Abstract: Methods of inhibiting mutant EGFR and methods of treating a subject afflicted with a lung cancer having a mutant EGFR, having for example a C797 mutation, are described. The methods comprise administering to a cell or a subject in need thereof a therapeutically effective amount of a compound selected from 3-(1,3-benzoxazol-2-yl)-7-(diethylamino)-2H-chromen-2-one and a structurally related analog thereof; midostaurin; and AZD7622 and a structurally related analog thereof; and mixtures thereof. Compositions and combinations comprising the compounds of the disclosure as well as uses are also provided.

Abstract: Provided are methods of sanitizing a subject, and methods of anesthetizing a subject. Further provided are methods of treating and/or preventing dermatological disorders, reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPA1 and/or TRPV4 inhibitor. Further provided are compositions including a TRPA1 and/or TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application.

Abstract: Provided herein are methods of treating a CDKL5 deficiency with tideglusib or a derivative thereof.

Abstract: A method for reducing pulmonary hypertension in a mammal that employs FK506 is provided. In certain embodiments, the method comprises administering FK506 to a mammal having pulmonary arterial hypertension associated with defective MBPR2 signaling at a dosage sufficient to reduce blood pressure in the pulmonary artery of the mammal.

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

Abstract: The present disclosure provides a combination comprising: (i) a drug against tuberculosis, or a pharmaceutically acceptable salt thereof, and (ii) a compound of Formula II, or a pharmaceutically acceptable combination thereof. The combination may be used in the treatment and/or prevention of tuberculosis.

Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.

Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.

Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.

Abstract: This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.

Abstract: A novel quantum-based computational process for drug discovery and design was used to identify potential novel liver-stage anti-malarial therapeutic molecules. The approach combined the latest big-data advances in high-throughput bioassay development with fundamental scientific knowledge to generate new pharmaceutical leads. Several molecules with no previous association with anti-parasitical activity were identified. These molecules and there use in prevention and/or treatment of Plasmodium infections are provided.

Abstract: The present invention relates to methods of inhibiting TIE2 kinase useful in the treatment of tumor growth, invasiveness, intravasation, dissemination, metastasis, and immunosuppression. Specifically, the invention relates to methods of using 1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea and salts thereof of Formula I.

Abstract: Certain embodiments described herein include methods and formulations for treating or preventing symptoms and conditions associated with exposure to ionizing radiation and/or radiation generally. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.

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 relates to methods of treating a condition associated with mTORC1 hyperactivation or TSC2-deficient cancer, the method comprising administering to a subject having the cancer a pharmaceutically-effective amount of a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor. In some embodiments, the condition associated with mTORC1 hyperactivation is tuberous sclerosis complex (TSC). In some embodiments, the condition associated with mTORC1 hyperactivation is lymphangioleiomyomatosis (LAM). In some embodiments, the condition associated with mTORC1 hyperactivation is TSC2-deficient cancer.

Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.

Abstract: The present disclosure provides a method of treating a subject that is resistant to one or more drugs by identifying a subject having one or more drug resistant cells; administering to the subject a pharmaceutically effective amount of an inhibitor compound, and contacting one or more drug resistant cells with the inhibitor compound to reduce the export of the inhibitor compound from the one or more drug resistant tumor cells and to block the transport of drug(s) from the one or more drug resistant cells.

Abstract: The present invention relates to the use in therapy of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione or a pharmaceutically acceptable salt thereof, to pharmaceutically acceptable salts of 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione and to pharmaceutical formulations comprising 6-((4-(2,3-dimethylphenoxy)piperidin-1-yl)methyl)pyrimidine-2,4(1H,3H)-dione or a pharmaceutically acceptable salt thereof.

Abstract: Inappropriate activation of innate immune responses in nematode intestinal epithelial cells underlies the pathophysiology of some inflammatory disorders. Immunostimulatory xenobiotics are known to protect nematodes from bacterial infection (e.g., Pseudomonas aeruginosa). Conversely, these same xenobiotics are toxic to uninfected nematodes. These xenobiotics were subjected to a forward genetic screen in uninfected nematodes to identify nematode mutants that were resistant to the deleterious effects of these xenobiotics. These resistant nematode strains contained hypomorphic mutations in each of the known components of the p38 MAP kinase cassette (tir-1, nsy-1, sek-1 and pmk-1), demonstrating that hyperstimulation of p38 MAPK innate immune responses may be responsible for the induced toxicity. A second genetic screen using dominant activators of the p38 MAPK pathway identified a single allele that had a gain-of-function (gf) mutation in nsy-1, the MAP kinase kinase kinase that acts upstream of p38 MAPK pmk-1.

