Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is selected from the group consisting of a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl and C1-C6haloalkylsulfonyl; X3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy and C1-C6alkylthio; X4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C1-C4alkoxy and C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b independently of each other are a halogen atom, or R3a and R3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C2-C5haloalkylene chain, and R3c is selected from the group consisting of a hydrogen atom, halogen atom, C1-C5haloalkyl, C1-C4haloalkoxy and C1-C4haloalkylthio, with a proviso that in case where X1 is a fluorine atom, chlo

Abstract: The object of the present invention is to inhibit oxidative metabolism of a compound of formula I by co-administration with ritonavir, a cytochrome P450 inhibitor.

Abstract: Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodmg comprises a step of coupling the drag molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.

Abstract: The current invention is in the field of molecular biology/pharmacology and provides methods of using compounds that modulate the effects of GPR30/GPER for treating obesity and diabetes (preferably agonists) as well as disease states and/or conditions that result from excessive formation of reactive oxygen species (preferably antagonists). These compounds may function as agonists and/or antagonists of the disclosed estrogen receptor and/or modulate the expression/upregulation of nox and nox-associated reactive oxygen species (ROS).

Abstract: Provided herein are novel and selective high affinity ?3?4 nicotinic acetycholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the ?3?4 nicotinic acetycholine receptor using the compounds and compositions disclosed herein.

Abstract: The present invention discloses new medical uses of phosphodiesterase 4 (PDE 4) inhibitors for treating dyslipoproteinaemia and of diseases when respectively correlated or associated with dyslipoproteinaemia or lipoprotein imbalance, in particular abnormally high low density lipoprotein (LDL) in blood or serum, such as endothelial dysfunction, cardiovascular diseases, in particular arteriosclerosis, myocardial infarction, stroke, peripheral artery disease, and vascular stenosis or restenosis, independent and distinct from inflammatory diseases or conditions such as inflammatory-associated cardiovascular pathology and cardiac hypertrophy. Accordingly the present invention allows reducing cardiovascular risks in new clinical settings, especially in circumstances of abnormal high LDL levels and especially LDL-cholesterol and LDL-triglyceride levels.

Abstract: The present invention relates to methods of treating a tumor or treating cancer in a subject having a p53 DNA contact mutation that involve administering, to the subject, a ROCK inhibitor. Also disclosed is a method of identifying a subject as a candidate for such treatment.

Abstract: Within the scope of the present invention is a new pharmacological strategy for the treatment of tumors based on anti-tumoral immune responses.

Abstract: The present invention relates to a cyclohexene derivative, a preparation method thereof, and a pharmaceutical composition for preventing or treating metabolic disease containing the cyclohexene derivative as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.

Abstract: The present disclosure pertains to a pharmaceutical combination comprising (a) an alpha-isoform specific PI3K inhibitor, (b) an MDM2 inhibitor, and optionally (c) a BCL-2 inhibitor; combined preparations and pharmaceutical compositions thereof; the uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer a subject in need thereof comprising administering a therapeutically effective amount of such combination.

Abstract: Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.

Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.

Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.

Abstract: The present invention generally relates to a topical composition including loperamide and a pharmaceutically acceptable carrier and to a method of using such a composition. One embodiment of the method provides for analgesia or antihyperalgesia.

Abstract: The present invention relates to a pharmaceutical preparation comprising modified release nicotinamide, as well as its use in a method of preventing and/or treating of elevated serum phosphate levels (hyperphosphatemia) and/or dyslipidemia, both particularly resulting from renal failure.

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: The present invention provides compositions and methods for providing controllable local delivery of a conjugate of chloroquine (CQ) and a bisphosphonate to treat diseases characterized by abnormal bone metabolism. In certain embodiments, the invention is used as a treatment for a subject with diseases and disorders characterized by bone loss.

Abstract: This invention concerns the use of mefloquine in relation to Mycobacterium tuberculosis. This invention also concerns the combination of mefloquine with drugs used in first and second choice treatment of tuberculosis, achieving a reduction in the treatment period of tuberculosis (TB) and the treatment of multi-drug resistant tuberculosis (MDR-TB).

Abstract: The present invention relates to a benzopiperidine derivative, a preparation method thereof and a medical use thereof. In particular, the present invention relates to a benzopiperidine derivative as shown by general formula (I), a preparation method thereof and a pharmaceutical composition containing the derivative, as well as a use thereof as an estrogen receptor modulator in the prevention and/or treatment of estrogen receptor-mediated or dependent diseases or conditions. Preferably, the disease is breast cancer. The substituents in the general formula (I) are the same as those defined in the description.

Abstract: We have determined that MeCP2 protein mediates modulation of long-gene expression in the brain and results in neurological dysfunction associated with autism spectrum disorders, including but not limited to, Fragile X Syndrome, Rett syndrome, and Angelman syndrome (AS). In particular, a lack of MeCP2 protein causes up-regulation of long gene expression in the brain which corresponds with the pathology of Rett syndrome and Fragile X Syndrome, while too much MeCP2 protein results in excessive repression of long gene expression in the brain and pathology related to MeCP2 duplication syndrome. Accordingly, embodiments of the invention are directed to methods for treatment of autism spectrum disorders. The methods involve administration, to a subject, agents that modulate the expression of long genes in the brain.

