# US 2014/0155338 A1 · Use of pde iii inhibitors for the reduction of heart size in mammals suffering from heart failure

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- Number: US 2014/0155338 A1
- Document ID: US20140155338A1
- Status: Published application
- Kind: A1
- Application number: 14/175,175
- Filed: 2014-02-07
- Published: 2014-06-05
- Earliest claimed: 2004-03-25
- Assignees: Boehringer Ingelheim Vetmedica GmbH
- Inventors: Juergen DAEMMGEN; Olaf JOENS; Rainer KLEEMANN
- Web page: https://patentgrep.com/patent/US20140155338A1

## CPC

- A61K 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- A61K 31/341: not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/4166: having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/4412: having oxo groups directly attached to the heterocyclic ring
- A61K 31/4427: containing further heterocyclic ring systems
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 31/50: Pyridazines; Hydrogenated pyridazines
- A61K 31/501: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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
- A61P 9/08: Vasodilators for multiple indications
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- 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

A phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof is provided for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.

## Claims

### Claim 1

A method for reducing heart size in a patient suffering from heart failure comprising administering to a patient suffering from heart failure at least one medicament comprising a therapeutically effective amount of pimobendan or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the administration of the at least one medicament is free from administering pimobendan with a combination of furosemide, enalapril and digoxin.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the heart failure is chronic congestive heart failure, heart failure due to myocardial infarction or myocardial ischemia due to worsening angina or cardiac arrest.

### Claim 4 (depends on 2)

The method according to claim 2, wherein the heart failure is chronic congestive heart failure, heart failure due to myocardial infarction or myocardial ischemia due to worsening angina or cardiac arrest.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the patient is selected from humans, dogs, cats and horses.

### Claim 6 (depends on 2)

The method according to claim 2, wherein the patient is selected from humans, dogs, cats and horses.

### Claim 7 (depends on 5)

The method according to claim 5, wherein the patient is a dog.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the therapeutically effective amount is effective to reduce the relative mean vertebral heart sum (VHS) of the patient by 0.05 to 0.25 vertebrae within 10 to 100 days of the administration.

### Claim 9 (depends on 2)

The method according to claim 2, wherein the therapeutically effective amount is effective to reduce the relative mean vertebral heart sum (VHS) of the patient by 0.05 to 0.25 vertebrae within 10 to 100 days of the administration.

### Claim 10 (depends on 1)

The method according to claim 1, wherein pimobendan or a pharmaceutically acceptable salt thereof is utilized in oral or parenteral form.

### Claim 11 (depends on 2)

The method according to claim 2, wherein pimobendan or a pharmaceutically acceptable salt thereof is utilized in oral or parenteral form.

### Claim 12 (depends on 1)

The method according to claim 1, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered in a daily dose from 10 μg/kg to 10 mg/kg.

### Claim 13 (depends on 2)

The method according to claim 2, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered in a daily dose from 10 μg/kg to 10 mg/kg.

### Claim 14 (depends on 1)

The method according to claim 1, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered in a single daily dose.

### Claim 15 (depends on 2)

The method according to claim 2, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered in a single daily dose.

### Claim 16 (depends on 1)

The method according to claim 1, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered together with a medicament selected from the group consisting of a calcium channel blocker, an ACE inhibitor, a diuretic, a platelet inhibitor, aspirin, a beta blocker, an angiotensin II antagonist, an aldosterone antagonist, a digitalis glycoside, an antiarrhythmic agent and combinations thereof.

### Claim 17 (depends on 2)

The method according to claim 2, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered together with a medicament selected from the group consisting of a calcium channel blocker, an ACE inhibitor, a diuretic, a platelet inhibitor, aspirin, a beta blocker, an angiotensin II antagonist, an aldosterone antagonist, a digitalis glycoside, an antiarrhythmic agent and combinations thereof.

### Claim 18 (depends on 16)

The method according to claim 16, wherein the calcium channel blocker is selected from the group consisting of diltiazem, verapamil and felodipine, and combinations thereof.

### Claim 19 (depends on 16)

The method according to claim 16, wherein the ACE inhibitor is selected from the group consisting of omapatrilat, MDL100240, alacepril, benazepril, captopril, cilazapril, delapril, enalapril, enalaprilat, fosinopril, fosinoprilat, imidapril, lisinopril, perindopril, quinapril, ramipril, ramiprilat, saralasin acetate, temocapril, trandoloapril, trandolaprilat, ceranapril, moexipril, quinaprilat and spirapril, and combinations thereof.

### Claim 20 (depends on 16)

The method according to claim 16, wherein the beta blocker is selected from the group consisting of bisoprolol, carvediol, metoprolol, propranolol and timolol, and combinations thereof.

### Claim 21 (depends on 16)

The method according to claim 16, wherein the angiotensin II antagonist is selected from the group consisting of saralasin acetate, candesartan, cilexetil, valsartan, losartan potassium, eprosartan, irbesartan, tasosartan, pomisartan and telmisartan, and combinations thereof.

### Claim 22 (depends on 16)

The method according to claim 16, wherein the aldosterone antagonist is selected from the group consisting of spironolactone, eplerenone, canrenone and potassium canrenone, and combinations thereof.

### Claim 23 (depends on 16)

The method according to claim 16, wherein the antiarrhythmic agent is selected from the group consisting of amiodarone, betrylium, disopyramide, dofetilide, flecamide, ibutilide, mexiletine, tocainide, procainamide, propafenone, quinidine and sotalol, and combinations thereof.

### Claim 24 (depends on 16)

The method according to claim 16, wherein the diuretic is selected from the group consisting of furosemide, torasemide, bumetanide, etacrynic acid, azosemide, muzolimine, piretanide, tripamide, bendroflumethazide, chlorothiazide, hydrochlorothiazide, hydroflumethiazide, methychlothiazide, polythiazide, trichlormethiazide, chlorthialidone, indapamide, metolazone, quinethazone, etozolin, triamteren and amiloride, and combinations thereof.

### Claim 25 (depends on 16)

The method according to claim 16, wherein the digitalis glycoside is selected from the group consisting of digoxin, digitoxin, g-strophantin, beta-methyldigoxin and beta-acetyldigoxin, and combinations thereof.

### Claim 26 (depends on 1)

The method according to claim 1, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered together with one or more medicaments selected from the group consisting of one or more ACE inhibitors, one or more diuretics and one or more digitalis glycosides.

### Claim 27 (depends on 2)

The method according to claim 2, wherein pimobendan or a pharmaceutically acceptable salt thereof is administered together with one or more medicaments selected from the group consisting of one or more ACE inhibitors, one or more diuretics and one or more digitalis glycosides.