Abstract: Novel co-crystal and eutectic crystal of kojic acid and a co-former that are excellent in physical properties are provided. In one aspect, novel co-crystals of kojic acid and a co-former that is maltol or ethyl maltol are provided. In another aspect, novel crystal of a eutectic mixture of kojic acid and a co-former that is selected from the group consisting of, maltol, ethyl maltol, methyl paraben and propyl gallate are provided. Methods for producing the novel co-crystal or eutectic crystal are also described. The novel co-crystals and eutectic crystals may be included in a pharmaceutical composition, a health food product or a medical food product for the treatment and/or prophylaxis of a neuropsychiatric disorder.

Abstract: Disclosed are small molecule antagonists of human ?4?7 integrin, and methods of using them to treat a number of diseases and conditions.

Abstract: Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).

Abstract: Disclosed is a compound as shown in formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and the present invention relates to the use of same in the preparation of a drug for treating FXR-related diseases.

Abstract: Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-? so as to effectively treat cancer and inflammatory diseases.

Abstract: The present application belongs to the field of medicine. In particular, the present application relates to a diarylthiohydantoin compound as an androgen receptor antagonist or a pharmaceutically acceptable salt thereof, a preparation method of the same, a pharmaceutical composition comprising the compound, and a use thereof in treating a cell proliferative disease mediated by androgen. The compound of the present application has good antagonistic effect on androgen receptor and exhibits excellent antitumor effect.

Abstract: A heteroaryl[4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and medical uses thereof are provided. Specifically, a heteroaryl[4,3-c]pyrimidin-5-amine derivative of formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and uses thereof as therapeutic agents are provided. In particular, the provided compounds can be used as A2a receptor antagonists and for treatment of conditions or symptoms that are ameliorated by inhibiting the A2a receptor. The various substituent groups in the formula (I) have the meanings as described in the specification.

Abstract: Provided herein are processes for preparing 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide.

Abstract: Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.

Abstract: The present invention provides compounds of the Formula wherein L is selected from the group consisting of —CH2NHCH2—, —CH2NH—, —NH—, —S—, —S(O)—, —S(O)2—, —O—, —OCH2—, —OCH2CH2O—, —NHSO2NH—, or a pharmaceutically acceptable salt thereof; a compound of the formula: processes for preparing the compounds and their salts, a pharmaceutical composition, and methods of treating patients in need of such treatment.

Abstract: The present invention relates to a method of separating racemic nicotine of Formula (1-a) as a mixture of the (R)- and (S)-enantiomers into the enantiomerically pure (S)- and (R)-nicotine represented by Formula (1-b) and (1-c), by adding a mixture of the L- and the D-enantiomer of a O,O?-disubstituted tartaric acid, wherein the molar ratio of the L- to the D-enantiomer is from 80:20 to 95:5, and obtaining the (S)-nicotine of formula (1-b), or by adding O,O?-dibenzoyl-D-tartaric acid and obtaining the (R)-nicotine of formula (1-c).

Abstract: The Present Invention relates to process for the preparation of 7-{4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one represented by the following structural formula-1.

Abstract: The present invention relates to certain novel substituted thiophene compounds and the finding that they display useful efficacy in the inhibition of the p38? MAPK enzyme. This provides for use of the compounds in various treatment methodologies related to MAPK inhibition, including the treatment of inflammation.

Abstract: The present invention relates to cyclopentane compounds of Formula (I), physical forms thereof, processes for their production and their use in medicine.

Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.

Abstract: Halogenated analogs of 5-aza-2?-deoxycytidine, such as halogenated analogs of 5-aza-4?-thio-2?-deoxycytidine (5-aza-T-dCyd) are described. Pharmaceutical compositions including a halogenated analog and methods of using the halogenated analogs to inhibit neoplasia are described.

Abstract: The invention relates to process for the preparation of grapiprant and its intermediates thereof. The invention also relates to grapiprant having a purity 98% or more and compounds of Formula (A), (B), (C) and (D) in an amount of 0.5 or less, relative to grapiprant, by area percentage of HPLC. The invention also relates to an amorphous form of grapiprant and process for preparation thereof.

Abstract: The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2 X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

Abstract: The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.