Cholesteryl ester transfer protein (CETP) inhibitor and pharmaceutical compositions comprising said inhibitor for use in the treatment or prevention of cardiovascular diseases

Patent metadata

Field	Value
Publication number	US-10653692-B2
Application number	US-201415117154-A
Country	US
Kind code	B2
Filing date	Feb 5, 2014
Priority date	Feb 5, 2014
Publication date	May 19, 2020
Grant date	May 19, 2020

Abstract

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor:

(hereinafter referred to as Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.

First claim

The invention claimed is:

1. A method of treating a subject suffering from or having an increased risk for cardiovascular diseases, the method comprising administering to said subject in need thereof an effective dosage amount of a compound of the formula A:

or a pharmaceutically acceptable salt thereof, wherein the effective dosage amount of said Compound A to be administered to said subject is 1 mg, 2.5 mg, 5 mg, 10 mg, or 25 mg daily, wherein said daily administration decreases LDL-C concentrations in a dose-dependent manner with maximum decreases from baseline of approximately 40% to 53% following said 1 mg, 2.5 mg, 5 mg, 10 mg, or 25 mg of said daily administration of compound A or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein said effective dosage amount of said compound A to be administered to the subject in need thereof is 5 mg or 10 mg daily.

3. The method according to claim 1 , wherein the effective dosage amount of said compound A to be administered to the subject in need thereof is 5 mg daily.

4. The method according to claim 1 , wherein the effective dosage amount of said compound A to be administered to the subject in need thereof is 10 mg daily.

5. The method according to claim 1 , wherein said compound A is to be administered to the subject in need thereof for 1, 5, 10, 20, 40, 52, 100, or 200 weeks.

6. The method according to claim 1 , wherein said compound A is to be administered to the subject in need thereof for at least one week or at least three weeks.

7. The method according to claim 1 , wherein said cardiovascular diseases are selected from hyperlipidemia or mixed dyslipidemia.

8. The method according to claim 2 , wherein said effective dosage amount of said compound A to be administered to the subject in need thereof is 5 mg or 10 mg daily in a solid oral dosage form or liquid oral dosage form.

9. The method according to claim 8 , wherein said solid oral dosage form is a tablet.

10. The method according to claim 8 , wherein said solid oral dosage form is a capsule.

Assignees

• Dezima Pharma B V
• Mitsubishi Tanabe Pharma Corp
• Dezima Pharma Bv

Inventors

• Ford John
• Round Patrick
• Kastelein John
• Kawaguchi Atsuhiro
• Tomiyasu Koichi
• Oka Kozo

Classifications

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/4725

  containing further heterocyclic rings · CPC title