The purpose of this column is to highlight and to summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in November, 2016.
Mouse for Predicting a Behavior of Drugs in Humans;
Gene Stream Pty. Ltd, Australia J.M. Daly; U.S. Patent # 9,497,944; November 22, 2016.
Animal models are widely used in the drug discovery stage to select few best molecules from thousands of molecules. A false-positive or a false-negative decision can result is wastage of billions of dollars, but more importantly may result in rejection of good molecules or acceptance of wrong molecules. The present invention provides the production, breeding and use of transgenic non-human animals such as mice in which specific genes or portions of genes have been replaced by homologs from another animal, such as a human, to make the physiology of the animals so modified more like that of the other animal with respect to drug pharmacokinetics and metabolism. The invention also extends to the use of the genetically modified non-human animals of the invention for pharmacological and/or toxicological studies.
Method of Treating Overactive Bladder, Not Due to Cancer, by Administering at Least One Jasmonate;
Broady Health Sciences, Texas; B. Broady; U.S. Patent # 9,492,403; November 15, 2016.
Jasmonates (JA) are an oxylipin - a derivative of oxygenated fatty acid which regulates a wide range of processes in plants, ranging from growth and photosynthesis to reproductive development. Various uses of JAs have been known. The patent provides a formulation or composition comprising jasmonate for treating bladder dysfunction, particularly an overactive bladder in a mammal, particularly a human and use of jasmonate for treating bladder dysfunction. The method claims that formulation further comprises a drug or natural substance, as antioxidant, a vitamin, amino acid, nutritional supplement, or combination of the foregoing.
Administration of Aerosolized Iloprost;
Vectura GMBH, Delaware T. Gessler, T. Schmeh, W. Seeger, and R. Voswinckel; U.S. Patent # 9,486,427, November 8, 2016.
Inhalable Iloprost (Ventavis RTM), a synthetic prostacyclin analogue, is marketed in two strengths (10 µg/mL and 20 µg/ mL) and administered from 6 to 9 times per day. Considering the required frequency of administration and the duration of each administration cycle, the use of inhalable iloprost does not appear to be very convenient or patient-friendly. There is a need for improving the patient-friendliness of iloprost administration via the pulmonary route. The invention provides a pharmaceutical composition of iloprost or a salt of iloprost, which is used as an aerosol for pulmonary administration. It is characterized in that an effective single dose of the active ingredient is provided in aerosolized form for inhalation within 2 minutes or less in 13 to 25 breathing maneuvers. It can also be provided as a kit for the treatment of pulmonary diseases.
Pharmaceutical Compositions with Enhanced Performance and Improved Processability;
Hercules LLC, Delaware; T.A. Brugel, T.T. Nguyen, S. Sahoo, D. Tewari, and Y. Zong; U.S. Patent # 9,492,550; November 15, 2016.
The present patent provides the inventive concept(s) relates to a polymer for enhancing drug performance and improving processability. Specifically, the polymer comprises hydroxypropyl methyl cellulose acetate succinate (HPMC-AS). HPMC-AS was originally developed as an enteric polymer for pharmaceutical dosage forms, which provides protection up to a pH of 5.5. In this patent, the polymer comprises HPMCAS with different degrees of substitution of succinoyl and/ or acetyl groups at C6-OH and C3-OH positions. The patent claimed the composition wherein drug is a low-solubility drug having a solubility equal to or less than about 0.5 mg/mL in an aqueous solution at a pH from 1 to 8. The drug compositions have enhanced performance and/or improved process ability.
Wound Healing Using Topical Systems and Methods;
Transdermal Biotechnology, Inc., Connecticut; Perricone; U.S Patent # 9,498,535, November 22, 2016.
Transdermal delivery systems with analgesics and skin refining compounds do not work effectively for all compounds. Also, there is a need for topical treatments for wound healing. The present invention generally relates to treating wounds and/or aiding wound healing. The invention claims a method comprises administering, a composition comprising an effective amount of thyrotropin-releasing hormone (TRH) and nitric oxide to treat the wound, and a carrier having a phosphatidylcholine component entrapping the nitric oxide. The composition can also be an emulsion comprising a first phase comprising a peptide, nitric oxide, and lecithin, and a second phase comprising an emulsifier. In some instances, the lecithin is present at least about 0.25% by weight of the composition. The first phase comprises no more than about 250 ppm of water by weight of the composition. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid “stick,” etc., that can be rubbed or sprayed onto the skin, e.g., wounded skin.
Pharmaceutical Formulations for Treating Ocular Conditions;
Oyster Point Pharma, Inc., San Francisco; D.M. Ackermann, Jr., J. Loudin, and K.J. Mandell; U.S. Patent # 9,504,645; November 29, 2016.
Varenicline (Chantix or Champix) is a prescription medication used to treat nicotine addiction. Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. Dry Eye Disease (“DED”) is a condition that affects ~40 million people in North America. DED results from the disruption of the natural tear film on the surface of the eye, and can result in ocular discomfort, visual disturbance and a reduction in vision-related quality of life. This patent describes the local administration of a therapeutically effective amount of a nicotinic acetylcholine receptor agonist into the nasal cavity of an individual suffering from DED. The agonist, varenicline, selectively binds to the peripheral nicotinic acetylcholine receptor and does not cross the blood-brain barrier in a pharmacologically relevant concentration.
Pharmaceutical Compositions Comprising POH Derivatives;
NeOnc Technologies, Inc., Los Angeles; T. Chen, D. Levin, and S. Puppali; U.S. Patent # 9,499,461, November 22, 2016.
Intrinsic drug resistance is a major problem in the chemotherapy of anti-cancer compounds. Hybrid molecules are prepared with two therapeutic agents. Perillyl alcohol (POH), a naturally occurring monoterpene, has been found to be effective against a variety of cancers. In the previous studies, hybrid molecules containing both POH and retinoids were found to be very effective. On the same lines, in this patent, derivatives of POH with other therapeutic agents were prepared. POH derivatives may be administered alone or in combination with other treatment methods including radiation, standard chemotherapy, and surgery. The administration can also be through various routes including intranasal, oral, oraltracheal for pulmonary delivery, and transdermal. The present invention provides for a pharmaceutical composition comprising a POH carbamate.