Abstract: [Problem] Provided is a pharmaceutical composition for treating cancer in which one or more kinases of BTK, JAK3, and ITK is involved. [Means for Solution] The present inventors studied compounds having a BTK inhibiting effect, a JAK3 inhibiting effect and an ITK inhibiting effect, and confirmed that a specific pyrazine carboxamide compound has the BTK inhibiting effect, the JAK3 inhibiting effect, and the ITK inhibiting effect, and that a pharmaceutical composition comprising the compound as an active ingredient has a therapeutic effect on cancer in which one or more kinases of BTK, JAK3 and ITK is involved, in another aspect, cancer in which BTK is overexpressed or activated, in another aspect, cancer in which a B cell receptor signal is activated, in still another aspect, cancer in which JAK3 is activation-mutated or activated, and in still another aspect, cancer in which ITK is activated, thereby completing the present invention.

Abstract: This invention relates to the new use of the compound 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide (orvepitant) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it for the treatment of chronic cough, including chronic refractory cough and to combinations for such a use.

Abstract: Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (Cmax) and slightly delaying the peak such as to avoid activating the dopaminergic and adrenergic receptors, while achieving sufficient active binding to the serotonin receptors to provide relief from migraine symptoms within a timeframe that permits rapid resolution of migraine symptoms. Inhaler devices suitable for the methods are disclosed. Kits for practicing the methods of invention are disclosed.

Abstract: The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

Abstract: A modified microbubble is provided. The modified microbubble includes an albumin microbubble and a plurality of chitosan oligosaccharide lactates. The albumin microbubble includes an albumin shell and a gas core inside the albumin shell. The plurality of chitosan oligosaccharide lactates is connected to an outer surface of the albumin shell.

Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

Abstract: Provided herein are compositions and methods for the treatment of autoimmune diseases, including lupus, uveitis and encephalitis. Said compositions useful for treating autoimmune diseases comprise pyrrolo-pyrazole PKC inhibitors.

Abstract: The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.

Abstract: Cancers that overexpress tyrosine kinase receptors of HER family are treated with drugs acting on these receptors. Although HER-targeting drugs have revolutionized the treatment of HER-positive cancers, high rates of primary and treatment-emergent resistance limit their clinical utility. The present inventors have now discovered that combining HER-targeting drugs with a selective inhibitor of CDK8/19 greatly improves the efficacy of such drugs, offering an improved approach to the treatment of HER-positive cancers.

Abstract: Methods of treating breast cancer are provided where a quantitative Her2 assay is used to identify whether a breast tumor will be responsive to treatment with anti-Her2 therapeutic agents such as lapatinib and trastuzumab, followed by selection of a suitable treatment regimen and administration of the regimen. A specific Her2 fragment peptide is precisely quantitated by SRM-mass spectrometry directly in breast tumor cells collected from breast tumor tissue that was obtained from a cancer patient and compared to a reference level in order to determine if the breast cancer patient will positively respond to treatment with a therapeutic agent that specifically targets the Her2 protein.

Abstract: Provided is a pharmaceutical composition for treating ulcerative colitis, comprising a compound represented by a formula (1) or a pharmaceutically acceptable salt thereof, wherein the compound or the pharmaceutically acceptable salt is administered in an amount of 600 mg or more per day to an ulcerative colitis patient.

Abstract: ATM kinase is shown to regulate proteasome-mediated protein turnover through suppression of the expression of the ubiquitin-like protein ISG15 (Interferon Stimulated Gene 15). Silencing of the ISG15 pathway restored both the ubiquitin and autophagy pathways, and the UV-mediated degradation of their substrates in A-T cells. The ATM kinase negatively regulates the ISG15 pathway, and the constitutively elevated ISG15 pathway induces proteinopathy in A-T cells, and in A-T patients. These findings indicate that proteasome-mediated protein degradation is impaired in A-T cells due to elevated expression of the ISG15 conjugation pathway, which contributes to progressive neurodegeneration in A-T patients. The ISG15 pathway is a new target for both detection and treatment of A-T. Inhibitors if ISG15 expression can be used to inhibit or attenuate neurodegeneration in A-T patients.

Abstract: The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.

Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.

Abstract: A therapeutic nanoparticle comprising: at least one oncologic drug; and taurolidine, whereby to provide the simultaneous delivery of the at least one oncologic drug and taurolidine, thereby harnessing the synergistic effect of taurolidine on the at least one oncologic drug.

