Use of Flibanserin in the Treatment of Obesity

• US 20130079355A1
• Filed: 07/16/2012
• Published: 03/28/2013
• Est. Priority Date: 08/03/2005
• Status: Active Grant

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Inventors: Ceci, Angelo, Schindler, Marcus
• Granted Patent: US 8,785,458 B2
• Time in Patent Office: Days
• US Class Current: 514/254.05
• 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 31/13 Amines A61K31/04 takes precedence
• CPC Class Codes: A61K 31/131 acyclic
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/335 having oxygen as the only ring hetero atom, e.g. fungichromin
• CPC Class Codes: A61K 31/34 having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• CPC Class Codes: A61K 31/365 Lactones
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/04 Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives

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

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.

2. The method according to claim 1, comprising administering a second active ingredient comprising active substances for the treatment of diabetes;

active substances for the treatment of diabetic complications;

active substances for the treatment of obesity;

active substances for the treatment of high blood pressure;

active substances for the treatment of hyperlipidaemia, including arteriosclerosis;

active substances for the treatment of dyslipidaemia, including arteriosclerosis;

or active substances for the treatment of arthritis.

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

4. 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.

5. The method according to claim 1, comprising administering a second active ingredient comprising an insulin sensitiser, insulin secretion accelerator, biguanide, insulin, α

-glucosidase inhibitor, or β

3 adrenoreceptor agonist, glycogen phosphorylase inhibitor, sorbitol dyhydrogenase inhibitor, protein tyrosine phosphatase 1B inhibitor, dipeptidyl protease inhibitor, aldose reductase inhibitor, glycation inhibitor, protein kinase C inhibitor, DPPIV blocker, GLP-1 or GLP-2 analogue, or SGLT-2 inhibitor, lipase inhibitor, anorectic, angiotensin converting enzyme inhibitor, calcium antagonist, potassium channel opener, angiotensin II antagonist, HMG-CoA reductase inhibitor, fibrate compound, or non-steroidal anti-inflammatory drug.

6. 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.

7. 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.

8. The method according to claim 7, comprising administering a second active ingredient comprising active substances for the treatment of diabetes;

active substances for the treatment of diabetic complications;

active substances for the treatment of obesity;

active substances for the treatment of high blood pressure;

active substances for the treatment of hyperlipidaemia, including arteriosclerosis;

active substances for the treatment of dyslipidaemia, including arteriosclerosis;

or active substances for the treatment of arthritis.

9. The method according to claim 7, comprising administering a second active ingredient comprising orlistat, phenetermine, sibutramine, or topiramate, or a pharmaceutically acceptable salt thereof.

10. The method according to claim 7, 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.

11. The method according to claim 7, comprising administering a second active ingredient comprising an insulin sensitiser, insulin secretion accelerator, biguanide, insulin, α

-glucosidase inhibitor, or β

3 adrenoreceptor agonist, glycogen phosphorylase inhibitor, sorbitol dyhydrogenase inhibitor, protein tyrosine phosphatase 1B inhibitor, dipeptidyl protease inhibitor, aldose reductase inhibitor, glycation inhibitor, protein kinase C inhibitor, DPPIV blocker, GLP-1 or GLP-2 analogue, or SGLT-2 inhibitor, lipase inhibitor, anorectic, angiotensin converting enzyme inhibitor, calcium antagonist, potassium channel opener, angiotensin II antagonist, HMG-CoA reductase inhibitor, fibrate compound, or non-steroidal anti-inflammatory drug.

12. The method according to claim 7, 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, 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.

13. 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.

14. The method according to claim 13, comprising administering a second active ingredient comprising active substances for the treatment of diabetes;

active substances for the treatment of diabetic complications;

active substances for the treatment of obesity;

active substances for the treatment of high blood pressure;

active substances for the treatment of hyperlipidaemia, including arteriosclerosis;

active substances for the treatment of dyslipidaemia, including arteriosclerosis;

or active substances for the treatment of arthritis.

15. The method according to claim 13, comprising administering a second active ingredient comprising orlistat, phenetermine, sibutramine, or topiramate, or a pharmaceutically acceptable salt thereof.

16. The method according to claim 13, 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.

17. The method according to claim 13, comprising administering a second active ingredient comprising an insulin sensitiser, insulin secretion accelerator, biguanide, insulin, α

-glucosidase inhibitor, or β

3 adrenoreceptor agonist, glycogen phosphorylase inhibitor, sorbitol dyhydrogenase inhibitor, protein tyrosine phosphatase 1B inhibitor, dipeptidyl protease inhibitor, aldose reductase inhibitor, glycation inhibitor, protein kinase C inhibitor, DPPIV blocker, GLP-1 or GLP-2 analogue, or SGLT-2 inhibitor, lipase inhibitor, anorectic, angiotensin converting enzyme inhibitor, calcium antagonist, potassium channel opener, angiotensin II antagonist, HMG-CoA reductase inhibitor, fibrate compound, or non-steroidal anti-inflammatory drug.

18. The method according to claim 13, 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, 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.