Abstract: The invention relates to pharmaceutical combination products comprising an HD AC inhibitor, e.g. (E)-N-(2-amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide as well as salts and or solvents thereof and TLR7 agonist and/or TLR8 agonist for the treatment of cancer. The present invention also relates to methods of treatment of patients suffering from cancer with these pharmaceutical combination products.

Abstract: Pharmaceutical compositions comprising a molecular inhibitor of Npr1 are disclosed. Also disclosed are methods of treating, reducing, or preventing acute and/or chronic pruritus in a mammal comprising administering a pharmaceutical composition comprising a molecular inhibitor of Npr1.

Abstract: A thiazolidinedione or rhodanine compound or a pharmaceutically acceptable salt, tautomer, solvate, hydrate, prodrug, derivative, stereoisomer, analog or isotopically labelled derivative thereof, for use in the treatment and/or prevention of a protein misfolding disease, wherein said compound is not Pioglitazone, Rosiglitazone, Rivoglitazone, Balaglitazone or Mitoglitazone.

Abstract: A thiazolidinedione or rhodanine compound or a pharmaceutically acceptable salt, tautomer, solvate, hydrate, prodrug, derivative, stereoisomer, analog or isotopically labelled derivative thereof, for use in the treatment and/or prevention of an ophthalmological condition, wherein said compound is not Pioglitazone, Rosiglitazone, Rivoglitazone, Balaglitazone or Mitoglitazone.

Abstract: The present invention relates to a pharmaceutical composition or a kit comprising, a first substance capable of raising intracellular cAMP levels, and a second substance capable of modulating intracellular calcium concentration. Likewise, the present invention relates to methods of treating patients suffering from autism spectrum disorder (ASD) phenotype 1 by administering an effective amount of a substance capable of raising intracellular cAMP levels and, optionally, an effective amount of a substance capable of modulating intracellular calcium concentration.

Abstract: Provided herein is a method of treating schizophrenia or a disease related to schizophrenia in a patient in need thereof. The method comprises orally administering to the patient twice daily an oral pharmaceutical composition comprising a plurality of xanomeline beads comprising xanomeline or a salt thereof, and plurality of trospium beads comprising a salt of trospium, via the titration scheme that comprises up-titration of the xanomeline, or a salt thereof, and the salt of trospium.

Abstract: The present disclosure relates to the use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea or 1-(5-(7-amino-1-ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-4-bromo-2-fluorophenyl)-3-phenylurea, or a pharmaceutically acceptable salt thereof, in combination with a MAPKAP kinase inhibitor for the treatment of cancers, including c-KIT-mediated cancers, such as GIST.

Abstract: This disclosure relates to the treatment of brain cancer, e.g., medulloblastoma using a combination of STAT3 and YB-1 inhibitors. In certain embodiments, the STAT3 inhibitor is 3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide (WP1066) or salts thereof and YB-1 inhibitor is 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one (Fisetin) or salts thereof. In certain embodiments, this disclosure relates to methods of diagnosing and treating a subject diagnosed with medulloblastoma using assays disclosed herein.

Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.

Abstract: The inventors have found that the compounds of formula (I) protect cardiomyocytes. Accordingly, the disclosure provides a pharmaceutical composition for protecting a cardiomyocyte comprising a compound of formula (I) or an ester, oxide, pharmaceutically acceptable salt or solvate thereof. The pharmaceutical composition may be used for treating or preventing a disease associated with cardiomyocyte death, such as myocardial infarction, chronic heart failure, hypertensive heart failure, or dilated cardiomyopathy, especially for treating myocardial infarction.

Abstract: A compound and methods are provided for treating, preventing or ameliorating infertility or reduced fertility in an individual, wherein said compound is capable of regulating the activity of Nuclear Factor, Erythroid 2 Like 2 (NFE2L2).

Abstract: Provided herein are compounds comprising compounds of formula I and/or salts thereof; wherein at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 are independently chosen from hydrogen and deuterium; with the proviso that when R1, R2, and R3 are fluorine, then at least one of R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine or at least one of R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.

Abstract: The present invention provides a method of treating cancer with tumors bearing MET exon 14 skipping or MET exon 14 skipping phenotype comprising administering to a patient in need of such treatment an effective amount of the compound of Formula (I), or a pharmaceutically acceptable salt thereof:

Abstract: Compounds with amino amide linkers and pharmaceutical compositions and medicaments comprising such compounds are disclosed. In addition, methods of making such compounds and their uses for treating or ameliorating diseases, disorders, or conditions associated with protein malfunction, such as cancer, are provided.

Abstract: The invention relates generally to sustained release compositions. Specifically, the invention relates to biphasic and triphasic compositions and methods for controlling the release of a medication to treat a heart disease.

