Abstract: Provided herein are methods, devices and compositions for assessing neuromodulation efficacy based on changes in the level of one or more biomarkers in plasma or urine collected from a human subject following a renal neuromodulation procedure.

Abstract: The present invention refers to new purified compositions of long chain polyunsaturated fatty acids, or their salts or esters, characterized by being essentially free from other usually present—but structurally different—components, such as furan fatty acids, phytanic and pristanic acids, squalene, and some oligomers, as well as several “persistent” environmental pollutants, such as polychlorinated dibenzo-dioxins and polychlorinated dibenzo-furans, polychlorinated biphenyls, polybrominated diphenyl-ethers, polycyclic aromatic hydrocarbons, and others, which are also usually present and extremely toxic. The invention also refers to the purification method to obtain said compositions and the use thereof as food, food for special medical use, food and diet supplement, and drug.

Abstract: The use of direct factor Xa inhibitors, administered in a dose sufficient to reduce the activity of factor Xa to about 25% less than normal or lower, has the effect of preventing the onset of atherosclerosis, and stabilizing atherosclerotic lesions, and preventing the occurrence or recurrence of atherosclerotic events.

Abstract: The present invention provides pharmaceutical composition of antineoplastic alkylating agent in oral suspension dosage form. The oral suspension composition comprises of alkylating agent with other pharmaceutical excipients such as vehicle, preservative, antioxidant, suspending agent, surfactant, sweetener and flavouring agent. The present invention is an oral suspension having improved stability and palatability. The present invention also provides oral solution with flavor that has masked bitter taste of the drug. Further, the present invention also provides a process for preparation thereof.

Abstract: The present invention relates to a coumarin (keto) oxime ester compound of formula (I), wherein n and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification. The compound has strong ultraviolet absorption in the range of 300 to 450 nm. After absorbing light energy, it can quickly transfer energy and continuously initiate polymerization. It has obvious advantages in terms of photosensitivity and pattern integrity, and is very suitable for radiation curing by UV-LED light source. In addition, the compound of formula (I) also has good thermal stability. The present invention also relates to a method for preparing the compound of formula (I) and use of the compound. The compound is suitable as a photoinitiator in a UV-LED light curing system and is suitable for the radiation wavelength of UV-LED light curing.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention provides 4-anilino-3-quinolinecarbonitriles compounds useful for treating a subject having an BcrAbl positive leukemia that is resistant to imatinib.

Abstract: The invention provides an amorphous metal-organic framework for use in methods of treatment. The amorphous metal-organic framework may hold a component for delivery. The amorphous metal-organic framework is obtained or is obtainable by amorphization of a crystalline amorphous metal-organic framework holding the component. The amorphous metal-organic framework may be a zirconium-containing or a bismuth-containing metal-organic framework, such as a framework having arylcarboxylate ligands, such as benzenedicarboxylate ligands.

Abstract: The present invention relates to substituted methanopyrido [2,1-a]isoindolones of formula I, wherein, R1 is selected from phenylsulfonyl or p-toluenesulfonyl; and n=1, 2, 3; their derivatives, stereoisomers, pharmaceutically acceptable salts and pharmaceutically acceptable compositions having potential muscarinic acetylcholine receptor modulator activity.

Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6, R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

Abstract: Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.

Abstract: A method for amelioriation of, or prophylaxis against, a viral infection comprising administering to a patient in need of treatment a therapeutically effective amount of 5 aminolevulinic acid, optionally with at least one of cucumarin nano, zinc, vitamin C and methylene blue, and compositions thereof. Such compositions may be used for the treatment of coronavirus infections, including the SARS-CoV-2 virus, and/or rhinoviruses.

Abstract: The present disclosure relates to compositions and methods for enhancing mosquito feeding.

Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.

Abstract: The invention relates to use of the trans-(E) isomer or isomeric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders.

