# US 8,785,458 B2 · Use of flibanserin in the treatment of obesity

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- Number: US 8,785,458 B2
- Document ID: US8785458B2
- Status: Granted
- Kind: B2
- Application number: 13/550,062
- Filed: 2012-07-16
- Published: 2013-03-28
- Granted: 2014-07-22
- Earliest claimed: 2005-08-03
- Assignees: Sprout Pharmaceuticals, Inc.
- Applicants: Angelo Ceci; Marcus Schindler
- Inventors: Angelo Ceci; Marcus Schindler
- Web page: https://patentgrep.com/patent/US8785458B2

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/13: Amines {(A61K31/04 takes precedence)}
- A61K 31/131: acyclic
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/34: having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K 31/365: Lactones
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- 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
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/335: having oxygen as the only ring hetero atom, e.g. fungichromin
- 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 invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.

## Claims

### Claim 1

A method of promoting, increasing or facilitating weight loss comprising administering to an individual in need thereof a therapeutically effective amount of filbanserin, or a pharmacologically acceptable acid addition salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1, comprising administering a second active ingredient comprising orlistat, phenetermine, sibutramine, or topiramate, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The method according to claim 1, comprising administering a second active ingredient comprising ergoset, pramlintinide, leptin, BAY-27-9955, glipazide, glyburide, alprostadil, thipride hydrochloride, cilostazol, mexiletine hydrochloride, ethyl eicosapentate, memantine, or pimagedine, or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The method according to claim 1, comprising administering a second active ingredient comprising pioglitazone or a pharmaceutically acceptable salt thereof, troglitazone, rosiglitazone or a pharmaceutically acceptable salt thereof, JTT-501, GI-262570, MCC-555, YM-440, DRF-2593, BM-13-1258, KRP-297, R-119702, GW-1929, tolbutamide, chloropropamide, tolazamide, acetohexamide, glyclopyramide, an ammonium salt of glyclopyramide, glibenclamide, gliclazide, glimepiride, repaglinide, nateglinide, mitiglinide, JTT-608, metformin, buformin, phenformin, bovine insulin, porcine insulin, semisynthetic human insulin, genetically-engineered human insulin, acarbose, voglibose, miglitol, emiglitate, AJ-9677, BMS-196085, SB-226552, AZ40140, tolrestat, epalrestat, imirestat, zenarestat, SNK-860, zopolrestat, ARI-50i, AS-3201, NGF, LY-333531, LAF237, MK431, 815541, 823093, 825964, liraglutide, exenatide, AVE-2268, T-1095, mazindol, baiamine, NGD-95-1, lipstatin, rimonabant, phenylpropanolamine, ephedrine, pseudroephedrine, dexfenfluramine, fenfluramine, BVT.933, APD356, bromocriptine, pramipexol, dehydroepiandrosterone, exendin, AC 2993, CJC-1131, ZP10, GRT0203Y, captopril, enalapril, alacepril, delapril, lisinopril, imidapril, benazepril, cilazapril, temocapril, trandolapril, manidipine, nifedipine, amlodipine, efonidipine, nicardipine, levcromakalim, L-27152, AL0671, NIP-121, telmisartan, losartan, candesartan cilexetil, valsartan, irbesartan, CS-866, E4177, pravastatin or a pharmaceutically acceptable salt thereof, simvastatin or a pharmaceutically acceptable salt thereof, lovastatin or a pharmaceutically acceptable salt thereof, atorvastatin or a pharmaceutically acceptable salt thereof, fluvastatin or a pharmaceutically acceptable salt thereof, lipantil or a pharmaceutically acceptable salt thereof, cerivastatin or a pharmaceutically acceptable salt thereof, itavastatin or a pharmaceutically acceptable salt thereof, ZD-4522 or a pharmaceutically acceptable salt thereof, bezafibrate, clinofibrate, clofibrate, simfibrate, meloxicam, ibuprofen, or mixtures thereof.

### Claim 5

A method of inhibiting body weight gain comprising administering to an individual in need thereof a therapeutically effective amount of flibanserin, or a pharmacologically acceptable acid addition salt thereof.

### Claim 6 (depends on 5)

The method according to claim 5, comprising administering a second active ingredient comprising orlistat, phenetermine, sibutramine, or topiramate, or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 5)

The method according to claim 5, comprising administering a second active ingredient comprising ergoset, pramlintinide, leptin, BAY-27-9955, glipazide, glyburide, alprostadil, thipride hydrochloride, cilostazol, mexiletine hydrochloride, ethyl eicosapentate, memantine, or pimagedine, or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 5)

