A01N43/04

Process for preparing an A2A-adenosine receptor agonist and its polymorphs

Disclosed is a synthesis suitable for large scale manufacture of an A.sub.2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

Maintenance of platelet inhibition during antiplatelet therapy

A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.

Combination of drugs with protein-binding prodrugs
10220101 · 2019-03-05 · ·

The present invention relates to a composition and a combination comprising at least one first drug and at least one protein-binding prodrug, wherein the proteinbinding prodrug comprises a protein-binding group, a second drug, and a linker that can be cleaved hydrolytically, enzymatically, or in a pH-dependent manner in the body, as well as to a kit and a pharmaceutical composition comprising said composition or combination.

Combination of biologically active substances for treatment of hyperglycaemic disorders
10213450 · 2019-02-26 · ·

The present invention relates to a synergistic composition which comprises (a) phlorizin, and (b) at least one further defined inhibitor of the enzyme lactase-phlorizin hydrolase. In particular, the present invention relates to such a composition for the treatment and/or prophylaxis of a hyperglycemic disease such as obesity, diabetes or a secondary disease associated with diabetes. The invention further relates to the use of such a composition for preparing a pharmaceutical composition, a dietary foodstuff and/or a food supplement. The invention further relates to pharmaceutical compositions, dietetic foods and food supplements which comprise a composition according to the present invention.

Chondroitin for use in medicine
10206944 · 2019-02-19 · ·

Chondroitin, a metabolic intermediate of chondroitin sulphate biosynthesis in mammals and other living organisms, possesses biological properties different from those of chondroitin sulphate, and can be advantageously used for applications in the pharmaceutical, nutraceutical, cosmeceutical and medical device fields. Chondroitin has biostimulating, anti-inflammatory and anti-microbial activity and can be used in the treatment of osteoarthritis, eye disorders, interstitial cystitis, lung disorders, inflammatory disorders in general, oncological disorders, peritoneal dialysis, tissue biorevitalisation and wound repair, as a skin filler, and as bioresorbable scaffolds.

3′-substituted methyl or alkynyl nucleosides nucleotides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3-substituted methyl or alkynyl nucleosides of Formula I: (I); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, PD, R.sup.A, R.sup.B1, R.sup.B2, R.sup.C and Z are as defined herein. ##STR00001##

Compounds antagonizing A3 adenosine receptor, method for preparing them, and medical-use thereof

The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.

Use of nicotinic acid riboside or nicotinamide riboside derivatives, and reduced derivatives thereof, as NAD+ increasing precursors

Compositions are provided including nicotinic acid riboside (NAR), and derivatives thereof including 1-(2,3,5-triacetyl-beta-D-ribofuranosyl)-nicotinic acid (NAR triacetate or NARTA); or derivatives of a reduced form of nicotinic acid riboside (NARH), including 1-(2,3,5-triacetyl-beta-D-ribofuranosyl)-1,4-dihydronicotinic acid (NARH triacetate or NARH-TA); or derivatives of nicotinamide riboside (NR), including 1-(2,3,5-triacetyl-beta-D-ribofuranosyl)-nicotinamide (NR triacetate or NRTA); derivatives of a reduced form of nicotinamide riboside (NRH), including 1-(2,3,5-triacetyl-beta-D-ribofuranosyl)-1,4-dihydronicotinamide (NRH triacetate or NRH-TA); or salts or prodrugs thereof, for use in food or beverage applications, pharmaceutical formulations, or as a dietary supplement. Methods of using the compounds above to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) or NADH in cells and tissues for improving cell and tissue survival or overall cell and tissue health are provided.

COMPOSITIONS, METHODS AND TREATMENTS FOR INHIBITING CELL ADHESION AND VIRUS BINDING AND PENETRATION
20190017095 · 2019-01-17 · ·

Disclosed herein are glyco-decoy acceptor compositions that sidetrack or inhibit the activity of biosynthetic enzymes participating in synthesis of ligands binding at selectin, galectin and siglecs receptors; methods of their preparation and uses in drug discovery and in treatments of diseases.

COMPOSITIONS, METHODS AND TREATMENTS FOR INHIBITING CELL ADHESION AND VIRUS BINDING AND PENETRATION
20190017095 · 2019-01-17 · ·

Disclosed herein are glyco-decoy acceptor compositions that sidetrack or inhibit the activity of biosynthetic enzymes participating in synthesis of ligands binding at selectin, galectin and siglecs receptors; methods of their preparation and uses in drug discovery and in treatments of diseases.