Abstract: The technical field of the invention is in pharmaceutical compounds and methods. In an aspect, the disclosure provides macrolide compounds suitable for use as antifungal agents, as well as methods for their use and compositions containing the same.

Abstract: The present invention provides therapeutic combinations of 5-aminolevulinic acid, with at least one of: Vitamin C, curcumin, zinc, and methylene blue for the treatment of coronavirus infections, including the SARS-CoV-2 virus, and/or rhinoviruses. Optionally such compositions may comprise other dietary supplements and one or more pharmaceutically acceptable excipients and also process for preparing it. The composition can also include other antiviral agents.

Abstract: The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutaric acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.

Abstract: The present disclosure provides methods for treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. In some embodiments, the method comprises lowering high sensitivity CRP (hs-CRP) levels in a subject including, for example, a subject with a HbA1c value of about 5.00%-8.50% or at least about 6.8%.

Abstract: The present disclosure relates to the control of fungal infection of horn-like envelopes covering dorsal and terminal phalanges in humans and animals and related cerebral protrusions in animals as well as keratin comprising material on surfaces of humans and animals. Agents and natural and synthetic formulations and extracts useful for the control of fungal infection of these envelopes and related protrusions and keratin comprising material are also encompassed by the subject disclosure. In an embodiment, the present disclosure teaches the treatment of fungal infection of nails and in particular onychomycosis in humans.

Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.

Abstract: The present invention relates in part a to multiparticulate sprinkle dosage form comprising duloxetine or a pharmaceutically acceptable salt thereof, having higher acid resistance as compared to commercially available delayed release formulations. It further relates to various methods of administering the said multiparticulate sprinkle dosage forms.

Abstract: A crystalline form of Mod. I of Formula I: And, a process for the preparation of the crystalline form and a pharmaceutical use of the crystalline form.

Abstract: A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Abstract: There are provided, inter alia, compounds and methods useful for the treatment of neurological conditions, such as neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

Abstract: Compounds of formula (I): wherein: R1 is butoxy or methylbutoxy; R2 is a group having the structure: where n is an integer having a value of five; Het is a six-membered saturated heterocycle containing five carbon atoms and one nitrogen atom, wherein Het is attached to the —(CH2)n— moiety at the carbon 4 position of the heterocycle; and R3 is hydrogen; or pharmaceutically acceptable salts thereof; and their use as vaccine adjuvants and in the treatment of various disorders.

Abstract: Methods for preventing or treating subjects having cancer based on the identification of pharmaceutical agents that target cancer stem cells (CSCs) have been identified. These methods include administering to the subject an effective amount of a COX2 inhibitor and an effective amount of a YAP1 inhibitor. In addition, methods of enhancing chemotherapeutic responses in cancer patients have been discovered and are described herein.

Abstract: A method for catalytically converting a dihydrotetrazine 1 into a tetrazine 2, wherein one R group on the dihydrotetrazine 1 is a substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl, or heteroatom-containing group, and the other R group is selected from the group consisting of H and substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl,- or heteroatom-containing groups; 1, 2 wherein the method comprises oxidizing dihydrotetrazine 1 in a reaction medium in the presence of a catalyst and a stoichiometric oxidant.

Abstract: The present disclosure provides a method for the treatment of Parkinson's disease comprising simultaneously or sequentially administering to a patient in need of treatment of Parkinson's disease a dosage form comprising (i) levodopa in an amount ranging from 50 mg to 300 mg, (ii) carbidopa in an amount ranging from 25 mg to 150 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and (iii) entacapone in an amount ranging from 50 mg to 300 mg, wherein the proportion of entacapone to carbidopa in said dosage form ranges from 0.3:1.0 to 3.2:1.0 by weight, a moderately potent COMT inhibitor in an amount ranging from 25 mg to 200 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.16:1.0 to 3.08:1.0 by weight, or a highly potent COMT Inhibitor in an amount ranging from 1 mg to 100 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.006:1.0 to 1.54:1.0 by weight.

Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.

Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract: Described are compositions comprising imino sugar acids for the treatment of energy utilization disease (e.g. metabolic syndrome, including any disease or disorder associated therewith, for example central obesity, elevated levels of triglycerides and diabetes, including type 1 diabetes, type 2 diabetes and insulin resistance), processes for producing said compositions from various plant sources, together with various products, compounds, compositions, medical uses and methods based thereon.

Abstract: Disclosed herein are methods for treating subjects with breast cancer, comprising determining a therapeutic regimen for cancer by measuring the level (amount) of proteins of one or more biomarkers. Also disclosed are methods of treating a subject with breast cancer by predicting or assessing a therapeutic outcome for subject.

Abstract: The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists.

Abstract: The present invention provides dietary formulations comprising polyunsaturated fatty acids and vitamin E. The present invention further provides methods of treating various conditions, generally involving administering to an individual in need thereof an effective amount of a subject dietary formulation.

Abstract: The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders

Abstract: The present invention relates to a mixture comprising (i) one or a plurality of 1,2-alkane diols with 5 through 8 carbon atoms and (ii) one or a plurality of ammonium-, sodium- or potassium-Ralk-sarcosinates, wherein the structural element Ralk represents alkanoyl, alkenoyl or alkadienoyl with 12 through 22 carbon atoms, and optionally (iii) one or a plurality of sodium- or potassium-C10-C16-alkyl-sulfoacetates. The invention further relates to particular compositions and cosmetic preparations, in particular body care products, containing said mixture or composition and methods of production thereof. The present invention further relates to the use of said mixture as solubilizer and for increasing the transparency or decreasing the turbidity of a preparation containing one or a plurality of further organic substances.

Abstract: The invention provides compositions and methods to treat a hyperproliferative disorder with phenyl butyric acid (PBA) or a pharmaceutically acceptable salt thereof and an anti-cancer composition.

Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.

Abstract: Methods for priming of vaccines including administering to a patient a composition including one or more integrin activating compounds capable of adjuvanting an antigen and capable of adjuvanting one or more antigens contained in a vaccine preparation.

Abstract: Disclosed herein are methods of treating pulmonary hypertension, including pulmonary arterial hypertension, by administering to a patient in need thereof an effective amount of temozolomide, optionally in conjunction with one or more additional therapeutic agents. Compositions and kits including temozolomide for use in treating pulmonary hypertension, including pulmonary arterial hypertension, are also disclosed.

Abstract: Compositions including one or more antigens and one or more integrin activating compounds capable of adjuvanting the one or more antigens contained and increasing an immune response to the one or more antigen in a vaccine preparation.

Abstract: In one aspect, provided herein are methods for predicting the responsiveness of DLBCL patients to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classifiers that correlate with responsiveness to one of these drugs. In another aspect, provided herein are methods for treating a DLBCL patient determined to be responsive to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classifiers (or output thereof) that correlate with responsiveness to one of these drugs.

Abstract: Pyrimidine-thiazolidinone derivatives may be used for preventing or treating diseases in humans or animals, and have demonstrated efficacy specifically in treating type-2 diabetes. Methods of synthesizing the pyrimidine-thiazolidinone derivatives, described herein, can provide high yields in a short time and with high purity. The pyrimidine-thiazolidinone derivatives demonstrate improved hypoglycemic activity compared to most anti-diabetic drugs currently available.

Abstract: The present invention pertains to specific clonidine and/or clonidine derivatives for use in the prevention and/or treatment of adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. It also pertains to the use of this clonidine and/or clonidine derivative for the manufacture of a pharmaceutical composition intended to prevent and/or alleviate the adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. This invention is further directed to a kit comprising: (a) a clonidine and/or clonidine derivative, and (b) at least one alkylating chemotherapeutic agent, as a combined preparation for simultaneous, separate or sequential use in the treatment of cancer.

Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.