The invention provides new pyrazine derivatives of formula (I):

##STR00001##

or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

The invention provides for a compound having the structure of Formula (I) to Formula (VI), including Compounds 1 to 6, their pharmaceutically acceptable salts, and compositions comprising thereof. This invention further includes methods of their use for the treatment of diseases or disorders associated with the modulation of calcium sensing receptors (CaSRs), including secondary hyperparathyroidism associated with chronic kidney disease in a subject in need thereof. This disclosure further relates to a process for the preparation of said pharmaceutical compositions.

An oral pharmaceutical formulation using 4, 8-dihydroxy-5, 5, 7, 9, 13-pentamethyl-16-[1-methyl-2-(2-methyl-thiazole-4-yl)-ethenyl]]-oxacyclohexadec-13-ene-2,6-dione (utidelone) as an active ingredient, suitable for oral administration. The pharmaceutical formulation is a solid formulation such as tablets and capsules, and the pharmaceutical dosage form has good stability, in vitro dissolution behavior, and bioavailability.

A composition having an autonomic nervous system modulatory function-improving effect or an effect for suppressing a decrease of an autonomic nervous system modulatory function, and a composition having a cognitive function-improving effect or an effect for suppressing a decrease of a cognitive function. A composition for modulating an autonomic nervous system, including a black soybean seed coat extract, a composition for improving a cognitive function, including a black soybean seed coat extract, and use of a black soybean seed coat extract in production of a composition for modulating an autonomic nervous system or a composition for improving a cognitive function.

The present invention relates to pharmaceutical compositions comprising Ibrutinib. More particularly, the present invention relates to a tablet composition comprising Ibrutinib and one or more pharmaceutically acceptable excipients and process for preparing such compositions.

The present disclosure concerns effervescent compositions and methods of making and using the same. In some embodiments, the disclosed effervescent compositions are formed from an input blend comprising an acid and a base by granulating the input blend in a twin-screw processor. The granules formed from the input blend can be formed by an in situ granulating agent, which can be a portion of the acid that melts during granulation. In some embodiments, the effervescent compositions can be made using a twin-screw processor comprising an intake zone for receiving an input blend comprising an acid and a base; a granulation initiation zone for melting only a portion of the acid to serve as an in situ granulating agent; a granulation completion zone for granulating the input blend; and an outlet for discharging the granules.

Provided herein is an amorphous compound represented by Formula (I): ##STR00001##
and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.

Disclosed in certain embodiments is a solid oral dosage form comprising a heat-labile gelling agent; a thermal stabilizer; and a drug susceptible to abuse.

A JAK kinase inhibitor pharmaceutical composition, containing (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide or a pharmaceutically acceptable salt thereof and a co-processed excipient, such as cellulose-lactose. The present invention has good stability, dissolution and bioavailability, and the preparation process thereof is simple and convenient.

The present invention relates to a prophylactic and/or therapeutic agent for cancer containing an mPGES-1 inhibitor as an active ingredient, the agent being useful in combination with an immune checkpoint inhibitor, and the invention has industrial applicability.