Abstract: The present invention provides a drug for preventing or treating chronic pain and a method for preventing or treating chronic pain. A pharmaceutical composition comprising a serotonin-3 receptor agonist such as a compound represented by the following formula (I): [wherein: m is an integer of 1 to 4; and R1 is each independently selected from the group consisting of a hydrogen atom, a halogen atom, a methyl group optionally substituted with 1 to 3 halogen atom(s), a methoxy group optionally substituted with 1 to 3 halogen atom(s), and a methylthio group optionally substituted with 1 to 3 halogen atom(s)] or a pharmaceutically acceptable salt thereof is useful for preventing or treating chronic pain. The above pharmaceutical composition is also useful for preventing or treating acute pain. Further, the present invention provides a method for screening a compound for preventing or treating chronic pain, the method comprising measuring a serotonin-3 receptor agonist activity.

Abstract: Disclosed are methods and products for improving the quality of sperm, methods for treating subjects to improve sperm quality or improve fertility, and use of sperm with improved quality in assisted reproductive technologies, including exposing the sperm to BGP-15 and/or a derivative thereof, such as BGP-15, propanolol, bimoclomol, arimoclomal, NG94, iroxanadine, and/or a pharmaceutically acceptable derivative, prodrug, solvate, salt, tautomer, stereoisomer, and/or racemate thereof.

Abstract: Using sulfobutylether ?-cyclodextrin a novel, physically transformed, molecularly dispersed forms lonafarnib may be prepared having pharmaceutical utility.

Abstract: Apixaban pharmaceutical formulation is provided. Also provided is a use of the apixaban formulation in treatment of a thromboembolic disorder.

Abstract: Aspects described herein relate to compositions, including edible compositions, infused with nicotine compounds and methods of use for the treatment of a nicotine-related disorders. More particularly, aspects described herein relate to compositions, including edible compositions, infused with nicotine compounds that provide enhanced bioavailability of the nicotine compounds in a subject, and that mask unpleasant tastes of the nicotine compounds.

Abstract: There is provided topical pharmaceutical formulations comprising montelukast, or a pharmaceutical acceptable salt of solvate thereof, as well as combination products comprising (a) at least one mussel adhesive protein or a derivative thereof; and (b) montelukast, or a pharmaceutically-acceptable salt or solvate thereof. The formulations and combination products find particular utility in direct topical administration for the treatment of inflammation, of inflammatory disorders and/or of condition characterized by inflammation, including wounds, burns, psoriasis, acne and atopic dermatitis.

Abstract: Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

Abstract: Methods and pharmaceutical compositions for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 4 (PFKFB4) and the treatment of cancer are described.

Abstract: Provided herein are spirolactone compounds of Formula I that are useful as inhibitors of ACC1 and/or ACC2. The spirolactone compounds described herein can be used for treating a disease or disorder associated with aberrant ACC1 and/or ACC2 activities, for example, non-alcoholic steatohepatitis (NASH), acne, obesity, diabetes, and cancer. Also provided herein are pharmaceutical compositions comprising the spirolactone compound of Formula I, or pharmaceutically acceptable salt thereof.

Abstract: The present invention includes methods for treating a FLT3 mutated proliferative disorder comprising: measuring expression of a mutated FLT3 and a loss of function mutation in DNMT3A in a sample obtained from a tumor sample obtained from the patient, wherein the presence of the one or more genetic abnormalities indicates that the patient has a poor prognosis; and administering to the patient a therapeutically effective amount of crenolanib or a pharmaceutically acceptable salt thereof, wherein the crenolanib increases a chance of survival of the patient having both the mutated FLT3 and the loss of function mutation in DNMT3A, wherein the crenolanib, as shown below, is administered to a subject suffering from said disorder:

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Abstract: Embodiments of the invention provide methods of attenuating, e.g., inhibiting or reducing, cellular proliferation and migration, particularly endothelial cell proliferation and migration, including that associated with angiogenesis, as well as attenuating cancerous tumor growth and metastasis, using opioid antagonists, including, but not limited to, those that are peripherally restricted antagonists.

Abstract: Topical administration of VEGF inhibitors such as, without limitation, rifamycin compounds are useful for treating skin disorders such as treating and/or reducing scars such as hypertrophic scars, and useful for treating acne and underlying acne symptoms such as skin redness.

Abstract: Antibiotic gel formulations for use in dental applications are disclosed. More particularly, the present disclosure is directed to antibiotic gel formulations including low concentrations of antibiotics that are capable of killing root canal pathogens without harming the stem cells inside the root canal. Additionally, the present disclosure is directed to delivery systems and methods for applying the antibiotic gel formulations into a subject's intracanal region.