The method according to claim 5, comprising administering a second active ingredient comprising pioglitazone or a pharmaceutically acceptable salt thereof, troglitazone, rosiglitazone or a pharmaceutically acceptable salt thereof, JTT-501, GI-262570, MCC-555, YM-440, DRF-2593, BM-13-1258, KRP-297, R-119702, GW-1929, tolbutamide, chloropropamide, tolazamide, acetohexamide, glyclopyramide, an ammonium salt of glyclopyramide, glibenclamide, gliclazide, glimepiride, repaglinide, nateglinide, mitiglinide, JTT-608, metformin, buformin, phenformin, bovine insulin, porcine insulin, semisynthetic human insulin, genetically-engineered human insulin, acarbose, voglibose, miglitol, emiglitate, AJ-9677, BMS-196085, SB-226552, AZ40140, tolrestat, epalrestat, imirestat, zenarestat, SNK-860, zopolrestat, ARI-50i, AS-3201, NGF, LY-333531, LAF237, MK431, 815541, 823093, 825964, liraglutide, exenatide, AVE-2268, T-1095, mazindol, baiamine, NGD-95-1, lipstatin, rimonabant, phenylpropanolamine, ephedrine, pseudroephedrine, dexfenfluramine, fenfluramine, BVT.933, APD356, bromocriptine, pramipexol, dehydroepiandrosterone, exendin AC2993, CJC-1131, ZP10, GRT0203Y, captopril, enalapril, alacepril, delapril, lisinopril, idapril, benazepril, cilazapril, temocapril, trandolapril, manidipine, nifedipine, amlodipine, efonidipine, nicardipine, levcromakalim, L-27152, AL0671, NIP-121, telmisartan, losartan, candesartan cilexetil, valsartan, irbesartan, CS-866, E4177, pravastatin or a pharmaceutically acceptable salt thereof, simvastatin or a pharmaceutically acceptable salt thereof, lovastatin or a pharmaceutically acceptable salt thereof, atorvastatin or a pharmaceutically acceptable salt thereof, fluvastatin or a pharmaceutically acceptable salt thereof, lipantil or a pharmaceutically acceptable salt thereof, cerivastatin or a pharmaceutically acceptable salt thereof, itavastatin or a pharmaceutically acceptable salt thereof, ZD-4522 or a pharmaceutically acceptable salt thereof, bezafibrate, clinofibrate, clofibrate, simfibrate, meloxicam, ibuprofen, or mixtures thereof.

### Claim 9

A method of inhibiting or reducing appetite comprising administering to an individual in need thereof a therapeutically effective amount of flibanserin, or a pharmacologically acceptable acid addition salt thereof.

### Claim 10 (depends on 9)

The method according to claim 9, comprising administering a second active ingredient comprising orlistat, phenetermine, sibutramine, or topiramate, or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 9)

The method according to claim 9, comprising administering a second active ingredient comprising ergoset, pramlintinide, leptin, BAY-27-9955, glipazide, glyburide, alprostadil, thipride hydrochloride, cilostazol, mexiletine hydrochloride, ethyl eicosapentate, memantine, or pimagedine, or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 9)

The method according to claim 9, comprising administering a second active ingredient comprising pioglitazone or a pharmaceutically acceptable salt thereof, troglitazone, rosiglitazone or a pharmaceutically acceptable salt thereof, JTT-501, GI-262570, MCC-555, YM-440, DRF-2593, BM-13-1258, KRP-297, R-119702, GW-1929, tolbutamide, chloropropamide, tolazamide, acetohexamide, glyclopyramide, ammonium salt of glyclopyramide, glibenclamide, gliclazide, glimepiride, repaglinide, nateglinide, mitiglinide, JTT-608, metformin, buformin, phenformin, bovine insulin, porcine insulin, semisynthetic human insulin, genetically-engineered human insulin, acarbose, voglibose, miglitol, emiglitate, AJ-9677, BMS-196085, SB-226552, AZ40140, tolrestat, epalrestat, imirestat, zenarestat, SNK-860, zopolrestat, ARI-50i, AS-3201, NGF, LY-333531, LAF237, MK431, 815541, 823093, 825964, liraglutide, exenatide, AVE-2268, T-1095, mazindol, baiamine, NGD-95-1, lipstatin, rimonabant, phenylpropanolamine, ephedrine, pseudroephedrine, dexfenfluramine, fenfluramine, BVT.933, APD356, bromocriptine, pramipexol, dehydroepiandrosterone, exendin, AC2993, CJC-1131, ZP10, GRT0203Y, captopril, enalapril, alacepril, delapril, lisinopril, imidapril, benazepril, cilazapril, temocapril, trandolapril, manidipine, nifedipine, amlodipine, efonidipine, nicardipine, levcromakalim, L-27152, AL0671, NIP-121, telmisartan, losartan, candesartan cilexetil, valsartan, irbesartan, CS-866, E4177, pravastatin or a pharmaceutically acceptable salt thereof, simvastatin or a pharmaceutically acceptable salt thereof, lovastatin or a pharmaceutically acceptable salt thereof, atorvastatin or a pharmaceutically acceptable salt thereof, fluvastatin or a pharmaceutically acceptable salt thereof, lipantil or a pharmaceutically acceptable salt thereof, cerivastatin or a pharmaceutically acceptable salt thereof, itavastatin or a pharmaceutically acceptable salt thereof, ZD-4522 or a pharmaceutically acceptable salt thereof, bezafibrate, clinofibrate, clofibrate, simfibrate, meloxicam, ibuprofen, or mixtures thereof.