Abstract: New oxathiazin-like compounds and their derivatives are useful as antineoplastic and antimicrobial agents. Compositions and methods of using oxathiazin-like compounds and their derivatives are disclosed.

Abstract: An object of the present invention is to provide a combination drug that has remarkably excellent preventive and/or therapeutic effects on polycystic kidney disease. The present invention provides a drug for preventing and/or treating polycystic kidney disease comprising a combination of tolvaptan or a prodrug thereof with a somatostatin derivative, and a method for treating polycystic kidney disease using this drug.

Abstract: The present invention relates to the use of CBP/EP300 inhibitors and BET inhibitors for the treatment of cancer. In some embodiments, the use is to treat cancer that is resistant to BET inhibitors.

Abstract: Provided herein is the use of compounds that modulate the activity of inhibitor of apoptosis proteins (1APs), alone or in combination with other therapeutic agents, in the treatment of human immunodeficiency virus (HIV). Described herein is the use of IAP antagonists in the treatment of human immunodeficiency virus (HIV) in a mammal, alone or in combination with other therapeutic agents used in HIV therapy. In one aspect, provided herein is a method of treating human immunodeficiency virus (HIV) in an individual in need thereof comprising administering a therapeutically effective amount of at least one inhibitor of apoptosis proteins (IAP) antagonist.

Abstract: A composition comprising a) a compound of Formula (I), where R1, R2, and R3 are, each one and independently, hydrogen or a protector group, wherein said protector group may consist of an alkyl group, a cycloalkyl group, a heterocyclic cycloalkyl group, a hydroxyalkyl group, a halogenated alkyl group, an alkoxyalkyl group, an alkenyl group, an alkynyl group, an aryl group, a heterocyclic aryl group, an alkylaryl group, an ester group, a carbonate group, a carboxylic acid group, an aldehyde group, a ketone group, a urethane group, a silyl group, a sulfoxide group or a combination thereof, R5, R6, R7, R8, R9 and R10 are, each one and independently, hydrogen, hydroxyl or an —OR,? group, where R4 is a protector group according to the previous definition; and b) at least one chemotherapeutic agent, suitable for use in the treatment of Breast Cancer.

Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The use of cobalt porphyrins for the manufacture of an agent for mobilizing bone marrow cells to peripheral blood, preferably used to treat congenital neutropenia, for the treatment and prevention of neutropenia caused by chemotherapy, radiotherapy and pharmacologically-induced neutropenia, for the treatment of acute myeloid leukemia, acute lymphocytic leukemia, myelodysplastic syndromes, and to increase the amount of circulating hematopoietic stem cells in peripheral blood for subsequent isolation in the process of apheresis and allogeneic or autologous transplantation.

Abstract: This present disclosure generally relates to medicine, and in particular to pharmacology and psychiatry, and discloses active agents and related methods of treatment which can be used for the treatment of treatment-resistant forms of schizophrenia. In some exemplary aspects, such treatments allow for eliminating both the positive and negative symptoms of schizophrenia, and cognitive disorders, without causing severe side effects that limit their use, such as sedation, tachycardia, orthostatism, agranulocytosis and sialorrhea.

Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Abstract: GABAA receptor mediated hypersomnia can be treated by administering a GABAA receptor antagonist (e.g., flumazenil; clarithromycin; picrotoxin; bicuculline; cicutoxin; and oenanthotoxin). In some embodiments, the GABAA receptor antagonist is flumazenil or clarithromycin. The GABAA receptor mediated hypersomnia includes shift work sleep disorder, obstructive sleep apnea/hypopnea syndrome, narcolepsy, excessive sleepiness, hypersomnia (e.g., idiopathic hypersomnia; recurrent hypersomnia; endozepine related recurrent stupor; and amphetamine resistant hypersomnia), and excessive sleepiness associated with shift work sleep disorder, obstructive sleep apnea/hypopnea syndrome, and hypersomnia (e.g., idiopathic hypersomnia; recurrent hypersomnia; endozepine related recurrent stupor; and amphetamine resistant hypersomnia.

Abstract: The present invention relates to a new use of tetrahydroxylated estrogens such as estetrol (1,3,5(10)-estratrien-3, 15?, 16?, 17?-tetrol), namely in a method of emergency contraception. The method of emergency contraception according to the invention comprises the oral administration of estetrol in a single dose within 120 hours of sexual intercourse.

