Abstract: The disclosure provides for multi-targeting agents that assist in the targeted removal of amyloid beta plaques from the brain and surrounding vasculature of subject's with Alzheimer's disease, and methods of treatment thereof.

Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.

Abstract: Methods of preparing and administering an injectable depot formulation of crystalline iloperidone are disclosed herein.

Abstract: The present invention relates to compositions, in particular dietary compositions, that comprise a combination of choline cation and succinate anion (2?) and nicotinamide, and use of these compositions for maintaining and enhancing the brain energy metabolism in a human, and for preventing and treating symptoms and physiological conditions associated with an imbalanced, damaged or slowed brain energy metabolism in a human subject.

Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

Abstract: This disclosure relates to managing conditioned fear and conditions induced by experiencing or witnessing an extreme traumatic event using neurokinin receptor antagonists. In certain embodiments, the disclosure relates to methods of treating or preventing conditioned fear comprising administering an effective about neurokinin 3 receptor antagonist to a subject in need thereof. In certain embodiments, the subject is diagnosed with Post-Traumatic Stress Disorder.

Abstract: Inventors have evaluated the effects of the FLT3 inhibitors on morphine analgesic potency, on tolerance to morphine analgesia and on morphine-induced mechanical pain hypersensitivity. When the FLT3 inhibitor was administered together with morphine, the amount of analgesic effect was higher than that produced by morphine alone. Repeated administration of morphine induced a progressive decrease in morphine-induced analgesia as showed by the decreased percentage of MPE in control animals. Intrathecal pre-treatment with an FLT3 inhibitor reduced the decrease in morphine analgesia. The administration of FLT3 inhibitors completely prevented both the development of morphine-induced pain hypersensitivity and morphine-revealed latent pain sensitization. Accordingly, the invention relates to an FLT3 inhibitor for increasing the efficacy of an opioid for its analgesic effect, and hereby reducing the opioid dose while maintaining the opioid efficacy in a subject suffering from pain in need thereof.

Abstract: Provided is a solution suitable for oral administration of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof. A solution for oral administration containing compound (I) or a salt thereof, and at least one compound selected from the group consisting of lactic acid, phosphoric acid, glycolic acid, malic acid, tartaric acid, citric acid, succinic acid and acetic acid and having pH 2.5-4.5.

Abstract: The present disclosure provides a method of treating a fibrotic lung disease in a subject comprising administering to the subject an effective amount of a therapeutic agent, wherein the subject is asymptomatic and wherein the subject is at risk of developing the fibrotic lung disease.

Abstract: The present invention relates to a pharmaceutical composition comprising brexpiprazole or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, wherein particle size of brexpiprazole or pharmaceutically acceptable salt thereof is D90 from about 10 ?m to about 40 ?m, particularly D90 is in the range from about 15 ?m to about 30 ?m and process of preparation of said pharmaceutical composition and its use for the adjunctive treatment of major depressive disorder (MDD) and treatment of schizophrenia.

Abstract: Prostacyclin (PGI2) analogues which are agonists of the prostacyclin receptor (PI) are demonstrated to activate lipolytic activity in adipocytes. Also described are pharmaceutical compositions and methods for using the PGI2 receptor agonists to reduce subcutaneous adipose tissue and to treat or reduce symptoms of obesity-related diseases or disorders such as diabetes mellitus, fatty liver disease and cardiovascular disease.

Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.

Abstract: Provided are compounds having HDAC6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by HDAC6.

Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.

Abstract: The present disclosure generally relates to the compounds that exhibits protein kinase inhibitory activity. Specifically, the present disclosure provides compounds of formula (I) that exhibits dual inhibitory activity against ALK5 and P38A MAP kinase. The present disclosure also provides process(es) for preparation of such compounds, pharmaceutical compositions containing one or a combination of these compounds, and methods of treatment of conditions associated with excessive activity of any or a combination of transforming growth factor-beta (TGF?) and p38 mitogen-activated protein kinase (MAPK) utilizing these compounds. An aspect of the present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salt, polymorph, solvate or stereoisomer thereof that exhibit dual inhibitory activity against ALK5 and P38 alpha.

Abstract: A solid dispersion, a method for preparing same, and a solid preparation including the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.

Abstract: The invention described herein provides a method for the treatment of an oestrogen receptor positive breast cancer in a subject in need thereof comprising administering to said subject a therapeutically effective amount of an MPS1 inhibitor, wherein: (i) said subject has previously been treated with an endocrine therapy; and/or (ii) said breast cancer is resistant to endocrine therapy.

