A61P31/12

Tetrazolones as a Carboxylic Acid Bioisosteres
20180002297 · 2018-01-04 ·

The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

COMBINED TREATMENT WITH A TLR7 AGONIST AND AN HBV CAPSID ASSEMBLY INHIBITOR
20180000824 · 2018-01-04 · ·

The present invention is directed to compositions and methods for treating hepatitis B virus infection. In particular, the present invention is directed to a combination therapy comprising administration of a TLR7 agonist and an HBV capsid assembly inhibitor for use in the treatment of chronic hepatitis B patient.

POLYMERIC DRUG CONJUGATES WITH TETHER GROUPS FOR CONTROLLED DRUG DELIVERY

Described herein is a cyclodextrin containing polymer conjugate.

SULPHATED HYALURONIC ACIDS AS REGULATOR AGENTS OF THE CYTOKINE ACTIVITY

The object of the present invention relates to the new and surprising use of sulfated hyaluronic acid (HAS) as regulator agent of the cytokine activity (pro- and antiinflammatory) and consequently the use of HAS for the preparation of a new medicine for the prevention and treatment of pathologies associated with the activation and/or deficiency of cytokines of a pro- and antiinflammatory nature. The Applicant has in fact discovered its exclusive capacity in modulating the activity of these particular proteins, it has studied the action mechanism and demonstrated the substantial difference between the different sulfated types known in the state of the art, but above all it has demonstrated an unexpectedly high activity of HAS vs different types and strains of Herpes virus, HIV, Cytomegalovirus and the virus of vesicular stomatitis.

POLYPEPTIDE FRAGMENTS COMPRISING ENDONUCLEASE ACTIVITY AND THEIR USE

The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase or variants thereof possessing endonuclease activity, wherein said PA subunit is from a virus belonging to the Orthomyxoviridae family. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds and pharmaceutical compositions comprising the identified compounds for the treatment of disease conditions due to viral infections caused by viruses of the Orthomyxoviridae family.

ENZYMES AND METHODS FOR PRODUCING OMEGA-3 FATTY ACIDS

The present invention relates to methods of synthesizing long-chain polyunsaturated fatty acids, especially eicosapentaenoic acid, docosapentaenoic acid and docosahexaenoic acid, in recombinant cells such as yeast or plant cells. Also provided are recombinant cells or plants which produce long-chain polyunsaturated fatty acids. Furthermore, the present invention relates to a group of new enzymes which possess desaturase or elongase activity that can be used in methods of synthesizing long-chain polyunsaturated fatty acids. In particular, the present invention provides ω3 destaurases, Δ5 elongases and Δ6 desaturases with novel activities. Also provided are methods and DNA constructs for transiently and/or stably transforming cells, particularly plant cells, with multiple genes.

FATTY ACIDS AS ANTI-INFLAMMATORY AGENTS

Compounds of formula I and their metabolites are potent mediators of an inflammatory response:

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where a, b, c, d, e, f, V, W, X, Y, R.sup.a, R.sup.a′, R.sup.b, R.sup.b′, R.sup.c, and R.sup.c′ are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.

NUTRITIONAL COMPOSITIONS COMPRISING HUMAN MILK OLIGOSACCHARIDES AND NUCLEOTIDES AND USES THEREOF FOR TREATING AND/OR PREVENTING ENTERIC VIRAL INFECTION
20180008623 · 2018-01-11 · ·

Disclosed are nutritional compositions including human milk oligosaccharides and nucleotides that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.

MODIFIED RNAi AGENTS

One aspect of the present invention relates to double-stranded RNAi (dsRNA) duplex agent capable of inhibiting the expression of a target gene. The dsRNA duplex comprises one or more motifs of three identical modifications on three consecutive nucleotides in one or both strand, particularly at or near the cleavage site of the strand. Other aspects of the invention relates to pharmaceutical compositions comprising these dsRNA agents suitable for therapeutic use, and methods of inhibiting the expression of a target gene by administering these dsRNA agents, e.g., for the treatment of various disease conditions.

METHODS FOR TREATING VASCULAR LEAK SYNDROME AND CANCER
20180009890 · 2018-01-11 ·

Disclosed are methods for treating Vascular Leak Syndrome and preventing cancer metastasis. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, sepsis, cancer or the presence of pathogens.