Abstract: In addition to its potent mechanism-dependent inhibition of estrogen biosynthesis, in accordance with the embodiments of the present invention, it has now been found that exemestane has novel chemoprotective properties which have hitherto not been explicitly recognized. The present invention provides methods for the use of compositions comprising exemestane for chemoprotection against a wide variety of non-mammary tumors (and possibly other chronic diseases) that are not estrogen-dependent, but have oxidative stress, inflammation and electrophile-damaging etiologies. The present invention also shows that exemestane shows powerful synergism with other classes of Nrf2-activators and phase 2 enzyme gene activators, including, for example sulforaphane (an isothiocyanate), shikonin (a naphthoquinone), zerumbone (a cyclic sesquiterpene) and resveratrol (a stilbene derivative), which increases the attractiveness of exemestane's novel uses.

Abstract: A method of treating cancer in a subject in need thereof is provided. The method comprising administering to the subject a receptor tyrosine kinase (RTK)-specific cancer therapy and a glucocorticoid or a glucocorticoid analog, such that an efficacy window of said RTK-specific cancer therapy and an efficacy window of said glucocorticoid or glucocorticoid analog substantially overlap.

Abstract: A stable oral spray formulation comprising a glucocorticoid together with other excipients is disclosed. In preferred embodiments, the spray formulation is used to treat neurological disorders such as ataxia by being sprayed in an effective dose into the mouth of a patient.

Abstract: Provided herein are complexes of metformin or metformin analogues and a TGR5 ligand that are useful in treating diseases including diabetes, cardiovascular disease, and cancer.

Abstract: Provided are methods of treating and/or reducing risk of lipodystrophy using compositions including at least one fatty-acid/bile-acid conjugate (FABAC). Further provided are methods of treating HIV-associated lipodystrophy using said FABACs.

Abstract: Described are oxysterols, pharmaceutical compositions including the oxysterols, and methods of using the oxysterols and compositions for treating diseases and/or disorders related to myelin injury, such as neonatal brain injury, traumatic brain injury, spinal cord injury, cerebral palsy, seizures, cognitive delay, multiple sclerosis, stroke, autism, leukodystrophy, schizophrenia and bipolar disorder.

Abstract: Provided herein are methods and compositions for treating demyelinating inflammatory diseases by administering to the subject an effective dose on an FXR agonist.

Abstract: The present invention relates to a pharmaceutical composition comprising (a) 7?-hydroxycholesterol, (b) a water soluble organic solvent, preferably propylene glycol and/or DMSO, and (c) a solubilizing agent, preferably PEG hydrated castor oil, and to a method for preparing the same. This composition is suitable for preparing an intravenously administered preparation and comprises the pharmaceutically active substance ?-hydroxycholesterol, which is poorly soluble in water.

Abstract: The present invention is about a pharmaceutical composition, an oral preparation, and an injection preparation containing a G protein-coupled Receptor19 (GPCR19) agonist, specifically sodium taurodeoxycholate(HY2191) and its derivative, as an active ingredient for preventing or treating allergic skin diseases. The present invention is also about an external preparation and a cosmetic composition containing said pharmaceutical composition for preventing and improving allergic skin diseases. The said pharmaceutical composition shows an excellent efficacy in treating and improving allergic dermatitis compared with the steroid ointments or immunosuppressive ointments currently used. The said pharmaceutical composition reduces the level of serum IgE, which is a major factor causing allergic dermatitis, increases TH1 cytokine alleviating allergic dermatitis and reduces TH2 cytokine that exacerbates allergic dermatitis.

Abstract: Disclosed herein are gel compositions for enhanced transdermal delivery of an active ingredient into a serum of a subject through production of a reservoir of the active ingredient in the stratum corneum of the subject. Also disclosed herein are methods of using the gel composition to at least partially ameliorate a condition, and kits comprising the gel composition.

Abstract: The present invention provides compositions and methods for use in the treatment of hyperproliferative dermal diseases. Specifically, the present invention teaches pharmaceutical compositions for topical administration that include a vitamin D metabolite, calcipotriol, and nicotinamide in a combination that is particularly effective in treating and in the maintenance therapy of psoriasis and other related dermal disorders and diseases.

Abstract: Suggested is a medicament which is particularly useful for preventing, curing or abating of cough and inflammations of the respiratory system, comprising or consisting of active pharmaceutical ingredients and 1,3-propandiol.

Abstract: The present invention relates to a stable pharmaceutical composition comprising tigecycline and arginine, to a process for the manufacture of said pharmaceutical composition as well as to its use in the treatment of bacterial infections.

