The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.

The present invention relates to a cocrystal of beta-sitosterol or a pharmaceutically acceptable ester thereof or an edible acceptable ester thereof and an organic carboxylic acid coformer, an hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol and a combination that comprises a cocrystal of beta-sitosterol and an organic carboxylic acid; and the hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol. It also relates to processes for their preparation, and compositions containing them, as well as their use as a medicament or dietary supplement or functional food, and in particular in the prophylaxis and/or treatment of a disease or conditions that involves an alteration of lipid metabolism, circulating levels of lipids in the blood and/or lipid composition in tissues and organs.

The invention relates to besylate salts of the compound of formula (I):

##STR00001##

Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.

The present invention discloses salts of a Compound 1:

##STR00001##

useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.

The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.

Pharmaceutical formulations with a tropomyosin-related kinase inhibitor (“Trk inhibitor”) are disclosed. The pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine in microcrystalline suspension formulations in its monohydrate form, which shows improved characteristics over the anhydrate form, and in extended release formulations. The extended release pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine-loaded microspheres.

Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A.sub.2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like:

##STR00001##

(wherein R.sup.1 represents furyl, R.sup.4, R.sup.5 and R.sup.6 are the same or different and each represents lower alkyl or aryl, R.sup.2 represents pyridyl or tetrahydropyranyl, and X.sup.1 represents halogen).

The present invention provides crystalline forms of efinaconazole, including crystalline efinaconazole forms designated herein as Form A, Form B and Form C, crystalline efinaconazole p-toluenesulfonate salt designated herein as Form I, and processes for their preparation.