven B. Leichter
• Inventors: Koppiker, Nandan P., Grossman, Eric B., Leichter, Steven B.
• Application Number:
  US10/206,615
• Publication Number:
  US 20030162782A1
• Time in Patent Office: Days
• US Class Current: 514/246
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

This invention relates to the use of cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of neuropathy, including in particular the treatment of diabetic neuropathy.

Claims

1. A method of treating a patient suffering from neuropathy which comprises treating said patient with an effective amount of a cGMP PDE5 inhibitor, with the proviso that the inhibitor is not a:

i) substituted 5-(3-pyridyl)pyrazolo[4,3-d]pyrimidin-7-one,

ii) substituted 2-(3-pyridyl)-4a,5-dihydroimidazo[5, 1-f][1,2,4]triazin-4(3H)-one, or

iii) substituted 2-phenylpurin-6-one or a substituted 2-(3-pyridyl)purin-6-one,

for treating peripheral diabetic neuropathy.

2. A method according to claim 1 wherein the neuropathy is diabetic polyneuropathy.

3. A method according to claim 1 or 2 wherein the inhibitor is administered orally

4. A method according to claim 3 wherein the daily dosage is 5 to 500 mg.

5. A method according to any preceding claim wherein the inhibitor has an IC50 at less than 100 nanomolar.

6. A method according to any preceding claim wherein the inhibitor has a selectivity ratio in excess of 1000.

7. A method according to any preceding claim wherein the inhibitor is sildenafil, or pharmaceutically acceptable salts thereof.

8. A method according to claim 7 wherein the daily dosage is 10 to 100 mg.

9. The use of a cGMP-PDE5 inhibitor for the manufacture of a medicament for the treatment of neuropathy, with the proviso that the inhibitor is not a:

i) substituted 5-(3-pyridyl)pyrazolo[4,3-d]pyrimidin-7-one,

ii) substituted 2-(3-pyridyl)-4a, 5-dihydroimidazo[5, 1-f][1,2,4]triazin-4(3H)-one, or

iii) substituted 2-phenylpurin-6-one or a substituted 2-(3-pyridyl)purin-6-one,

for treating peripheral diabetic neuropathy.

10. The use according to claim 9 wherein the neuropathy is diabetic polyneuropathy.

11. The use according to claim 9 or 10 wherein the inhibitor is administered orally.

12. The use according to claim 11 wherein the daily dosage is 5 to 500 mg.

13. The use according to any one of claims 9 to 12 wherein the inhibitor has an IC50 at less than 100 nanomolar.

14. The use according to any one of claims 9 to 13 wherein the inhibitor has a selectivity ratio in excess of 1000.

15. The use according to any one of claims 9 to 14 wherein the inhibitor is sildenafil, or pharmaceutically acceptable salts thereof.

16. The use according to claim 15 wherein the daily dosage is 10 to 100 mg.