Abstract: Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.

Abstract: Provided herein are compositions and methods for treating ER+, HER2? HRG+ breast cancer (e.g., metastatic ER+, HER2? breast cancer) in a patient by administering to the patient an anti-ErbB3 antibody (e.g., seribantumab), a CDK4/6 inhibitor (e.g., palbociclib), and an endocrine based therapy (e.g., letrozole or fulvestrant) according to a particular clinical dosage regimen (i.e., at a particular dose amount and according to a specific dosing schedule). Also provided herein are compositions and methods for treating ER+, HER2? HRG+ breast cancer (e.g., metastatic ER+, HER2? breast cancer) in a patient by administering to the patient an anti-ErbB3 antibody (e.g., seribantumab) and an endocrine based therapy (e.g., letrozole or fulvestrant) according to a particular clinical dosage regimen (i.e., at a particular dose amount and according to a specific dosing schedule).

Abstract: The present invention relates to a substance with pharmaceutical activity against a medical condition for use in a treatment of said medical condition in combination with a computer program product comprising instructions causing a computer to perform a method comprising the steps—providing a patient with a set of questions according to a question schedule, wherein said set of questions is specific to the pharmaceutical product;—collecting answers to said questions from said patient;—subjecting said answers to a set of functions specific for the set of questions and the pharmaceutical product thereby generating patient specific feedback information;—providing said feedback information to the patient; and optionally extracting clinically relevant information from said answers and providing said clinically relevant information to a database adapted for collecting clinically relevant information during clinical use of said substance.

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: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

Abstract: Methods of treating developmental disorders and/or seizure disorders with etifoxine, a deuterated analog of etifoxine, or a pharmaceutically acceptable salt, solvate, or prodrug thereof are provided. The methods provide therapeutic compositions that may be used to improve one or more symptoms of the developmental disorder and/or seizure disorder.

Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.

Abstract: A method of treating a patient suffering from TNBC by a multidisciplinary method involving treating the patient with a plurality of the following treatments: i) one or more checkpoint inhibitors; ii) hyperthermia treatment; iii) low dose chemotherapy; iv) Interleukin-2 (IL-2); and v) a compound selected from the group consisting of taurolidine, taurultam, oxathiazin-like compounds, and combinations thereof.

Abstract: A method of reducing a subject's plasma triglyceride level, comprising administering to a subject in need thereof a gamma-secretase inhibitor in an amount effective to reduce the subject's plasma triglyceride level.

Abstract: The invention comprises methods of modulating the complement cascade in a mammal and for treating and/or preventing diseases and disorders associated with the complement pathway by administering a compound of Formula I or Formula II, such as, for example, 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof, that inhibit dipeptidyl peptidase 1 (DPP1) activity. Methods provided herein are useful for prophylaxis, increasing the lung function in a patient, and/or and/or decreasing the rate of pulmonary exacerbation in a patient. In one embodiment, the compound of Formula (I) is (2S)—N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide.

Abstract: Disclosed is a composition for the prevention or treatment of diabetic complications, containing a benzodiazepine-based compound, thereby effectively preventing or treating diseases resulting from hyperglycemia, which is the leading cause of diabetes, especially diseases caused by vascular leakage.

Abstract: Provided is a method of preventing and/or treating a skin disorder and/or an oral disorder including administering to a subject in need thereof an effective amount of a compound of formula (I) or a prodrug or derivative thereof, and salts thereof.

Abstract: The present disclosure relates to novel pharmaceutical composition for the administration of testosterone or testosterone derivatives using an aqueous nasal administration. The present disclosure also provides methods of treatment of diseases and disorders associated with fear and anxiety, a decrease in libido, or hypogonadism.

Abstract: The present invention relates to certain cortexolone derivatives of formula (I) and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.

