Pharmaceutical P.I.N. Points - Patent Innovation News June 2022

Neelam Sharma, MS, Lavanya Kundurthy, BE and Hemant N. Joshi, PhD, MBA - Tara Innovations, LLC. www.tarainovations.com and www.tara-marketing.com; [email protected]

Pharmaceutical Compositions for Combination Therapy

M. Pruzanski and L. Adorini; Intercept Pharma; USA; U.S. Patent #11,311,557; April 26, 2022.

Elevated concentrations of circulating lipid compounds in the blood, such as cholesterol and triglycerides, accompany many conditions, some include Type II diabetes, Primary Biliary Cirrhosis (PBC), and various chronic hepatitis states (Hepatitis B and C). The treatments of these conditions need an improved therapy. The present invention relates to a pharmaceutical composition comprising a combination of an FXR (Farnesoid X Receptor) agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and/or a statin). Also, disclosed are the use of combinations for the treatment of the FXR-mediated condition, such as Primary Biliary Cirrhosis (PBC), Primary Sclerosing Cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), other chronic liver diseases with elevated lipid and liver enzyme levels.

Method for Enhancing Wound Healing by Administrating Adenine

H.M. Chen, C.Y. Cheng, C.F. Huang, J.T. Lin; Energenesis Biomedical Co., TW; U.S. Patent #11,311,546; April 22,2022.

Adenine is one of the four nitrogenous bases found in DNA and RNA, and also, an important component of Adenosine Triphosphate (ATP), which is a molecule that is responsible for delivering energy to cells. The inventors have incorporated adenine as is or as a salt in a formulation to enhance the healing of wounds in the following tissues – skin, mouth, gingiva and corneal epithelium. The composition activates Adenosine-5’-Monophosphate Protein Kinase (AMPK) in the patients. It suppresses fibroblast proliferation and prevents scar formation during wound healing. The rate of healing wounds, such as chronic wounds, including diabetic ulcers, pressure ulcers, and a burn may be enhanced by adenine and/or the pharmaceutically acceptable salt.

Compositions and Methods for Targeting Cancers

R. Bindra, P. Glazer, P. Sulkowski, and B. Shuch; Yale University, USA; U.S. Patent #11,311,538; April 26, 2022.

Genomic instability is a hallmark of cancer cells. Cells possess a complex network of surveillance and repair pathways to confront DNA damage directly. The deregulation of DNA repair pathways is associated with the initiation and progression of cancer. Present patent discloses compositions and methods for targeting cancers. The present invention relates to the unexpected discovery of novel compounds that sensitize a tumor cell to anticancer therapies and that comprise succinate, fumarate, and/or derivatives or analogues. The present invention also includes methods for treating or preventing cancer in a subject, wherein the cancer cells have a Fumarate Hydratase (FH) and/or Succinate Dehydrogenase (SDH) mutation. The method includes administering to the subject a therapeutically effective amount of at least one compound selected from the group consisting of a DNA repair inhibitor, a DNA strand break repair inhibitor, and a Homologous Recombination (HR) repair inhibitor.

Lymph Directing Prodrugs

C. Porter, J. Simpson, N. Trevaskis, T. Quach, S. Han, and L. Hu; Monash University, AU; U.S. Patent #11,311,512; April 26, 2022.

The lymphatic system consists of a specialized network of vessels, nodes and lymphoid tissues that are distributed throughout the body in close proximity to the vascular system. Targeted drug delivery to and through the lymphatic system has been suggested as a means to improve both pharmacokinetic and pharmacodynamic profiles. It has the potential to enhance oral bioavailability through avoidance of first pass metabolism, to alter systemic drug disposition, and to enhance efficacy against lymph or lymphocyte mediated pathologies. The present invention relates to compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system.

Efficient Tobramycin Compound Conjugate Compositions

M.V. Shah, V. Subramanian, and I. Subramanian; Somerset Therapeutics, USA; U.S. Patent #11,298,368; April 12, 2022.

Tobramycin is an aminoglycoside that has been used in ophthalmological and other settings as an antibiotic. Tobramycin, is unique among major aminoglycoside antibiotics. Tobramycin products show limited concentration, as well as low corneal permeability. Despite significant investigation and a multitude of formulation approaches, no tobramycin or tobramycin derivative product address the limitations associated with on-market tobramycin products. The present patent discloses compositions comprising tobramycin or a tobramycin derivative that exhibit improvements in permeation of corneal cells, retention in corneal cells, or both. Compositions can comprise tobramycin or tobramycin derivative(s) complexed to an agent (PCL-PVCc-PEG). Such conjugate compositions facilitate improved permeation of corneal cells, retention in corneal cells, or both. The invention also relates to a process of preparing such compositions.

Triamcinolone and Moxifloxacin Compositions

M.V. Shah; I. Subramanian; V. Subramanian, and A. Trehan; Somerset Therapeutics, USA; U.S. Patent #11,298,315; April 12, 2022.

The eye is a sensitive and complex system. Numerous known challenges exist in formulating ophthalmological products. Inventive approaches are required to develop new effective ophthalmological products that exhibit desirable properties such as reduced inflammation risk, uniform API distribution, and API stability. Present patent describes physically and chemically stable pharmaceutical suspension compositions to be used before or after ophthalmic procedures. Compositions comprise therapeutically effective amounts of one or more moxifloxacin compounds and one or more triamcinolone compounds in a suspension. Composition also includes an effective amount of least one non-ionic suspension agent or one ionic suspension agent or both. It also includes an effective amount of a chelating agent. Compositions do not contain HPMC, and any block copolymer of poly(ethylene oxide) and poly(polypropylene oxide).

Composition for Inhibiting Growth of SARS-CoV-2 and Method of Preparing the Same

D.H. Na, K.P. Kang, J.H. Jun, G. Go, H.J. Na, S.J Kang, Y.H. Na, S. J. Yoon, and S.J. Na; Medicare Pharmaceuticals, KR; U.S. Patent #11,292,789; April 5, 2022.

The present disclosure relates to a composition for inhibiting the growth of SARS-CoV-2, and more particularly including a component derived from Phallus indusiatus. In the SARS-CoV-2 replication cycle, Post-Translational Modification (PTM) occurs during viral assembly and maturation and it refers to the covalent modification of a protein after it is translated by the ribosome. PTM involving structural changes in polypeptides includes proteolytic cleavage and disulfide bond formation and phosphorylation, glycosylation and lipidation (palmitoylation and myristoylation). In addition, proteins may be modified by covalent conjugation of one or more small proteins or peptides. Accordingly, the present disclosure sets a virus assembly part as a clear treatment target to solve the above problems, and proposes a substance capable of targeting glucosylation of the PTM stage that is the last stage of the SARS-CoV-2 replication cycle.

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