Abstract: Provided herein are systems for treating a subject with a pulmonary infection, for example, a nontuberculous mycobacterial pulmonary infection, a Burkholderia pulmonary infection, a pulmonary infection associated with bronchiectasis, or a Pseudomonas pulmonary infection. The system includes a pharmaceutical formulation comprising a liposomal aminoglycoside dispersion, and the lipid component of the liposomes consist essentially of electrically neutral lipids. The system also includes a nebulizer which generates an aerosol of the pharmaceutical formulation at a rate greater than about 0.53 gram per minute. The aerosol is delivered to the subject via inhalation for the treatment of the pulmonary infection.

Abstract: In alternative embodiments, provided are therapeutic combinations, pharmaceutical compositions, formulations, kits and devices for treating, preventing or ameliorating a tumor or a cancer, and methods for treating, preventing or ameliorating a tumor or a cancer. In alternative embodiments, provided are therapeutic combinations, pharmaceutical compositions, formulations, kits and devices comprising: a beta adrenergic receptor antagonist (a “beta blocker”) such as propranolol; a non-steroidal anti-inflammatory drug (a NSAID) such as etodolac; a gemcitabine or GEMZAR™; and, a taxane, a paclitaxel, TAXOL™, ONXOL™, an albumin-bound paclitaxel (nab-paclitaxel) or ABRAXANE™, or any equivalent thereof. In alternative embodiments, the therapeutic combinations further comprise an anti-cancer or anti-tumor antibody, a cytokine, and/or a chemotherapeutic agent.

Abstract: The present invention belongs to the field of medicine technology, particularly relating to an application of cyclic dinucleotide (cGAMP) in tumor treatment. Researches carried out in the present invention show that, cGAMP can inhibit growth of many types of tumor cells, with remarkable anti-tumor effect, thus, it can be used in preparation of anti-tumor drugs; and the prepared anti-tumor drugs have low toxicity and favorable effect. Proved by a subcutaneous tumor model in nude mice, cGAMP has a remarkable inhibition effect on tumors of human gastric carcinoma cell line MNK-45, human lung adenocarcinoma cell line A549, human colorectal carcinoma cell line Lovo, human hepatocellular carcinoma cell line SMMC-7721, human prostatic carcinoma cell line PC-3 and human pancreatic carcinoma cell SW1990, which are subcutaneously implanted in nude mice, and also proved by animal acute toxicity experiment. cGAMP has a relatively low acute toxicity, therefore and may be used for preparing anti-tumor drugs.

Abstract: The present invention is directed to compositions and methods of removing potassium or treating hyperkalemia by administering pharmaceutical compositions of cation exchange polymers with low crosslinking for improved potassium excretion and for beneficial physical properties to increase patient compliance.

Abstract: Silicone oil-containing formulation for nasal application for use in a method for intranasal treatment of endogenous diseases of the nose and/or those due to exogenous causes, e.g. those which are caused by bacteria, fungi, viruses and/or allergens, wherein the silicone oil or the formulation is optionally enriched with oxygen, preferably in the presence of emulsifiers, and optionally in the presence of further active ingredients, such as ?-sympathomimetic drugs, e.g. oxymetazoline or xylometazoline, and related subjects of the invention.

Abstract: The present invention relates to nitric oxide (NO)-releasing nail coating compositions, NO-releasing coatings, and methods of using the same, for example, to treat fungal infections of a nail. It is noted that aspects described with respect to one embodiment may be incorporated in different embodiments although not specifically described relative thereto. Provided according to embodiments of the invention are nitric oxide (NO)-releasing nail coating compositions and/or coatings.

Abstract: The invention discloses means of utilizing Noble Gases for inhibition of pathogenic processes associated with Alzheimer's Disease progression, as well as reversal of Alzheimer's Disease. In one embodiment compositions containing xenon gas are administered alone or together with therapeutic interventions for treatment of Alzheimer's Disease. In another embodiment, taupathies such as chronic traumatic encephalopathy are treated by administration of xenon or Noble Gas containing mixtures.

Abstract: A replacement fluid for dialysis treatment includes selenium in a concentration of 0.6-1.8 ?M, and rubidium in a concentration of 1.4-4.2 ?M. The replacement fluid is essentially free of one or more of the trace elements selected from chromium, manganese, and copper.

Abstract: A method of treating diabetic retinopathy in a subject in need thereof includes administering to the subject a therapeutically effective amount of one or more agents that act as a trap of reactive aldehydes and/or inhibit diabetes-induced superoxide generation and capillary degeneration regulated by GPCR signaling pathways.