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Message: Re: New patent application - USA Inventor

I don't think it is a very new patent. Original filing date for patent named "Pharmaceutical compositions for substituted quinazolinones" is October 2012. Pretty sure this is all old news. I've cited a few paragraphs below. Nothing to get excited about, IMO.

http://www.freepatentsonline.com/9610251.html

"Many active compounds, including compounds of Formula I, have poor aqueous solubility, thus reducing their potential for absorption from the gastrointestinal tract. A challenge to working with compounds having poor aqueous solubility is that it can be difficult to improve solubility without decreasing stability of the compound, thus reducing shelf life to an unacceptable levels. The hydrophobicity of compounds of Formula I can be altered when substituted with ionizable basic substituents, such as amines and/or amides, providing an opportunity for increased solubilization and absorption from the acidic gastric environment when dosed orally. However, due to the increasing pH gradient (pH 3 to 7) in the gastrointestinal cavity, the opportunity for dissolution and absorption is dependent on the rate of dissolution. As a result, if these compounds are not dissolved in the right gastric environment, absorption and bioavailability in the small intestine is reduced or lost. Thus, any improved biological activity gained from substituting compounds of Formula I with ionizable basic subsitutents is compromised because of their diminished solubility in the small intestine, which leads to a decrease in the overall efficacy and therapeutic effects of the active drug substance.

Because compounds of Formula I have been shown to regulate expression of Apo-A1 and given the correlation between increased expression of Apo-A1 and treating or preventing cardiovascular and cholesterol- or lipid-related disorders, there is a need to develop solid pharmaceutical formulations comprising substituted quinazolinones, such as those described herein, where the pharmaceutical formulations improve dissolution of the quinazolinone drug substance, have favorable bioavailability, are convenient to administer, and which are stable for an extended period of time.

The invention provides novel solid pharmaceutical formulations comprising compounds of the Formula I, as defined above, and processes for their preparation. The formulations of the invention are stable and have improved disintegration and dissolution profiles for compounds of Formula I and improved bioavailability of the drug substance. The present invention also provides, in part, methods of using the pharmaceutical formulations of the invention that are useful for regulating the expression of apolipoprotein A-I (ApoA-I) and as BET inhibitors, for the treatment and prevention of cardiovascular disease, and cholesterol- or lipid-related disorders, including, for example, metabolic syndrome, inflammatory disease, Alzheimer's disease, atherosclerosis, diabetes, and cancer. Cancers that may be treated or prevented with the methods of the invention include cancers that are sensitive to a compound that binds to bromodomains of BET family proteins, including NUT midline carcinoma; cancers that exhibit c-myc overexpression, including, but not limited to, Burkitt's lymphoma, acute myelogenous leukemia, multiple myeloma, aggressive human medulloblastoma; cancers overexpressing n-myc; and cancers that rely on the recruitment of p-TEFb to regulate activated oncogenes such as, e.g., NOTCH1."

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