Abstract: Disclosed are methods for ameliorating glycocalyx damage by administering a neuraminidase inhibitor. Also disclosed are methods for treating endothelial dysfunction and for improving flow mediated dilation.

Abstract: Disclosed are compounds for medical uses, for example, compounds of formula Ia, wherein A1, A2, A3, A4, A5, A6, A7, R6, R7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: Provided herein are radiolabeled compounds useful for minimally invasive imaging techniques. An exemplary radiolabeled compound provided herein is useful as a radiotracer for position emission tomography imaging of voltage gated sodium channels. Methods for prepared unlabeled and labeled compounds, and diagnostic methods using the compounds are also provided.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Abstract: The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.

Abstract: An object of the present invention is to provide a drug and a method which suppress progress of disease in which the amount of amyloid ? protein in the brain is increased, such as Alzheimer's disease. 1-(3-(2-(1-Benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof has an effect of reducing the amount of amyloid ? protein in the brain parenchyma, and thus is effective as an agent for reducing the amount of amyloid ? protein in the brain. Disease in which the amount of amyloid ? protein in the brain is increased, such as Alzheimer's disease, can be prevented or treated by administering 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof.

Abstract: Silicon-based tetrahydrocannabinol derivatives and methods for their synthesis are provided, in which the derivatives contain a tetrahydrocannabinol molecule and at least one silicon-based group containing Si—O—Si bonds. The derivatives are useful in topical and dermatological compositions, have potential beneficial topical properties, and enhance solubility and compatibility in topical and dermatological formulations containing the silicon-based materials.

Abstract: Pharmaceutical compositions and methods of their use are provided for reducing inflammation in a subject, blocking leukocyte recruitment, inhibiting tumor metastasis, treating sepsis and preventing/reducing acute kidney injury.

Abstract: The present invention relates to a method for increasing the blood-brain barrier permeability, and more particularly, to a method for increasing the blood-brain barrier permeability, the method including: (S1) a step of delivering a nanogenerator carrying a nitric oxide (NO) donor to a site adjacent to the blood-brain barrier; (S2) a step of delivering a first triggering stimulus to an area where the nanogenerator has been delivered so as to release nitric oxide from the nanogenerator; and (S3) a step of allowing the released nitric oxide to activate matrix metallopeptidase-9 (MMP-9) and inducing the activated MMP-9 to weaken the tight junction between a cerebrovascular endothelial cell and another cerebrovascular endothelial cell.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The invention relates to a process for producing ethylene glycol and/or ethylene carbonate, said process comprising contacting at least a portion of a recycle gas stream comprising an alkyl iodide impurity with a guard bed system positioned upstream of an ethylene oxide reactor to produce a treated recycle gas stream, wherein the guard bed system comprises silver on alumina; contacting a feed gas stream comprising ethylene, oxygen and at least a portion of the treated recycle gas stream with an epoxidation catalyst in the ethylene oxide reactor to produce an epoxidation reaction product comprising ethylene oxide; and contacting at least a portion of the epoxidation reaction product comprising ethylene oxide with an aqueous absorbent in the presence of an iodide-containing catalyst in an absorber to produce an aqueous product stream comprising ethylene carbonate and/or ethylene glycol and the recycle gas stream comprising the alkyl iodide impurity.

Abstract: The present invention relates to a composition comprising a) at least one oil phase, b) at least one aqueous phase, c) at-least one emulsifier, wherein the at-least one emulsifier is any or combination of at-least one emulsifier agent, water with emulsification properties, oil with emulsification properties, and active ingredient with emulsification properties; and d) optionally, one or more biologically active ingredients. The present invention also relates to use of the composition for personal care, pet care, home care, deodorants, pesticides, moisturizers, disinfectants, cleansers, therapeutic devices, topical supplements and/or nutrition. The present invention also relates to a method for preparing such a composition.

Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII and, the methods for the treatment of oral infectious diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral infectious diseases.

Abstract: Disclosed herein is a ready-to-use liquid, injectable formulation comprising lidocaine and epinephrine. Also disclosed herein is a process for preparing a ready-to-use liquid formulation comprising lidocaine and epinephrine, as well as methods for using the ready-to-use liquid formulation.

Abstract: The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, RCM reactions. Specifically, the subject invention provides the synthesis of the first catalytically active V oxo alkylidene, VO(CHSiMe3)(PEt3)2Cl, which exhibits superior performance compared to other analogs.

Abstract: The invention provides an aqueous pharmaceutical solution for use in the treatment of diseases of the central nervous system (CNS), the solution comprising at least 5 mg/ml dissolved levodopa, and having a pH in the range of 3.0 to 8.5. Said solution is provided by mixing a) an aqueous stock solution comprising levodopa, said stock solution having a pH of less than 2.8 at 25° C. and b) an aqueous buffering solution, for increasing the pH of said stock solution, said buffering solution having a pH of at least 4.0 at 25° C. The aqueous pharmaceutical solution is administered to a subject suffering from a disease of the central nervous system (CNS) shortly after mixing of the aqueous stock solution and the aqueous buffering solution. Furthermore, the invention provides a kit for administration of aqueous pharmaceutical solutions to subjects suffering from diseases of the central nervous system (CNS).

Abstract: Disclosed are compounds of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and to a process for the preparation of the compounds: R1 is independently selected from hydrogen atom, amine group, monocyclic or bicyclic aliphatic, aromatic, heteroaliphatic or heteroaromatic ring. R2 is independently selected from monocyclic or bicylic aliphatic, heteroaliphatic, aromatic or heteroaromatic ring, C1-C6 alkyl, alkenyl or alkynyl chain. n is 1 or 2; preferably n is 1. m is 0, 1 or 2; preferably m is 0. R3 and R4 can be, independently, —H, —F, C1-C4 alkyl, —OH, —OC1-C4 alkyl; preferably they are both —H. X is O or S. R5 is —H or —CH3 optionally substituted by one or more fluorine atoms; preferably R5 is hydrogen. The compounds can be used in the treatment of conditions or diseases mediated by P2X7 receptor.

Abstract: The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXR? and/or LXK?) and act preferably as inverse agonists of LXR.

Abstract: The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R1? wherein R1 contains from 1 to 7 atoms other than hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.