# US 10,869,859 B2 · Methods of preventing the occurrence of cardiovascular events

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- Number: US 10,869,859 B2
- Document ID: US10869859B2
- Status: Granted
- Kind: B2
- Application number: 15/663,787
- Filed: 2017-07-30
- Published: 2018-02-01
- Granted: 2020-12-22
- Earliest claimed: 2016-07-29
- Assignees: Kowa Company, Ltd.
- Applicants: Kowa Company, Ltd.
- Inventors: Ryu Oshima; Gary Gordon
- Web page: https://patentgrep.com/patent/US10869859B2

## CPC

- A61K 31/423: condensed with carbocyclic rings
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/366: having six-membered rings, e.g. delta-lactones
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K 31/47: Quinolines; Isoquinolines
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to pharmacological interventions with pemafibrate for cardiovascular diseases and adverse cardiovascular events. In addition, the invention relates to the use of pemafibrate to treat dyslipidemia and type 2 diabetes mellitus and thereby reduce the risk of cardiovascular disease and adverse cardiovascular events.

## Claims

### Claim 1

A method of preventing the occurrence of cardiovascular events in a patient with one or more risk factors, wherein the patient is on concomitant lipid-lowering therapy other than concomitant moderate to high intensity statin therapy and has an LDL-C concentration ≤70 mg/dL, comprising administering to the patient a therapeutically effective amount of pemafibrate or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the patient has type 2 diabetes mellitus.

### Claim 3 (depends on 1)

The method of claim 1, wherein the patient has an age greater than or equal to 50 years if male or 55 years if female, or systemic atherosclerosis.

### Claim 4 (depends on 1)

The method of claim 1, wherein the patient is taking concurrent statins.

### Claim 5 (depends on 1)

The method of claim 1, wherein the patient has a fasting TG concentration ≥200 mg/dL and <500 mg/dL.

### Claim 6 (depends on 1)

The method of claim 1, wherein the patient has an HDL-C concentration ≤40 mg/dL.

### Claim 7 (depends on 1)

The method of claim 1, wherein the patient has:
a) type 2 diabetes mellitus;
b) a fasting TG concentration ≥200 mg/dL and <500 mg/dL; and
c) an HDL-C concentration ≤40 mg/dL.

### Claim 8 (depends on 1)

The method of claim 1, wherein the patient is taking concurrent statins and has:
a) type 2 diabetes mellitus;
b) a fasting TG concentration ≥200 mg/dL and <500 mg/dL; and
c) an HDL-C concentration ≤40 mg/dL.

### Claim 9 (depends on 7)

The method of claim 7 wherein:
a) the patient has an age greater than or equal to 50 years if male or 55 years if female, or systemic atherosclerosis;
b) the therapeutically effective amount of pemafibrate or pharmaceutically acceptable salt thereof is 0.4 mg, administered orally per day; and
c) the cardiovascular events are selected from nonfatal myocardial infarction, nonfatal ischemic stroke, hospitalization for unstable angina requiring unplanned coronary revascularization, cardiovascular death, and combinations thereof.

### Claim 10 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of pemafibrate or pharmaceutically acceptable salt thereof is 0.4 mg, administered orally per day.

### Claim 11 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of pemafibrate or a pharmaceutically acceptable salt thereof is 0.2 mg, administered orally twice daily.

### Claim 12 (depends on 1)

The method of claim 1, wherein the cardiovascular events are selected from nonfatal myocardial infarction, nonfatal ischemic stroke, hospitalization for unstable angina requiring unplanned coronary revascularization, cardiovascular death, and combinations thereof.

### Claim 13 (depends on 1)

The method of claim 1, wherein the patient has type 2 diabetes mellitus as defined by:
a) a hemoglobin A1c level of 6.5% or greater; and
b) a plasma glucose level:
i) greater than or equal to 126 mg/dL when fasting;
ii) greater than or equal to 200 mg/dL at 2 hours during oral glucose tolerance testing; or
iii) greater than or equal to 200 mg/dL with classic type 2 diabetes mellitus symptoms.

### Claim 14 (depends on 1)

The method of claim 1, wherein the patient has cardiovascular disease.

### Claim 15

A method of preventing the occurrence of cardiovascular events in a patient with one or more risk factors, wherein the patient has an LDL-C concentration ≤70 mg/dL, comprising administering to the patient a therapeutically effective amount of pemafibrate or a pharmaceutically acceptable salt thereof.

### Claim 16 (depends on 15)

The method of claim 15, wherein the patient is taking concurrent statins.

### Claim 17 (depends on 15)

The method of claim 15, wherein the patient has a fasting TG concentration ≥200 mg/dL and <500 mg/dL.

### Claim 18 (depends on 15)

The method of claim 15, wherein the patient is a man with an HDL-C concentration >35 mg/dL and ≤40 mg/dL.

### Claim 19 (depends on 15)

The method of claim 15 wherein the patient has:
a) type 2 diabetes mellitus;
b) a fasting TG concentration ≥200 mg/dL and <500 mg/dL; and
c) an HDL-C concentration ≤40 mg/dL.