Abstract: The present invention is directed to 1, 2, 5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2, 3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1, 2, 5-oxadiazole derivatives.

Abstract: Disclosed are methods for separating, recovering, and purifying tetrahydrocannabinolic acid (THCA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in a selected C5-C7 hydrocarbon solvent, adding thereto a selected amine to thereby precipitate a THCA-amine salt therefrom, dissolving the recovered THCA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified THCA-amine salt therefrom. The recrystallized THCA-amine salt may be decarboxylated to form a mixture of ?9-tetrahydrocannabinol (?9-THC) and amine. The ?9-THC amine mixture may be acidified to separate the amine from ?9-THC. The recovered ?9-THC may be concentrated to produce a highly purified ?9-THC. Also disclosed are THCA-amine salts produced with amines selected from groups of diamines, amino alcohols, and tertiary amines.

Abstract: A novel multi-arm polyethylene glycol (PEG) (I) and preparation method thereof. Active derivatives (II) based on the multi-arm PEG. Gels formed of the active derivatives. Drug conjugates formed of the active derivatives and drug molecules and uses thereof in medical preparation. The multi-arm PEG is formed by polymerizing ethylene oxide with pentaerythritol oligomers as initiator, wherein PEG is the same or different and is a —(CH2CH2O)m-, the average value of m is an integer of 3-1000, l is an integer more than or equal to 2. An 8-arm PEG is preferred, wherein l is equal to 3. The active derivatives (II) comprise link groups X attached to PEG and active end groups F attached to X.

Abstract: Inhibitors of ALCAT1 are described having the general formula: (I). These compounds offer a treatment for aging and age-related diseases.

Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

Abstract: The present invention provides compounds of formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.

Abstract: To provide a medical device including a substrate and a hydrophilic polymer layer formed on at least a part of the substrate, which satisfies the following conditions (a) to (d): (a) a polymer constituting the hydrophilic polymer layer is a hydrophilic polymer having an acidic group; (b) the hydrophilic polymer layer has a thickness of 1 nm or more and less than 100 nm; (c) a number ratio of basic group/acidic group of the hydrophilic polymer layer is 0.2 or less; and (d) a liquid film retention time at 40 minutes after ultrasonic cleaning in a phosphate buffer solution is 15 seconds or more. The present invention provides a medical device in which a surface of a substrate is hydrophilized, and a method for manufacturing same by a simple method.

Abstract: Disclosed are compound and methods of using the compounds for modulating ornithine aminotransferase (OAT) activity. The disclosed compound are characterized as analogs of 3-amino-4-(propan-2-ylidene)cyclopentane-1-carboxylic acid which may be formulated as therapeutic agents for treating diseases and disorders associated with ornithine aminotransferase (OAT) activity such as hepatocellular carcinoma and other cancers.

Abstract: A bioadhesive includes a crosslinked biodegradable hydrogel that includes a plurality of oxidized, acrylated or methacrylated, natural polymer.

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.

Abstract: An object of the present invention is to provide a crystal of L-alanyl-L-glutamine having a low loose specific volume, and a method for producing the same. The present invention relates to a crystal of L-alanyl-L-glutamine in which the loose specific volume is 5.0 mL/g or less, and a method for producing the same.

Abstract: The invention generally relates to compositions comprising degradable polymers and methods of making degradable polymers. Specifically, the disclosed degradable polymers comprise a biodegradable polymer backbone, a nitric oxide linker moiety, and a nitric oxide molecule. 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 invention.

Abstract: Prodrugs of glutamine analogs, such as prodrugs of acivicin, are disclosed.

Abstract: The disclosure provides chemical compounds possessing therapeutic and/or protective properties against oxidative damage. Methods of making such therapeutic and/or protective compounds and associated compositions are also provided, as are methods for their use, which include protecting cells from oxidative damage and/or inhibiting production of ROS in a cell or subject, as well as preventing or reducing the extent of tissue damage caused by an ischemic event in a subject at elevated risk of such an event.

Abstract: The invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms.

Abstract: A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

Abstract: A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

Abstract: The present invention relates to macromolecular transition metal complexes, characterized by having the general formula (I), to the process for their preparation, and to bidentate and monodentate macroligands. The invention also refers to pharmaceutical compositions and medicaments containing said macromolecular transition metal complexes, and to the use of said pharmaceutical compositions, medicaments and macromolecular transition metal complexes for cancer therapy and/or cancer prevention, as antitumor agent in solid tumors, liquid tumors and/or metastases and/or as radiosensitizer agents.

Abstract: The present invention inter alia relates to a method of promoting collateral circulation comprising the step of exposing a subject to a therapeutically effective amount of an NO donor wherein the therapeutically effective amount of the NO donor promotes arteriogenesis sufficient to augment collateral circulation in a physiological or pathological condition.

Abstract: The present invention relates to compounds for use in the prevention and/or treatment of PAR-related diseases, such as for example: pain and ocular disorders. More in particular, the present invention provides bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of pancreatitis-related pain, IBS (irritable bowel syndrome), IBD (inflammatory bowel disease), dry eye disease and conjunctivitis sicca. These inhibitors were found to have a different inhibitory profile compared to diphenyl guanidinophenylethylphosphonates leading to a more pronounced effect on these conditions.