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: 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: 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: 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.

Abstract: Derivatives of N,N-diethyl-N?-phenyl-piperazine, a silent agonist of the mammalian ?7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Abstract: The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: This disclosure relates to tetrahydroisoquinolines, salts, and derivatives useful for managing mental or cognitive diseases or conditions of the brain or central nervous system. In certain embodiments, the disclosure relates to compounds and compositions having formula I: prodrugs, esters, or salts thereof, wherein the substituents are described herein.

Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, X, Y and A have the meanings given in the description—and to their use for controlling animal pests.

Abstract: Use of allosteric modulators and/or gaboxadol for the treatment of epileptic disorders in a subject in need thereof.

Abstract: The present invention provides, in certain aspects, novel syringolin analogues, In certain embodiments, the compounds of the invention are proteasome inhibitors, In other embodiments, the compounds treat or prevent a cancer such as, but not limited to, leukemia in a subject.

Abstract: The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.

Abstract: A method for treating benign prostatic hyperplasia (BPH), prostatitis, and/or prostate cancer, including the step of administering an isothiocyanate functional surfactant to a patient affected by benign prostatic hyperplasia, prostatitis, and/or prostate cancer.

Abstract: The present invention provides novel compositions and methods for using the insect neuromodulator tyramine and/or one or more derivatives thereof delivered to insect populations to control certain aspects of such populations. The amount of tyramine and/or one or more derivatives thereof delivered on a per insect basis is significantly greater than a naturally-occurring amount of tyramine normally found in insects and causes deleterious effects including mortality of certain insect life forms and disruption of the reproductive capacity of others in the population.

Abstract: The present invention discloses processes for the preparation of phospholipid-enriched dairy products as nutraceuticals for the formulation of functional foods, the processes include the steps of: combining a non-dairy-based PL-containing material, having phosphatidylserine (PS) and/or phosphatidic acid (PA) in the PL-containing material, wherein the PS and/or PA is derived in part from an enzymatically-processed lecithin as a PS-calcium and/or -magnesium salt and/or a PA-calcium and/or-magnesium salt via transphosphatidylation with phospholipase D in the presence of L-serine and a calcium and/or magnesium salt, with water and an oil component to form a paste; removing an excess amount of the water from the paste to form a PL-oil solution; and mixing the PL-oil solution with a dairy component, thereby obtaining a PL-enriched dairy product. Alternatively, the PL-oil solution has a weight-to-weight (w-w) concentration of at least about 0.01% of a residual amount of the water to the PL-containing material.

Abstract: Apparatus, systems, and methods for achieving thermally-induced renal neuromodulation by intravascular access are disclosed herein. One aspect of the present application, for example, is directed to apparatuses, systems, and methods that incorporate a treatment device comprising an elongated shaft. The elongated shaft is sized and configured to deliver a thermal element to a renal artery via an intravascular path. Thermally-induced renal neuromodulation may be achieved via direct and/or via indirect application of thermal energy to heat or cool neural fibers that contribute to renal function, or of vascular structures that feed or perfuse the neural fibers.

Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.

Abstract: Described herein are thienopyrimidine compounds of Formula (I), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the thienopyrimidine compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., brain tumors such as DIPGs) in a subject. The invention further provides an embryonic stem cell-based tumor cell model, which can be used for drug screening and disease target identification.

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 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 disclosure relates to compositions of an aqueous colloidal dispersion of hydroxypropyl methyl cellulose acetate succinate (HPMCAS), and methods for making such colloidal dispersions.

Abstract: Compounds of formula (I) defined herein are useful as a dopamine D1 receptor positive allosteric modulators (D1 PAM) and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, schizophrenia negative symptom, CIAS, Parkinson's disease, Alzheimer's disease, Huntington's disease, depression, ADHD, drug dependency, or the like.

Abstract: Methods for treating chronic myeloid leukemia (CML), e.g., BCR-ABL inhibitor imatinib mesylate (IM)-resistant CML, using combination treatments, e.g., combined treatment with a BCR-ABL inhibitor, e.g., IM, and a MEK inhibitor, e.g., trametinib.

Abstract: An oral care composition including an enzyme and an anhydrous matrix that at least partially stabilizes the enzyme. The anhydrous matrix includes a source of hydrogen peroxide, an acyl donor, a non-aqueous anhydrous liquid, and a thickener.

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 provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions, in which aldehyde toxicity is implicated in the pathogenesis, by the administration of small molecule therapeutics acting as a scavenger for toxic aldehydes.

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: A medicinal composition for diseases caused by dyslipidemia and/or autophagy dysfunction, etc., said medicinal composition comprising polyrotaxane that carries bulky substituents introduced, via intracellularly degradable bonds, into both ends of a linear molecule penetrating through plural cyclic molecules.

Abstract: The present invention relates to a combination comprising an aminothiolester compound or a pharmaceutically acceptable salt thereof, in particular the S-methyl 4-(dimethylamino)-4-methylpent-2-ynethioate or a pharmaceutically acceptable salt thereof, and more particularly the 4-(Dimethylamino)-4-methyl-2-pentynethioic acid S-methyl ester fumarate, and a compound able to increase H2O2 level in cancer cells of a subject, in particular for use for the treatment of cancer in a subject, wherein cancer cells of said subject do not overproduce H2O2 in comparison to a control value and have a level of GSH below 5 nmol for 25000 cells.

Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

Abstract: The present invention describes compounds according to formula I: and compounds according to formula II: and additional related flavonoid compounds, as well as the use of the compounds in methods for the prevention or treatment of IL-17A-mediated disease in a subject.

Abstract: The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

Abstract: The present disclosure is directed to a novel class of peptide-like oligomers called peptide tertiary amides (PTAs) and a combinatorial library of PTAs along with synthetic routes for the preparation of large combinatorial libraries of these compounds. The peptide tertiary amides provide an exceptional source of high affinity and selective protein ligands that are useful as tools for biological research and as drug leads, among others.

Abstract: Use of 5?-androstane-3?,5,6?-triol and analogs thereof in the preparation of a drug for the prophylaxis or treatment of an altitude sickness caused by hypobaric hypoxia is provided, so as to provide a new drug for the prophylaxis or treatment of an altitude sickness. Researches revealed that 5?-androstane-3?,5,6?-triol treatment can effectively reduce vasogenic edema of brain tissue of Macaca fascicularis caused by hypobaric hypoxia, reduce the increased cerebral water content, and protect from neuronal vacuolar degeneration caused by hypobaric hypoxia, therefore it can improve neurological dysfunctions caused by hypobaric hypoxia and is useful in prophylaxis or treatment of an altitude sickness.

Abstract: Small molecule integrin ligand mimetics facilitate integrin-ligand interactions, which may be used to prepare vaccines, adoptive cell therapies, immunotherapies for cancer, and a variety of other conditions. As integrin mediated cell-cell interactions are critical to antigen presentation and effector cell killing, increasing the efficiency of integrin receptor-ligand interactions will stabilize the immune synapse and improve effector functions. Compositions and methods including the mimetics enhance: (1) the priming of vaccines (including, but not limited to, cancer vaccines); (2) cytolytic activity of adoptive cell therapies (including, but not limited to ??T-cells, CTLs, NK, iNKT); (3) immunotherapies (including, but not limited to, negative checkpoint blockage strategies such as anti-CTLA-4 and anti-PD-1); and (4) biologic therapies (including, but not limited, to trastuzumab and rituxamab), whereby the mechanism-of-action includes antibody dependent cellular cytotoxicity (ADCC).

Abstract: The present invention provides a compound of Formula (I) and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds and said stereoisomers, and pharmaceutical compositions thereof, and methods for using said compounds and compositions for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Abstract: Dosage forms comprising preparations of slightly water-soluble active substances in a polymer matrix of polyether copolymers, the polyether copolymers being obtained by free radical polymerization of a mixture of from 30 to 80% by weight of N-vinyllactam, from 10 to 50% by weight of vinyl acetate and from 10 to 50% by weight of a polyether, and of at least one slightly water-soluble polymer in which the slightly water-soluble active substance is present in amorphous form in the polymer matrix.

Abstract: The disclosure provides a pediculicidal composition comprising a metal chelating agent; a carrier vehicle comprising water and an activating solvent system comprising an alcohol and a hydrocarbon. The carrier vehicle may be in the form of a solution, a cream, an ointment, a foam, a spray, an emulsion or a gel. The disclosure also provides method for use of a pediculicidal composition to treat human head lice and their eggs and methods for controlling head lice infestation.

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: The present invention provides compounds (n-3 PUFA derivatives) of formula (I): that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.

Abstract: Described herein are nitroxyl progenitor compounds, and compositions including, and methods or generating, the compounds thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.

Abstract: Methods and compositions for increasing nuclease-mediated genomic modification using DNA repair inhibitors are provided.

Abstract: Compositions and methods for inhibiting and/or sensitizing or re-sensitizing a parasite to an antiparasitic drug are provided. The compositions can comprise a rifamycin derivative or a pharmaceutically acceptable salt, hydrate, or prodrug thereof in an amount and formulation sufficient to inhibit or induce drug-sensitization in a parasite. The methods can comprise administering a rifamycin derivative or a pharmaceutically acceptable salt, hydrate, or prodrug thereof to a parasite in an amount and formulation sufficient to inhibit or induce drug-sensitization in the parasite.

Abstract: The invention pertains to a formulation comprising magnetic nanoparticles (MENPs) conjugated to or mixed with a therapeutic cargo, the therapeutic cargo comprising an HIV inhibitor, an inhibitor of BACE-1 activity or expression, and a cocaine antagonist. In one embodiment, the formulation comprises WA, miR-107, and BD1063. The MENPs conjugated or mixed with the therapeutic cargo can be encapsulated within liposomes. The liposomes can be surface modified with an affinity ligand that targets the liposomes to the brain. The invention also pertains to a method of treating an HIV infection in a subject having cocaine addiction, by administering to the subject the formulation of the invention and applying to the subject magnetic forces to guide the MENPs across the blood brain barrier and into brain parenchyma and releasing the therapeutic cargo into the brain parenchyma by applying to the subject an alternating current.