Abstract: The present invention relates to solid dispersion of Naloxegol oxalate. Further, the present invention relates to an improved process for Naloxegol oxalate and intermediates thereof.

Abstract: Disclosed herein Eire pharmaceutical compositions having a mixture of at least one active agent, an ion exchange resin, a binder, and a matrix material such that the composition, when administered to a patient in need thereof, provides the patient with a therapeutic effect for at least about 8 hours and related methods. Also disclosed herein are pharmaceutical compositions having a mixture of a drug susceptible to abuse, a non-opioid analgesic and an ion exchange resin, the composition further including at least one gelling agent and related methods.

Abstract: The invention relates to a method of treating pain in a patient by applying a transdermal therapeutic system for the transdermal administration of buprenorphine for 7 days on the skin of a patient, said transdermal therapeutic system comprising a buprenorphine-containing self-adhesive layer structure comprising A) a buprenorphine-impermeable backing layer, and B) a buprenorphine-containing matrix layer on said buprenorphine-impermeable backing layer, the matrix layer comprising a) a polymer base, b) buprenorphine, and c) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said buprenorphine is solubilized therein to form a mixture, and the carboxylic acid buprenorphine mixture forms dispersed deposits in the polymer base, and C) a skin contact layer on said buprenorphine-containing matrix layer comprising a polymer-based pressure-sensitive adhesive, and optionally wherein the buprenorphine-conta

Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

Abstract: The present invention relates to the use of the compound according to Formula I in the prophylaxis and/or treatment of fibrotic diseases, more particularly idiopathic pulmonary fibrosis.

Abstract: A method of treating a subject, comprising: (a) diagnosing a subject with bronchiectasis and chronic respiratory bacterial infections, with at least one strain of a bacteria such as Pseudomonas aeruginosa bacteria in an airway sample taken from the subject; (b) administering to the subject over a plurality of days (such as 28 days) by inhalation a formulation comprised of the un-encapsulated and encapsulated antibiotic, such as ciprofloxacin; (c) discontinuing the administering over a plurality of days; (d) repeating the administering over a plurality of days; (e) whereby an antibacterial impact of the formulation on the bacteria is not decreased with each repeating step (d).

Abstract: The present invention relates to novel amine substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.

Abstract: The invention relates to a method for the treatment of vasomotor symptoms comprising the administration of a therapeutically effective amount of flibanserin.

Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.

Abstract: Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.

Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.

Abstract: Provided herein are pharmaceutical compositions, such as emulsions and nanosuspensions, comprising a CRAC channel inhibitor. Also provided herein are methods of treating pancreatitis, viral infections, stroke, traumatic brain injury, fibrosis, inflammation, and autoimmune diseases by administering such pharmaceutical compositions.

Abstract: The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.

Abstract: The present invention features solid pharmaceutical compositions comprising Compound 1 and Compound 2. In one embodiment, the solid pharmaceutical composition includes (1) a first layer which comprises 100 mg Compound 1, as well as a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant, all of which are formulated in amorphous solid dispersion; and (2) a second layer which comprises 40 mg Compound 2, as well as a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant, all of which are formulated in amorphous solid dispersion.

Abstract: Disclosed herein are novel compounds of formula (I) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the disclosure.

Abstract: This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant.

Abstract: The present invention relates to a method for prophylactically treating or treating a viral disease, comprising administering to a subject in need thereof a dihydropyrimidine compound, and the viral diseases include, but are not limited to, Hepatitis A, Hepatitis B, Hepatitis C, influenza, herpes and acquired immunodeficiency syndrome (AIDS).

Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

Abstract: Described herein are methods of treating cancers and other tumors related to the decreased proliferation, the depletion, or the repolarization of tumor-associated macrophages (TAMs) and treatment of associated disorders, including tenosynovial giant cell tumor (TGCT) and diffuse-type tenosynovial giant cell tumor (DTGCT).

Abstract: The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.

Abstract: An antitumor agent for treating a malignant tumor patient expressing EGFR having at least one mutation selected from the group consisting of G719X mutation of exon 18, E709X mutation of exon 18, and L861X mutation of exon 21, wherein X represents an arbitrary amino-acid residue, the antitumor agent comprising (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide or a salt thereof.