Abstract: This invention relates to methods of treating or preventing a sleep disorder, sleep disturbance, or related symptom in a subject with aminosterols or pharmaceutically acceptable salts or derivatives thereof. In particular, the disclosed methods generally comprise administering an aminosterol to a subject in need, thereby stimulating an aminosterol-induced CNS response to treat and/or prevent a sleep disorder, sleep disturbance, or related symptom.

Abstract: Provided herein are dietary supplement compositions comprising a plurality of beadlets and an oil. Provided herein are also dietary supplement compositions comprising a plurality of mini-tabs and oil. The beadlets or mini-tabs comprise at least one nutrient that is miscible in aqueous solution, and the oil comprises at least one fat-soluble nutrient. The composition may be contained within one or more capsules, and be packaged with a scented insert.

Abstract: Methods for individualized therapy of arthritic pain using a non-steroidal anti-inflammatory drug (COX-2 inhibitor). Said methods comprise basing COX-2 inhibitor dose on each patient's pharmacokinetic response to said COX-2 inhibitor.

Abstract: A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.

Abstract: The present invention provides modified metformin compounds, particularly mito-metformin compounds, and pharmaceutical compositions thereof. Methods of using the compounds to provide neuroprotection and in the treatment and/or prevention of neurodegenerative diseases are also described.

Abstract: Combination therapy with sorafenib or regorafenib and a phosphoramidate prodrug of troxacitabine with the formula: where Y is C1-C8 straight or branched chain alkyl, X is H, halo, C3-C4cycloalkyl or C1-C4alkyl and Z is H or fluoro, or a pharmaceutically acceptable salt thereof, shows surprising utility in the treatment of liver cancer or liver metastasis.

Abstract: The present disclosure relates to, inter alia, a method of treating cancer in a human patient in need thereof, comprising administering a therapeutically effective amount of a substrate of AKR1B1, AKR1B10, or both to said patient, wherein said patient has, or is suspected to have, cancer cells with elevated levels of AKR1B1, AKR1B10, or both, wherein said substrate is not 2-deoxy-D-glucose.

Abstract: [Problem] To provide: an agent for increasing intestinal butyric acid which is capable of effectively increasing intestinal butyric acid; a food composition for increasing intestinal butyric acid; a proliferation agent for butyric acid-producing bacteria; a food composition for proliferating butyric acid-producing bacteria; a method for increasing intestinal butyric acid; a method for proliferating butyric acid-producing bacteria; a method for treating or preventing intestinal inflammation, fatty liver, diabetes, colorectal cancer or obesity using the same; and use of 1-kestose for producing a pharmaceutical preparation for treatment or prevention of these diseases. [Solution] An agent for increasing intestinal butyric acid and a proliferation agent for butyric acid-producing bacteria, each comprising 1-kestose as an active ingredient. According to the present invention, intestinal butyric acid in humans or animals can be easily and effectively increased with little side effects or safety concerns.

Abstract: Preparations of glycan therapeutics, pharmaceutical compositions, dietary supplements and medical foods thereof are provided, and methods of using said gycan therapeutics, e.g. in cancer therapy.

Abstract: The present application provides a method of increasing relative abundance of Oscillospira in gastro-intestinal tract of a subject. The method comprising administering to said subject at least 2.5 g per day of fructo-oligosaccharide, such that the abundance of Oscillospira is increased to a statistically significant level when measured by F-test. A composition for increasing relative abundance of Oscillospira in gastro-intestinal tract of a subject is also disclosed.

Abstract: The present application provides a method of increasing abundance of Lachnospira in gastro intestinal tract of a subject. The method comprising administering to said subject at least 5 grams per day of fructo-oligosaccharide, such that the abundance of Lachnospira is increased to a statistically significant level when measured by F-test. A composition for increasing abundance of Lachnospira in gastro intestinal tract of a subject is also provided.

Abstract: The present disclosure provides methods, compositions, and kits for treating cancer using a combination of L-rhamnose and a leucine aminopeptidase inhibitor.

Abstract: The present invention relates to therapies and therapeutic agents for use in the treatment of cardiomyopathies. In particular, the invention is concerned with, but not limited to therapies and therapeutic agents for use in the treatment of hypertrophic cardiomyopathy. Such therapeutic agents comprise hypomethylating agents.

Abstract: The present invention relates to the use of a DBait molecules by systemic routes without any combination with an endosomolytic agent.