Abstract: There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, ring A, m and n have meanings as provided in the description.

Abstract: Provided are a novel derivative of ?-apopicropodophyllin and a method of preparing the same, and more particularly, a compound represented by Formula 1 below, which is a novel derivative of ?-apopicropodophyllin derived from podophyllotoxin, which is an anticancer agent, a method of preparing the same, and a composition for treating cancer, which includes the compound. In Formula 1, R is a C2 to C10 alkyl group, a C2 to C10 alkyl group containing an allyl- or alkyne, a —[CH2]n—C3 to C8 cycloalkyl group, a substituted or unsubstituted —[CH2]n-phenyl group, a substituted or unsubstituted —[CH2]n—C5 to C6 heteroaromatic group, a —C(?O)—C1 to C8 alkyl group, a substituted or unsubstituted —C(?O)—[CH2]n-phenyl group, or a substituted or unsubstituted —C(?O)—[CH2]n—C5 to C6 heteroaromatic group, wherein n is an integer of 0 to 6.

Abstract: The present invention provides triazole carboxylic acids and related compounds, as well as pharmaceutically acceptable salts thereof, which are useful as glycolate oxidase inhibitors. Pharmaceutical compositions and methods for treating primary hyperoxaluria, type I (PH) and kidney stones are also described.

Abstract: The invention concerns a method for isolation of cytisine from plant material. The method according to the invention, consists in extraction of the plant raw material by lower alcohol, acidified with mineral acid to pH within a range 1.5-3.5. The combined alcohol-aqueous extracts are concentrated under vacuum distillation till the alcohol is eliminated and after filtration they are extracted with chloroform, methylene chloride, butyl acetate or normal butanol in a ratio of 1:1. The purified from ballast substances acid aqueous concentrate is alkalized to pH 9-12 with alkaline hydroxide or ammonium hydroxide and the resulting alkaline aqueous concentrate is extracted at least twice with chloroform, methylene chloride, butyl acetate or normal butanol in a ratio of concentrate:extractant of 1:5 to 1:10. The combined organic extracts are evaporated to dryness, then acetone or ethyl acetate are added to obtain a suspension which is allowed to crystallize completely at 5-10° C., then it is filtered and dried.

Abstract: The present invention relates to novel methods for the preparation of 1,3-benzo-dioxole heterocyclic compounds and intermediates for the same. The compounds are useful as PDE4 inhibitors.

Abstract: The present invention includes compositions and methods for treating a subject afflicted with a neurodegenerative disorder or disease by determining that the subject is in need of treatment for the neurodegenerative disorder or disease; and administering to the subject an amount of an effective amount of a compound comprising a flupirtine derivative as disclosed herein.

Abstract: There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the ring containing Q1 to Q5, and the groups R1, R2 and R3, have meanings as provided in the description.

Abstract: Disclosed herein are compounds, 3,4,6,8-substituted-2-([1?-biphenyl]-4-yl)quinoline analogs, that are inhibitors of dihydroorotate dehydrogenase (DHODH) with improved pharmacokinetic properties. The disclosed compounds can be used in the treatment of a variety of disorders and diseases in which inhibition of DHODH can be clinically useful, including cancer, such as a hematological cancer, including acute myeloid leukemia (AML); graft-versus-host-diseases; autoimmune disorders; and disorders associated with T-cell proliferation. The disclosed compounds can demonstrate flip-flop kinetics when administered orally, i.e., pharmacokinetics in which the rate of absorption, rather than the rate of elimination, dominates the pharmacokinetics. The disclosed compounds can demonstrate a sustained pharmacokinetic profile instead of an immediate release profile. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: Provided herein are cyclic plasmenylethanolamines and plasmalogen precursors of formula A, wherein R1 and R2 are each, independently, a saturated, unsaturated, or polyunsaturated hydrocarbon group. Methods and uses thereof in the treatment of plasmalogen deficiency are also described. Cyclic plasmenylethanolamines described herein may act as plasmalogen precursors which, following administration, may be converted to at least one plasmalogen species, thereby elevating the plasmalogen level in a subject.

Abstract: Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.

Abstract: Pharmaceutical compositions that include inhibitors of mitochondrial fission are described for the treatment and/or mitigation of cancer, pulmonary arterial hypertension, cardioprotection, stroke, coronary heart disease, neurological disorder, a neurodegenerative disease, Parksinonism, Huntington's Chorea, Alzheimer's disease, diabetic cardiomyopathy, fatty liver diseases, non-alcoholic fatty liver diseases, or alcohol-related liver disease.

Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.

Abstract: The invention relates to 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

Abstract: The invention provides novel pyridylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and X are as defined in the specification.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Abstract: The present document describes methods of using compositions for inhibiting biofilm formation, or disrupting existing or developing biofilms in a subject, which composition comprises at least one chromophore and a pharmacologically acceptable carrier.

Abstract: The present invention relates to an inhibitor of miR-671-5p for use in a method of preventing or treating fibrosis. Further, the present invention encompasses a kit comprising said inhibitor of miR-671-5p. The present invention also relates to an in vitro method for identifying a compound for preventing or treating fibrosis.

Abstract: The invention provides compounds of formula (I): and salts thereof wherein R1-R5 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Abstract: Forms of 6-(3-chloro-4-cyclopropoxyphenyl)pyrimidine-4-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I and salts or co-crystals thereof.