Abstract: The “amyloid hypothesis” has dominated Alzheimer research for more than 20 years, and proposes that amyloid is the toxic cause of neural/synaptic damage and dementia. Despite discrepancies in the proposed mechanism, and failed clinical trials, amyloid continues to be considered the cause of a degenerative cascade. The present invention proposes that AD is precipitated by impaired microvascular function, resulting primarily from decreased Notch-related angiogenesis. With impaired microvasculature, a lack of vascular endothelial-derived trophic factors and decreased cerebral blood flow cause the atrophy of neural structures. Therapeutic strategies are proposed that focus on supporting normal angiogenesis.

Abstract: Provided herein are methods for treating, delaying progression of, or reducing the severity of amyotrophic lateral sclerosis (ALS) in a subject through administration of therapeutically effective amounts of agents (e.g., JAK kinase inhibitors (e.g., tofacitinib)) capable of interfering with central nervous system related natural killer cell (NK) levels and function.

Abstract: This disclosure relates to heterocyclics as selective inhibitors of the fibroblast growth factor receptor 4 (FGFR-4), in particular relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the compound.

Abstract: The disclosure provides methods for treating cancer, including but not limited to, hematopoietic and lung cancers, using the HSP90 inhibitor, MPC-0767, as monotherapy and in combination therapy with additional active agents, including but not limited to, inhibitors of Bcl-2, EZH2 inhibitors, Ras/Raf/MEK/ERK pathway inhibitors, checkpoint inhibitors, DNMT inhibitors, ATO and chemotherapeutic agents. The disclosure also provides related compositions and methods of use.

Abstract: The present invention relates to a pharmaceutical combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor or pharmaceutically acceptable salt thereof, and (b) at least one c-Met receptor tyrosine kinase inhibitor or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential administration for the treatment of a proliferative disease, particularly a c-Met dependent proliferative disease; a pharmaceutical composition comprising such combination; a method of treating a subject having a proliferative disease comprising administration of said combination to a subject in need thereof; use of such combination for the treatment of proliferative disease; and a commercial package comprising such combination.

Abstract: The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.

Abstract: The present invention relates to Orally Inhaled and Nasal Drug Product (OINDP) comprising a benzodiazepine, in particular remimazolam.

Abstract: The present disclosure is directed to generally methods and/or compositions for treating mammographic breast density and/or breast stiffness in a patient in need thereof, such as a pre-menopausal, a peri-menopausal or a post-memopausal patient, comprising the administration of an effective amount of androgenic agent and an effective amount of an aromatase inhibitor. The present disclosure is also directed to methods and/or compositions for reducing breast pain. The present disclosure is also directed to method and/or compositions for reducing elasticity and/or decreasing mechano-transduction on the genome of breast cells. The present disclosure is also directed to methods and/or compositions for stabilizing and/or increasing the levels of androgen receptor expression in breast tissue.

Abstract: Described herein are methods of treating tremor, e.g., essential tremor; depression, e.g., postpostum depression; and anxiety disorder, the method comprising administering to a human subject suffering from 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: The present application provides Triptonide or a functional equivalent or pharmaceutically acceptable salt thereof, or a composition comprising the same for use in treating or preventing hyperproliferative disorders. Also provided is a method for treating or preventing hyperproliferative disorders, preferably cancer in a subject using the above substances.

Abstract: The method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25-hydroxyvitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1,25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1,25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25-hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1,25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies.

Abstract: Methods, compositions, and kits for adjunctive therapy using 25-hydroxyvitamin D are disclosed. The 25-hydroxyvitamin D may be administered with an agent that increases the risk of hypocalcemia and/or an anticancer agent. The adjunctive therapy is effective to treat and prevent iatrogenic hypocalcemia and/or secondary hyperparathyroidism, as well as delay cancer progression and the time to a post-treatment skeletal related event.

Abstract: A scalable vitamin composition unit dosage adapted to treat a fat-soluble vitamin deficiency in a subject is provided herein, the unit dosage consisting essentially of vitamin D, vitamin E, vitamin K, and vitamin A, wherein the unit dosage is substantially free of additional vitamins and wherein the unit dosage is scalable based on the weight, age, and condition of a subject without inducing toxic effects. Also provided are methods of treating a fat-soluble vitamin deficiency in a subject in need thereof by administering to the subject an effective amount of a unit dosage as described herein.

