Salts and Crystal Forms Y. Okumura, Y. Iwata, T. Numata, M. Sudo, and T. Okumura; U.S. Patent # 9,447,066; September 20, 2016.
Prostaglandins play a major role in the inflammation process and the inhibition of prostaglandin production, has been a common target of anti-inflammatory drug discovery. The use of high doses of most common NSAIDs can affect other prostaglandin-regulated processes not associated with the inflammation process resulting in sever side-effects. This invention relates to salts and crystal forms of (S)-6-chloro-7-(1,1-dimethylethyl)-2- trifluoromethyl-2H-1-benzopyran-3-carboxylic acid, Compound A, which is cyclooxygenase-2 inhibitor. The present invention provides a salt of compound A having high aqueous solubility, a crystal form thereof, a process for preparing the said salt and a pharmaceutical composition thereof and its use.
Combination Composition Comprising Oxycodone and Acetaminophen for Rapid Onset and Extended Duration of Analgesia K.R. Devarakonda, M.J. Giuliani, V.K. Gupta, R.A. Heasley and S. Shelby; U.S. Patent # 9,468,636; October 18, 2016.
A number of options for pain management are available. Modified release (MR) dosage forms administered once or twice daily offer advantages over their immediate release (IR) counterparts because they provide longer dosing intervals, sustained analgesic effect, and increased patient compliance. MR combination products have a drawback – lack of rapid onset of analgesia which is extremely desirable. This patent provides an extended release pharmaceutical composition comprising oxycodone and acetaminophen that provides a rapid onset of analgesia, and reduced levels of acetaminophen near the end of the dosing interval. The composition, when orally administered, maintains a therapeutic plasma concentration of oxycodone of at least about 5 ng/mL from about 0.75 hour to about 10 hours after administration. Additionally, at least about 90% of the acetaminophen is released from the composition by about 8 hours after administration and by about 10 hours after administration, acetaminophen has a blood plasma concentration that is less than about 30% of acetaminophen's maximum plasma concentration.
Delayed Release Pharmaceutical Composition of Mesalamine V.K. Kakumanu, A. Bansal, S.P. Isloor, and V.K. Arora; U.S. Patent # 9,463,163, October 11, 2016.
Mesalamine, 5-aminosalicylic acid, belongs to the class of antiinflammatory agents and is used for the treatment of mild to moderate active ulcerative colitis. Delayed release tablets, in general, are prepared by entering coating. The procedure in this patent includes: (a) preparation of granules, which include mesalamine or pharmaceutically acceptable salts thereof and a hydrophilic polymer; and (b) mixing extra-granular excipients selected from the group consisting of hydrophilic polymers, glidants, lubricants, diluents and disintegrants; wherein the pharmaceutical composition is further coated with a single layer of polymer. For the single layer coating, they used enteric polymer selected from phthalates or acrylates.
Mucosal Delivery Compositions Comprising a Peptide Complexed with a Crown Compound and/or a Counter Ion P. Botti and S. Tchertchian; U.S. Patent # 9,445,992; September 20, 2016.
Peptide-based drugs are typically delivered by injection, since oral delivery by ingestion is often hindered by poor intrinsic permeability and degradation in the gastrointestinal (GI) tract. This patent provides a mucosal delivery composition comprising an effective amount of a stable hydrated peptide active agent complexed with a crown compound and/or a counter ion solubilized in a non-aqueous hydrophobic vehicle at a pH different from the isoelectric point (pI) of the peptide active agent, wherein the non-aqueous hydrophobic vehicle is acidic or neutral. The patent also claims peptide active agent complex as a dry powder or residue obtainable by drying an aqueous organic solution or suspension.
Methods for Treating Pancreatic Cancer Using Combination Therapies Comprising Liposomal Irinotecan E.Bayever, N. Dhindsa, J.B. Fitzgerald, P.Laivins, V. Moyo, C. Niyikiza and J. Kim; U.S. Patent # 9,452,162, September 27, 2016.
The present invention provides the methods for treating pancreatic cancer in patients by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin. The patent claims a method comprising of intravenously administering an antineoplastic therapy once every two weeks. The antineoplastic therapy consists of (a) 60- 80 mg/m2 of liposomal irinotecan composition having a diameter of approximately 80-140 nm, (b) 200 mg/m2 of the (l) form of leucovorin; and (c) 2,400 mg/m2 of 5-fluorouracil. The terminal elimination halflife of irinotecan in the patient was about 21-48 hours. The irinotecan liposomes comprised of phosphatidylcholine, cholesterol, and a polyethyleneglycol-derivatized phosphatidyl-ethanolamine.
Compositions and Methods for Improving Glucose Uptake N.V. Dhurandhar, and B.C. Das; U.S. Patent # 9,469,659; October 18, 2016.
Infectobesity, obesity of infectious origin, has been receiving increasing attention in the recent years. Ten obesity promoting pathogens have been reported. The first human virus, Adenovirus 36 (AD-36) was reported to cause obesity in experimentally infected animals. AD-36 stimulates preadipocytes to differentiate into adipocytes and increase their lipid content. Embodiments disclosed in the patent relate to compounds and pharmaceutical compositions comprising structures of general Formula I and II, pharmaceutically acceptable salts thereof. Both are boronated compounds. When four bonds to boron are present, boron bears a formal negative charge and the structure further comprises a counteraction selected from the group consisting of potassium and sodium.
Prodrug Activation in Cancer Cells Using Molecular Switches M.A. Ostermeier and C.M. Wright; U.S. Patent # 9,469,841; October 18, 2016.
The complexity of biological systems, stems from a high degree of interactions amongst their constituent components. Fusion proteins that function as molecular switches and serve to couple cellular functions are key components of this network. The present invention provides a method to convert a prodrug into a toxin in a cell that expresses a cancer specific marker. It expresses a polypeptide comprising a prodrug activating enzyme and a protein that binds a cancer specific marker in a cell. This involves treating the cells with a prodrug, wherein the protein that binds the cancer specific marker binds to the marker in a cell that expresses the marker and activates the prodrug activating enzyme, thereby converting the prodrug into a toxin. In one example, the prodrug is 5-FC. The system converts fluorocytosine (5-FC) into 5-fluorouracil (5-FU) in a cell that expresses a cancer specific marker, wherein the marker is HIF-1a, comprising expressing a polypeptide comprising a cytosine deaminase (CD) and a CH1 domain in a cell. In these embodiments, then 5-FC and 5-FU are thus each, and together, responsible for the therapeutic benefit.