Abstract: Provided herein are methods for inhibiting contraction and/or promoting relaxation of airway smooth muscle cells (e.g., human airway smooth muscle cells), comprising contacting the cells with a G?12 or RhoA inhibitor. Also provided herein are methods for inhibiting and/or treating bronchoconstriction or promoting bronchodilation in a subject, for example, a subject with airway hyperresponsiveness and/or a disease associated with bronchoconstriction, such as asthma, chronic obstructive pulmonary disease, chronic bronchitis, bronchiectasis or cystic fibrosis, using a G?12 or RhoA inhibitor, as well as pharmaceutical compositions comprising a G?12 or RhoA inhibitor.

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.

Abstract: This document provides methods for determining biological age of mammalian subjects or assessing whether the subjects are aging normally. Also provided herein are methods for determining whether therapeutic treatment or other interventions for reversing or slowing down aging are effective. This document also provides methods and materials for slowing the progression of biological aging.

Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.

Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.

Abstract: Disclosed are methods improving or stimulating hair regeneration; treating, inhibiting, or reducing hair loss; improving or stimulating hair growth; treating, inhibiting, or reducing pigmentation loss; and/or improving or stimulating pigmentation production in a subject with one or more autophagy inducing agents.

Abstract: Provided are a combination of poziotinib and at least one agent selected from the group consisting of cytotoxic agents and molecularly targeted agents; and a use of the combination.

Abstract: Described herein are methods and compositions for treating HER2-amplified cancer. The methods include administering to an individual in need thereof ibrutinib.

Abstract: The invention refers to a process for preparing sterile active pharmaceutical ingredients (APIs) useful in the preparation of sterile product for ophthalmic use. The process comprises the gamma-ray sterilization treatment of the APIs powder in a protective atmosphere.

Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, tautomer, prodrug, solvate, metabolite, polymorph, analog or derivative thereof, which modulates the activity of BTK, a pharmaceutical composition comprising the compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

Abstract: The current invention relates to selective PDE4D inhibitors for use in the prevention and/or treatment of demyelinating diseases of the central nervous system and of the peripheral nervous system.

Abstract: Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.

Abstract: Described herein are methods for treating T-cell lymphoma in a subject in need thereof, comprising administering to the subject in need thereof, an ETP compound. Also described herein are pharmaceutical compositions and compositions for use that include such ETP compound.

Abstract: Aspects described herein relate to edible compositions and methods for the enhancement of delivery of lipophilic active agents across the blood-brain barrier, particularly wherein the lipophilic active agent infused edible compositions produce greater concentrations of lipophilic active agents in subjects' central nervous system tissues as compared to control compositions. Further provided are methods for treating central nervous system disorders comprising administering the edible compositions to subjects in need thereof.

Abstract: The present invention provides nazartinib, or a pharmaceutically acceptable salt thereof, preferably the mesylate salt thereof, for use in treating or preventing Central Nervous System (CNS) metastasis, brain metastasis, and/or leptomeningeal metastasis, particularly when the CNS or brain metastasis, or leptomeningeal metastasis is present in a patient with locally advanced or metastatic NSCLC.

Abstract: The present disclosure relates to compositions and methods associated with haptoglobin related protein (HRP), including compositions and methods associated with diagnosis and treatment of renal salt wasting (RSW) and the syndrome of inappropriate anti-diuretic hormone secretion (SIADH), as well as diuretic compositions and associated methods.

Abstract: Disclosed is a combination therapy for reducing nicotine addiction or aiding in the cessation or lessening of tobacco use in a mammal, comprising administering to said mammal an amount of an ALDH-2 inhibitor, such as a compound of Formula (I), in combination with an amount of the nicotinic acetylcholine receptor agonist, varenicline. The disclosure further relates to methods and pharmaceutical compositions useful with the combination therapy.

Abstract: This invention is directed to a method of treating alcohol dependence, including acute and post-acute withdrawal symptoms, comprising treating an alcohol dependent patient with ibogaine, ibogaine derivative, or pharmaceutically acceptable salt and/or solvate thereof at a dosage that provides an average serum concentration of about 50 ng/mL to about 850 ng/mL under conditions where the QT interval prolongation does not exceed about 50 milliseconds.

Abstract: The present disclosure is directed to a pharmaceutical composition suitable for intramuscular (IM) administration, comprising fulvestrant, a pharmaceutically acceptable alcohol(s), a cosolvent(s), a lipophilic vehicle comprising a release-controlling oil, and, optionally, at least one surfactant and/or an antioxidant. The composition comprises fulvestrant at a concentration of at least 50 mg/ml, e.g., 100 mg/ml, wherein the composition exhibits excellent storage stability at long-term and accelerated storage conditions. The composition of the disclosure can deliver a 250-500 mg dose of fulvestrant as a single IM injection from a prefilled syringe, e.g., 500 mg/5 ml or 250 mg/2.5 ml in a prefilled syringe.

Abstract: Topical pharmaceutical compositions comprise a combination of a corticosteroid a retinoid; and methods for treating psoriasis with same.

Abstract: Compounds are provided according to Formula (I): Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2, R3, R6, R7, R8, and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.