C07B2200/13

CRYSTAL OF AMMONIUM N-ACETYLNEURAMINATE ANHYDRATE, AND PROCESS FOR PRODUCING SAME
20180002364 · 2018-01-04 · ·

According to the present invention, a crystal of ammonium N-acetylneuraminate anhydrate, and a process for producing a crystal of ammonium N-acetylneuraminate anhydrate, comprising adding or adding dropwise a solvent selected from the group consisting of alcohols and ketones to an aqueous N-acetylneuraminic acid solution containing an ammonium-containing compound and having a pH of 3.0 to 9.0 to precipitate a crystal of ammonium N-acetylneuraminate anhydrate, and collecting the crystal of ammonium N-acetylneuraminate anhydrate from the aqueous solution, can be provided.

METHODS FOR CHIRAL RESOLUTION OF TROLOX

The invention relates to methods of separating Trolox isomers (R)-Trolox and (S)-Trolox, comprising: (a) contacting a mixture of (R) and (S)-Trolox with a resolving agent selected from the group consisting of (1S,2S)-(+)-Pseudoephedrine, (R)-(+)-2-Amino-3-phenyl-1-propanol, (1R,2R)-(−)-Pseudoephedrine, and (S)-(−)-2-Amino-3-phenyl-1-propanol, wherein the resolving agent forms a solid salt with one of (R)-Trolox and (S)-Trolox, and substantially does not form a solid salt with the other; and (b) separating the solid salt from the Trolox isomer that did not form the solid salt with the resolving agent.

COMPLEXES OF CELECOXIB AND ITS SALTS AND DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Disclosed herein are stable complexes with controlled particle size, increased apparent solubility and increased dissolution rate comprising as active compound Celecoxib, its salts, or derivatives thereof, which is useful in the treatment of osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, acute pain especially in cancer related acute pain, primary dysmenorrhea. More specifically, the complexes possess instantaneous redispersibility, increased apparent solubility and permeability that provide faster onset of action for acute pain relief and lower GI related side effects. Further disclosed are methods of formulating and manufacturing the complexes described herein, pharmaceutical compositions, and uses and methods of treatment.

ASYMMETRIC SYNTHESIS OF FUNAPIDE

This invention is directed to asymmetric synthesis of funapide, which is useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS

The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
20180009824 · 2018-01-11 ·

Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.

HIGH-SOLUBILITY ACETONE-ADDED PYRROLOQUINOLINE QUINONE SALT
20180009803 · 2018-01-11 · ·

There are provided an alkali metal salt of 5-hydroxy-4-oxo-5-(2-oxopropyl)-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid, a method for producing the alkali metal salt, and a cocrystal comprising the alkali metal salt.

Crystalline composition of tildacerfont and methods of use and preparation thereof

Described herein are crystalline composition comprising a Corticotropin-releasing hormone receptor 1 (CRF1) antagonist, such as Compound 1: ##STR00001##
methods of making such crystalline composition, pharmaceutical compositions and medicaments comprising such crystalline composition, and methods of using such crystalline composition in the treatment of conditions, diseases, or disorders that would benefit from modulation of CRF.

HYDROXYETHYL SULFONATE OF CYCLIN-DEPENDENT PROTEIN KINASE INHIBITOR, CRYSTALLINE FORM THEREOF AND PREPARATION METHOD THEREFOR
20180009804 · 2018-01-11 ·

Provided are a hydroxyethyl sulfonate of a cyclin-dependent protein kinase inhibitor, a crystalline form thereof and a preparation method therefor. Specifically, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydroxyethyl sulfonate (compound of formula (I)), a crystal form I thereof and a preparation method therefor are provided. Crystal form I of the compound of formula (I) has good chemical and crystalline stability, low toxicity, and low residual crystallization solvent. Therefore, the crystal form I can be used in improved clinical therapy.

##STR00001##

Crystal form of ethyl (S)-3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate hydrochloride

The present invention provides a crystalline form of a benzodiazepine derivative hydrochloride of Formula I or its ethanolate, wherein R is methyl or ethyl. The present invention also provides a method of preparing the crystal form of the compound of Formula I and a pharmaceutical composition comprising the crystal form. ##STR00001##