A61K9/146

Annelated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxamides as HIV integrase inhibitors, methods of preparation and application thereof

The present invention relates to a novel compound that has antiviral activity, in particular, inhibitory activity against the integrase of the human immunodeficiency virus (HIV).

The subject of this invention is a novel annelated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxamide of general formula 1 or 2, or any stereoisomer, any pharmaceutically acceptable salt, any solvate, or any crystalline or polycrystalline form thereof

##STR00001## wherein ring A.sup.1 is an optionally methyl-substituted 5-7 membered saturated heterocycle or heterobicycle; ring A.sup.2 is a 5-6 membered optionally methyl-substituted saturated or partially saturated monocyclic heterocycle; ring A.sup.3 is a 5-6 membered monocyclic saturated cycloalkane or tetrahydro-2H-pyran; R is a 5-7 membered optionally substituted with one, two, or three optionally identical substituents monocyclic or bicyclic heterocyclic radical comprising 1-4 heteroatoms selected from the series O, S, and N except (2S,5R,13aS)-8-hydroxy-7,9-dioxo-N-{[3-(trifluoromethyl)-pyridin-2-yl]methyl}-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopurido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide (formula A4) and (1R,4S,12aR)-N-[(3,5-difluoropyridin-2-yl)methyl]-7-hydroxy-6,8-dioxo-1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2-a:1′,2′-d]pyrazine-9-carboxamide (formula A5).

PHARMACEUTICAL COMPOSITIONS COMPRISING LONAFARNIB AND RITONAVIR
20230218530 · 2023-07-13 ·

Lonafarnib and ritonavir, or a pharmaceutically acceptable salt thereof, are used in combination to treat HDV infection. In one aspect, amorphous co-precipitates comprising lonafarnib, ritonavir, and a co-polymer are provided.

CHEMICAL COMPOSITION

A solid composition comprising nanoparticles of atovaquone dispersed within one or more carrier materials, wherein the atovaquone is present in an amount of at least 10 wt %. Also described is an intramuscularly- or subcutaneously-injectable formulation of nanoparticles of atovaquone.

Solid Self-Nanoemulsifying Drug Delivery System (S-SNEDDS)

A pharmaceutical composition contains at least one methacrylic copolymer having units derived from methacrylamide; at least one pharmaceutically active ingredient; at least one lipid component; and at least one surfactant. The pharmaceutical composition can be used as a medicament. A method can be used to prepare a solid self-nanoemulsifying drug delivery system using the different compounds of the pharmaceutical composition.

Fast Disintegrating Cannabinoid Tablets

The present invention relates in a first aspect to a fast disintegrating cannabinoid tablet, the tablet comprising a sugar alcohol composition comprising one or more sugar alcohol particles in an amount of at least 20% by weight of the tablet, a cannabinoid composition comprising one or more cannabinoids, and a disintegrant composition comprising one or more disintegrants operable to disintegrate the tablet within a period of 2 minutes or less in contact with oral saliva. In a second aspect, the invention relates to a modular tablet, wherein the tablet comprises a further tablet module that is different in composition.

PHARMACEUTICAL COMPOSITION COMPRISING A POTENT INHIBITOR OF URAT1

The present invention relates to pharmaceutical compositions containing 2-((3-(4-cyanonaphthalen-1-yl)pyridine-4-yl)thio)-2-methylpropanoic acid or a pharmaceutically acceptable salt (hereinafter referred to as the “Agent”), more particularly to orally deliverable compositions containing the Agent; to the use of said compositions as a medicament; and to processes for the preparation of said compositions.

Formulations of Enzalutamide

This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.

EXTRUDED DEPOT FORM FOR CONTROLLED ACTIVE SUBSTANCE RELEASE

The invention concerns an extruded depot form for sustained active substance release, comprising at least one active substance, at least one first compound from the class of biodegradable organic polymers based on lactic acid and/or glycolic acid and at least one second compound from the class of lipids.

NON-TOBACCO ORAL NICOTINE POUCH COMPOSITION

A non-tobacco oral nicotine pouch composition is provided, including water in an amount of at least 15% by weight of the pouch composition; nicotine; and at least one sugar alcohol, the pouch composition being free of humectants consisting of alginate, propylene glycol, hydroxypropyl cellulose, and glycerol. An oral pouched nicotine product is also provided, including a saliva-permeable pouch and the non-tobacco oral nicotine pouch composition enclosed in the saliva-permeable pouch.

NON-PORCINE FORMULATIONS AND METHODS THEREOF

Disclosed are compositions and formulations of non-porcine lipase and methods of treatment and manufacture thereof.