By a News Reporter-Staff News Editor at Pharma Business Week -- NOVARTIS AG (Basel, CH) has been issued patent number 9623012, according to news reporting originating out of Alexandria, Virginia, by NewsRx editors (see also Pharmaceutical Companies).
The patent's inventors are Achour, Miloud (Basel, CH); Fairhurst, Robin Alec (Basel, CH); Grandeury, Arnaud (Basel, CH); Hatakeyama, Shinji (Basel, CH); Koziczak-Holbro, Magdalena (Basel, CH); Tufilli, Nicola (Basel, CH); Ullrich, Thomas (Basel, CH).
This patent was filed on February 26, 2014 and was published online on April 18, 2017.
From the background information supplied by the inventors, news correspondents obtained the following quote: "Benzothiazolone compounds which are beta-2-adrenoceptor agonists are described in WO2004/16601 and WO2006/056471. WO2005/110990 also describes benzo-condensed heterocycles as beta-2 agonists.
"While beta-2 agonists have long been known for their bronchodilating properties, they are also known for their capability to produce skeletal muscle hypertrophy.
"Numerous studies have focused on therapeutic applications of the anabolic properties of beta-2 agonists for ameliorating muscle wasting and improving muscle function. However, this class of compounds has also been associated with undesirable side-effects, including increased risk of adverse cardiovascular-related events. Thus, the use of beta-2 agonists in muscle wasting diseases has hitherto been limited by cardiac hypertrophy and potentially deleterious effects on cardiovascular function.
"There is a need to provide new beta-2 agonists that are good drug candidates. In particular, a new beta-2 agonist should bind potently to the beta-2 adrenoceptor whilst showing little affinity for other receptors, such as e.g. the beta-1 adrenoceptor, the alpha-1A adrenoceptor, or the 5HT.sub.2C receptor, and show functional activity as an agonist. It should be metabolically stable and possess favourable pharmacokinetic properties. It should be non-toxic and demonstrate few side-effects, in particular fewer cardiac side-effects than known marketed beta-2 agonists, such as e.g. formoterol. Furthermore, the ideal drug candidate will exist in a physical form that is stable, non-hygroscopic and easily formulated."
Supplementing the background information on this patent, NewsRx reporters also obtained the inventors' summary information for this patent: "There is therefore a need to provide a compound having at least some of the properties described above wherein the compound is in a physical form which may improve efficiency, bioavailability, stability and/or acceptance by the patient.
"These objectives are aimed to be achieved by providing a composition as described herein, by providing the composition for use in diseases, particular for the treatment of muscular dystrophy, disuse-related atrophy, cachexia or sarcopenia, as described herein and by providing a process to produce the composition as described herein.
"Various embodiments of the invention are described herein.
"Within certain aspects, provided herein is a pharmaceutical composition in solid oral dosage form comprising 0.01 to 15% (w/w) of ®-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-- hydroxybenzo[d]thiazol-2(3H)-one and one or more pharmaceutically acceptable excipients, wherein ®-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-- hydroxybenzo[d]thiazol-2(3H)-one is in acetate salt form.
"In another embodiment, the invention provides a method for the manufacture of said pharmaceutical composition.
"In another embodiment, the invention provides a method of treatment or prevention of muscular dystrophy, disuse-related atrophy, cachexia or sarcopenia comprising administering said pharmaceutical composition."
For the URL and additional information on this patent, see: Achour, Miloud; Fairhurst, Robin Alec; Grandeury, Arnaud; Hatakeyama, Shinji; Koziczak-Holbro, Magdalena; Tufilli, Nicola; Ullrich, Thomas. Formulation Comprising Benzothiazolone Compound. U.S. Patent Number 9623012, filed February 26, 2014, and published online on April 18, 2017. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=9623012.PN.&OS=PN/9623012RS=PN/9623012
Keywords for this news article include: Pharmaceutical Companies, Cachexia, Cardiology, Sarcopenia, NOVARTIS AG, Cardiovascular, Muscular Atrophy, Risk and Prevention, Muscular Dystrophies, Neurologic Manifestations, Atrophic Muscular Disorders, Neuromuscular Manifestations, Neuromuscular Diseases and Conditions, Nervous System Diseases and Conditions.
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