Abstract: The invention provides an artificially synthesized single sphingosine lipid and use of delivering a nucleic acid thereof.

Abstract: Compositions and methods for treatment of cancer according to aspects of the present disclosure comprise compounds comprising or consisting of: structural formula (I) or (II) disclosed herein, or a salt, isomer, or derivative thereof.

Abstract: Provided herein are compounds and compositions thereof for modulating S1P5. In some embodiments, the compounds and compositions are provided for treatment of neurological diseases.

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: An oil-based formulation comprising a cannabinoid and pico size carbon particles. The formulation is suitable for administration to a patient having a medical condition requiring the use of cannabinoid.

Abstract: The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.

Abstract: Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.

Abstract: Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

Abstract: The present invention relates to novel hydrochloride salt forms of N-(2?,4?-difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1?-biphenyl]-3-yl)cyclopropanesulfonamide (I). Compound (I) is a selective inhibitor of FGFR/VEGFR kinase families and is useful in the treatment of cancer.

Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

Abstract: Forms of (S)-2-hydroxy-6-((4-(2-(2-hydroxyethyl)nicotinoyl)morpholin-3-yl)methoxy)benzaldehyde (Compound I), or salts or solvates thereof, were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms of Compound I.

Abstract: An object of the present invention is to provide an ascorbic acid formulation that can be prepared by a simple method, and that has a reduced unpleasant taste and coloration. The inventors found that an ascorbic acid formulation that is in the form of a water-in-oil type emulsion, that comprises an aqueous phase with a pH of 4 or more and an average particle size of 300 nm or less, and that has a mass ratio of water/ascorbic acid of 0.05 to 0.40 has a reduced unpleasant taste and coloration; and accomplished the present invention. Additionally, the present invention can be prepared by a simple method.

Abstract: A memantine paroxetine cocrystal salt and its preparation method, pharmaceutical composition and application thereof are provided. The cocrystal salt of the invention is memantine paroxetine sulfate hydrate. Its mechanism of action is 5-HT inhibitor and NMDA receptor antagonist. It is a multi-target drug. The preliminary pharmacokinetic experiments showed that the main pharmacokinetic parameters of cocrystal salt and memantine, such as T1/2, Tmax, Cmax and AUC(0-?), were significantly different. The results also showed that cocrystal salt could improve drug absorption, blood drug concentration, bioavailability and curative effect. This provides a material basis for reducing dosage and adverse drug reactions. In addition to that the cocrystal salt of this invention can be used as a multi-target drug, it can also combine with other drugs of different action mechanisms to form compound preparations or be used in combination, so as to obtain unexpected clinical efficacy.

Abstract: Provided is a crystal of a specific oxazole compound that has specific inhibitory activity against PDE4, and that shows excellent stability. Specifically, provided is a crystal of an oxazole compound represented by formula (5) wherein the crystal has peaks at diffraction angles 2?(°) of 9.6±0.2, 19.1±0.2, and 21.2±0.2 in an X-ray powder diffraction pattern measured using CuK? characteristic X-rays.

Abstract: The present invention relates to compounds derived from ursodeoxycholic acid of formula (I), to methods for obtaining same, as well as the use thereof in the treatment of polycystic diseases, particularly autosomal dominant polycystic liver disease, autosomal dominant polycystic kidney disease, or autosomal recessive polycystic kidney disease.

Abstract: A method of treating a subject suffering from an ischemic disease associated with Ca2+ overload is provided, the method including administering to the subject an effective amount of an inhibitor of Ataxia telangiectasia and Rad3-related (ATR) kinase. Also provided is a method of treating a subject suffering from acute ischemic stroke, the method including administering to the subject an effective amount of the ATR kinase inhibitor berzosertib.

Abstract: Disclosed are PPAR receptor modulators and their uses in medicine. The novel agonists for PPAR-? were found by screening molecules through a chemoinformatics-based model. The novel agonists for PPAR-? are proposed for use in medicine.

Abstract: Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

Abstract: The present disclosure provides methods of synthesizing a compound of Formula (P)-I. The method proceeds through several different pathways including several novel chiral separations, a Sonogashira coupling, a zinc mediated reductive cyanation, as well as through various halide containing intermediates. Also disclosed is the multi-kilogram preparation of several novel intermediates.