Abstract: Herein are provided a combination of palbociclib and of 6-(2,4-dichlorophenyl)-5-[4-[(S3)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a combination, and the therapeutic uses thereof, in particular for the treatment of cancer, including breast cancer.

Abstract: Provided herein are methods of treating follicular lymphoma (FL) and gene mutations that can be used to predict a subject's nonresponsiveness to treatment of follicular lymphoma with ibrutinib.

Abstract: The present invention relates generally to the use of gene mutations, whose presence or absence are useful for predicting a patient's response to treatment with an anti-proliferative agent, in particular a WEE1 inhibitor. The presence or absence of a mutation to the TP53 gene, can be used to predict response to treatment with a WEE1 inhibitor in a patient presenting with a cancerous condition.

Abstract: Discussed herein are pharmaceutical compositions containing Ibrutinib and processes for preparing them. The compositions may be utilized in the treatment of a variety of conditions including, without limitation, B-cell proliferative disorders such as non-Hodgkin lymphoma (diffuse large B cell lymphoma, follicular lymphoma, mantle cell lymphoma or burkitt lymphoma), Waldenstrom macroglobulinemia, plasma cell myeloma, chronic lymphocytic leukemia, lymphoma, or leukemia. These compositions are designed for oral ingestion. The compositions are contained within a capsule such as a standard or sprinkle or in a liquid formulation such as a suspension. In one embodiment, the pharmaceutical composition contains Ibrutinib, a salt, prodrug, or metabolite thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, and magnesium stearate.

Abstract: The present invention relates to dosing regimen of a new antimalarial drug, as monotherapy or combination therapy.

Abstract: The present invention relates to a certain DPP-4 inhibitor for use in combination with metformin in CKD patients.

Abstract: Methods for treating or preventing HIV in a patient using a combination of bictegravir and emtricitabine and optionally with other anti-HIV agents are disclosed, as well as compositions containing such compounds.

Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.

Abstract: The presently claimed invention is related to compositions and methods for treating H2S related diseases comprising administering a pharmacologically effective amount of pharmaceutical composition containing a first therapeutic, wherein the first therapeutic includes one of an ATR kinase inhibitor and an ATR kinase promotor. According to further embodiments the H2S related disease is one of cancer, cardiovascular disease, acute inflammation, chronic inflammation, and neurological disease.

Abstract: The present invention provides a chromone oxime derivative of formula (I), which is a modulator of nervous system receptors sensitive to the neuroexcitatory amino acid glutamate and presents an advantageously high brain exposure upon oral administration, for the treatment or prevention of levodopa-induced dyskinesia. The present invention also provides an improved therapy of Parkinson's disease, using the chromone oxime derivative of formula (I) in combination with levodopa.

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.

Abstract: The present inventive concept describes a method for treating the neurovascular disruption underlying Epileptic Seizures and other traits of Epilepsy and Infantile Spasms by improving the neurophysiological environment and then enabling by sustained sedation a biomechanism of glial cells for neuronal repairs.

Abstract: The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.

Abstract: Methods, compositions and systems are presented to deliver estradiol benzoate to an animal so as to sterilize the animal. A physiologically acceptable oil or other carrier in a capsule is used to deliver the estradiol benzoate. The estradiol benzoate is delivered intraperitoneally, intramuscularly, or subcutaneously to a companion or livestock animal.

Abstract: Methods, compositions and systems are presented to deliver estradiol benzoate to prevent and/or inhibit boar taint and/or male aggression as compared to animal that has not been administered estradiol.

Abstract: Described herein are methods of treating a disorder, e.g., tremor, e.g., essential tremor; depression, e.g., postpostum depression; and anxiety disorder, the method comprising administering to a human subject suffering from a disorder, e.g., tremor, e.g., essential tremor; depression, e.g., postpostum depression, an anxiety disorder with a neuroactive steroid or a composition comprising a neuroactive steroid (e.g., pregnanolone, allopregnanolone, alphadalone, ganaxolone, or alphaxolone).

Abstract: According to various embodiments of this disclosure, pharmaceutical formulations comprising solubilized estradiol are provided. In various embodiments, such formulations are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.