Abstract: Provided are methods for enhancing the efficacy of aspirin. Also provided are methods for reducing pain or preventing or treating heart attack, stroke or blood clot in a subject in need thereof. The methods entail orally administering to the subject a first composition comprising a first amount of aspirin, and a second composition comprising a second amount of aspirin, wherein the first composition is formulated so as to, upon administration, disintegrate or dissolve intraorally providing rapid release of the aspirin of the first composition in the subject, and wherein the second composition is formulated to be substantially more difficult than the first composition to disintegrate or dissolve intraorally but is ingestible and releasable in the gastrointestinal track of the subject. The method can further include administering to the subject a painkiller or an agent suitable for treating a cardiovascular disease or condition.

Abstract: This invention is based on the discovery that many eye conditions associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The data show that in age-matched patients, the severity of age-related conditions correlates with the abundance of senescent cells, and that clearing senescent cells can help abrogate the condition. Small molecule drugs that remove senescent cells from affected tissue in the eye are provided that have special efficacy in treating ophthalmic conditions. They not only inhibit progression of the disease, they can also reverse some of the pathophysiology—such as neovascularization and vaso-obliteration—that lead to vision loss. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable ophthalmic conditions.

Abstract: Methods for identification of new dosing strategies which optimize positive treatment outcomes and patient safety. Specifically, new dosing strategies for fosfomycin and pharmaceutically acceptable salt thereof which have improved treatment outcomes in mammals. For example, a method of treating mammals having a bacterial infection with fosfomycin or a pharmaceutically acceptable salt thereof using improved dosing regimens.

Abstract: Compound of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, X, Y and G are as defined in the description, and their use in the manufacture of medicaments.

Abstract: Compositions and methods for treating skin lesions and skin infections using topically administered pyrimidine derivative such as cidofovir.

Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

Abstract: The present invention relates to the compounds of formula (I) below: wherein: X represents an oxygen atom, a sulfur atom, a nitrogen atom or a CH radical, The bond X—Y and Y are absent if X represents an oxygen or sulfur atom, the bond X—Y and Y are present if X represents a nitrogen atom or a CH radical, When present, Y represents a group R if X represents a nitrogen atom, a hydrogen atom or a group —NR1R2 if X represents a CH radical, (Het)Ar is an aromatic ring selected from the group consisting of aryl and heteroaryl groups, R3, R4, R5, R6 represent, independently of one another, a hydrogen atom, a halogen atom, a —NR12R13, a —SR14 group, a —OR14 group or a —CF3 group, When Y is —NR1R2, the groups —NR1R2 and (Het)Ar are in the cis-conformation, or a pharmaceutically acceptable salt thereof, for use in the treatment of proliferative diseases, infectious diseases, allergies, inflammation and/or asthma.

Abstract: The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: The present invention provides novel immunotherapeutic compositions and methods useful for treating or preventing microbial infections, weakened immune systems, diseases in which cells have become obligately anerobic and cellular proliferative disorders including cancer. The irnmunotherapeutics herein use benzaldehyde derivatives, precursors and intermediaries alone or in combination with additional therapeutic agents to stimulate the immune system and inhibit cellular proliferation.

Abstract: The present invention relates to a pharmaceutical product comprising a) as a first component an inhibitor of the MDM2-p53 interaction; and b) as a second component cytarabine; as a combined preparation for the sequential or simultaneous use in the treatment of cancer, particularly AML.

Abstract: An ophthalmic solution, which comprises diquafosol tetrasodium salt and is free from benzalkonium chloride, treats onset and/or exacerbation of dry eye symptom caused by wearing soft contact lenses.

Abstract: The object of the present invention is to find a pharmaceutical having strong cancer therapeutic effect. The present invention provides a pharmaceutical composition for cancer therapy comprising a transcription or processing product of a gene encoding a miRNA, wherein said miRNA is one or more miRNAs selected from the group consisting of miR-3140, miR-137, miR-631, and miR-657, pharmaceutical composition.

Abstract: The present disclosure relates to methods of treating Duchenne's Muscular Dystrophy by administering an antisense oligonucleotide that induces exon skipping and a non-steroidal anti-inflammatory compound.

Abstract: A purified oligosaccharide compound having antithrombotic activity or a mixture of a homologous compound thereof and a pharmaceutically acceptable salt thereof, a preparation method for the mixture, a pharmaceutical composition containing the mixture, and uses thereof serving as an intrinsic factor X-enzyme (Xase) inhibitor in the preparation of drugs for preventing and/or treating thrombotic diseases.

Abstract: The present disclosure provides compositions comprising one or more polymers capable of forming a hydrogel and methods for making and using the same. More specifically, the present disclosure provides compositions comprising one or more polymers capable of forming a hydrogel with prolonged mucosal retention, and methods for making and using the same.