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Publication Number
US-10335407-B2
Publication Date
2019-07-02
Expiration Date
Abstract
The invention relates to compositions for the treatment of obesity and related diseases comprising a) an active substance being not flibanserin, selected from the group consisting of active substances for the treatment of obesity and obesity related diseases and b) flibanserin, optionally in the form of pharmacologically acceptable acid addition salts thereof.
Core Innovation
The disclosed subject matter provides pharmaceutical compositions for treating and/or preventing obesity and related disorders by using flibanserin. Flibanserin is described as being used in the form of a free base and/or pharmaceutically acceptable acid addition salts, including hydrates/solvates.
The disclosed compositions are associated with obesity-related disorders including metabolic syndrome, diabetes type II, dyslipidaemia, hypertension, and osteoarthritis. The disclosure further includes a broad set of obesity-related conditions and presents flibanserin polymorph A. Flibanserin salt examples include succinate, acetate, fumarate, maleate, methanesulfonate, lactic, phosphoric, and hydrochloride.
The disclosure describes flibanserin pharmaceutical compositions that include dosage ranges and formulation types for administration. It also describes combinations or co-administration with non-flibanserin active ingredients, including anti-diabetics, anti-obesity agents such as orlistat, sibutramine, phenetermine, and topiramate, as well as antihypertensives, lipid-modifying drugs, and anti-arthritis agents.
Claims Coverage
The independent claim covers a pharmaceutical composition in which flibanserin is combined with a selected non-flibanserin active ingredient or its pharmaceutically acceptable salt. The claim enumerates multiple possible non-flibanserin actives and requires flibanserin optionally as free base and/or as a pharmacologically acceptable acid addition salt, thereby defining multiple inventive-feature paths within the same claim.
Pharmaceutical composition with a non-flibanserin active plus flibanserin
A pharmaceutical composition comprising an active substance being not flibanserin, selected from the group comprising pioglitazone or a pharmaceutical acceptable salt thereof, troglitazone, rosiglitazone or a pharmaceutical 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, 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 pharmaceutical acceptable salt thereof, simvastatin or a pharmaceutical acceptable salt thereof, lovastatin or a pharmaceutical acceptable salt thereof, atorvastatin or a pharmaceutical acceptable salt thereof, fluvastatin or a pharmaceutical acceptable salt thereof, lipantil or a pharmaceutical acceptable salt thereof, cerivastatin or a pharmaceutical acceptable salt thereof, itavastatin or a pharmaceutical acceptable salt thereof, ZD-4522 or a pharmaceutical acceptable salt thereof, bezafibrate, clinofibrate, clofibrate, simfibrate, or mixtures thereof, together with flibanserin optionally in form of the free base and/or a pharmacologically pharmaceutically acceptable acid addition salt thereof.
The coverage further includes specifying flibanserin as particular pharmaceutically acceptable acid addition salts, including phosphoric acid or hydrochloric acid and enumerated succinic, hydrobromic, acetic, fumaric, maleic, methanesulphonic, lactic, phosphoric, hydrochloric, sulphuric, tartaric, and citric acids and mixtures, as well as constraining flibanserin amounts including 0.01 mg to 400 mg and 100 mg.
Stated Advantages
Treating and/or preventing obesity and related disorders.
Appetite inhibition, promoting weight loss, and preventing body weight gain.
Dose-dependent reductions in body-weight gain in a rat body-weight study.
Documented Applications
Obesity and related disorders, including metabolic syndrome, diabetes type II, dyslipidaemia, hypertension, and osteoarthritis.
Medicaments for appetite inhibition, promoting weight loss, and preventing body weight gain.
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