Abstract: The present invention relates to methods for treating acute kidney injury that utilize a glucocorticoid prodrug. The glucocorticoid prodrug selectively delivers a glucocorticoid to the kidney, where it is capable of eliciting a p21 protective response. The present invention also contemplates several novel glucocorticoid prodrugs capable of use in the above manner.

Abstract: This invention relates to methods and compositions for use improving cell viability, particularly neural cell viability, and more particularly to methods and compositions for use improving cell viability by reducing reactive oxygen metabolite-mediated oxidative damage in a cell, regulating redox homeostasis in a cell, or reducing mitochondrial dysfunction in a cell. The invention further relates to the administration of the bile acid tauroursodeoxycholic acid (TUDCA) in combination with phenylbutyric Acid (PBA) to improve cell viability, and treat at least one symptom associated with, prevent the time of onset of, or slow the development of a disease related to oxidative stress.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: Disclosed herein are oral dose formulations of aldosterone receptor antagonists, such as eplerenone and spironolactone, for the treatment of heart failure with preserved ejection fraction and uncontrolled hypertension.

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 a sulfonylurea compound for use in the treatment and/or amelioration of a disease that is associated with UV-induced DNA damage, wherein the subject to be treated expresses enzymatically active mutY homolog (MUTYH), in wherein the sufonylurea compound preferably is acetohexamide or a derivative thereof, or glimepiride or a derivative thereof. The invention furthermore relates to pharmaceutical compositions comprising a sulfonylurea compound for use in the treatment and/or amelioration of a disease that is associated with UV-induced DNA damage. Also, a screening method for identifying a compound that treats and/or ameliorates a disease that is associated with UV-induced DNA damage in a subject that expresses enzymatically active MUTYH is provided.

Abstract: Methods of treatment and dosage regimes using hydrophobic gel or foam compositions comprising a tetracycline antibiotic for accelerating the return of skin integrity and or in treating or alleviating a disorder including impetigo, acne, rosacea, a skin disease caused by a bacteria or a tetracycline antibiotic responsive disease, wherein the foam composition or gel is administered topically to a target area on a subject having the disorder and wherein the target area comprises an area of skin, or mucosa or an eye.

Abstract: The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to a particular 1-di-alkyl-phosphinoyl-alkane, 1-(Diisopropyl-phosphinoyl)-nonane, referred to herein as “DIPA-1-9”. Surprisingly and unexpectedly, DIPA-1-9, is able to selectively treat (e.g., suppress) sensory discomfort arising from the lumenal epithelial lining of the pharynx and esophagus without side effects. Compared to structurally similar compounds, DIPA-1-9 did not have the problems of painful cold, stinging, or irritancy, or of adverse taste when applied in the oral cavity. To deliver the DIPA-1-9 to the lumenal epithelium of the pharynx and esophagus, an ideal formulation for delivery is a solution of DIPA-1-9 in syrup, at a concentration of 5 to 12 mg/mL and a delivery volume of less than 1 mL. The delivery unit can be a plastic vial with a design such that the syrup is poured onto the base of the tongue, next to the pillars of fauces.

Abstract: Expression of a phosphatase inhibitor in heart cells can be used to treat cardiac disorders, e.g., heart failure. Decreasing phosphatase activity can improve ?-adrenergic responsiveness.

Abstract: The present invention is directed to compounds, methods and compositions for treating or preventing viral infections using nucleosides analogs. Specifically, the present invention provides for the design and synthesis of acyclic fleximer nucleoside analogues having increased flexibility and ability to alter their conformation structures to provide increased antiviral activity potential with the result of inhibiting flaviviruses, filoviruses and/or coronaviruses.

Abstract: The present disclosure relates to methods or dosing regimens comprising a proteasome inhibitor of formula (I), or a pharmaceutically acceptable salt thereof, for treating cancer, or preventing cancer recurrence or progression; wherein ring A, Z1 and Z2 are as defined herein.

Abstract: The invention concerns the use of fucosylated non-digestible human milk oligosaccharide, or a composition comprising a fucosylated non-digestible human milk oligosaccharide, for use in improving immune fitness in a human subject, wherein the human subject is male.

Abstract: Methods of treatment of sonic hedgehog associated malignancies in addition to methods that support the survival and proliferation of medulloblastoma cells in culture are provided.

Abstract: The present invention relates to methods for reducing soluble P-selectin and major thrombotic events in cancer patients.

Abstract: A method for treatment of a liver disease, the method including administering kinsenoside to a patient in need thereof.