Abstract: The present invention relates to the field of pharmaceutical chemistry, and specifically relates to a fused heterocyclic compound derivative and an application thereof. The fused heterocyclic compound derivative has the structure of general formula (I), and can be used to treat neuropsychiatric diseases.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where x, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.

Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.

Abstract: The present invention relates to improved compositions and methods for the treatment or prevention of various diseases, including forms of depression, including, for example, breakthrough depression and treatment-refractory depression, and other mood disorders, as well as Parkinson's disease, bipolar disorder, bipolar disorder, attention deficit disorder (ADHD), Restless Leg Syndrome (RLS), and obesity. In some embodiments, the compositions and methods comprise low dose naltrexone or related opioid antagonists.

Abstract: The present invention relates to morphinans selected from nalmefene and naltrexone and their related derivatives of formula (I), and pharmaceutical formulations thereof, for use in the prevention and treatment of a liver disease selected from the group consisting of NASH (non-alcoholic steatohepatitis), NAFLD (non-alcoholic fatty liver disease) and ASH (alcoholic steatohepatitis).

Abstract: MyD88 inhibitor can be used to prevent, for example, post myocardial infarction ischemia reperfusion injury, post severed limb replantation ischemia reperfusion injury and post transplantation ischemia reperfusion injury, and to play important role in production of organ preservation solution, cell preservation solution etc. Furthermore, results of in vitro experiment show that MyD88 inhibitor TJM2010-5 can effectively reduce the level of inflammatory factors in graft through inhibiting the pathway, which means that it is closely related to the generation of inflammatory factors, therefore, the TJM2010-5 can become the effective method for treating of various inflammations, prevent the vicious circle and vicious transformation of chronic inflammation, and prevent and treat inflammatory cancerization etc.

Abstract: Indazole compounds for treating various diseases and pathologies are provided. More particularly, the use of an indazole compound or analogs thereof, in the treatment of inflammatory diseases or disorders is provided.

Abstract: Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.

Abstract: Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: [Problem] A compound useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for cancer immunotherapy, and/or a pharmaceutical composition for immunological activation is provided. [Means for Solution] The present inventors have conducted intensive studies for the purpose of creating a pharmaceutical composition for cancer immunotherapy and/or a pharmaceutical composition for immunological activation.

Abstract: Various scaffolds of small molecules capable of binding to the active site of sortilin are identified by in silico methods. These scaffolds include norbornene anhydride amino acid adducts and 2-substituted 3-oxo-1,2,3,4-tetrahydro-2-quinoxalines. These sortilin ligands increase the uptake of glucose in 3T3L1 cells and can be employed in compositions to increase uptake of glucose for the treatment of diabetic patents.

Abstract: In some embodiments, the invention relates to a BTK inhibitor or a pharmaceutically acceptable salt, cocrystal, ester, prodrug, solvate, hydrate or derivative thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to imidazopyrazine compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of a hyperproliferative disorder, an inflammatory disorder, an immune disorder, or an autoimmune disorder.

Abstract: A method of treating obesity and obesity-related disorders in a mammal is provided. The method comprises the step of administering to the mammal a compound or entity that inhibits the HTR2a receptor.

Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

Abstract: Provided herein are compositions and methods for the treatment of autoimmune and alloimmune diseases and conditions, including rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease (IBD) (e.g., Crohn's disease, ulcerative colitis), optic neuritis, Neuromyelitis Optica, Sjögren's syndrome, psoriasis, systemic scleroderma, Ankylosing Spondylitis, autoimmune hepatitis, Graft vs host disease (GvHD), and organ transplant rejection. Said compositions useful for treating autoimmune diseases comprise pyrrolo-pyrazole PKC inhibitors.

Abstract: A pharmaceutical composition comprises: a) 5 wt % to 95 wt % of a HCl salt of Compound (1).xH2O by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt % to 95 wt % of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/mL to 20 mg/mL of Compound (1) in water; and b) 0.01 M to 0.1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1) that includes the HCl salt of Compound (1).xH2O and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HCl salt of Compound-(1).xH2O and the pH modifier to form 1 mg/mL to 20 mg/mL of Compound (1) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, and treating influenza each independently employ such pharmaceutical compositions.

Abstract: Methods of treating or slowing the growth of a lesion associated with geographic atrophy and methods of evaluating a drug or agent for use in treating, reducing the progression of or slowing the growth of a lesion associated with geographic atrophy.

Abstract: In part, the disclosure relates to methods of treating myeloproliferative disorders by administering one or more Serum Amyloid Protein (SAP) proteins. In certain aspects, the method further comprises monitoring treatment efficacy by measuring change in mutant allele burden. In certain aspects, the disclosure relates to methods of treating myelofibrosis in patient sub-populations who carry myelofibrosis-associated mutations in some of their cells by administering an SAP protein.

Abstract: In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat dermatoses, such as psoriasis, atopic dermatitis, contact dermatitis, scleroderma, and cutaneous lupus erythematosus. In other embodiments, the methods of the invention further comprise the step of administering a therapeutically effective dose of an anti-inflammatory agent.

Abstract: The present invention relates to a pharmaceutical combination comprising, separately or together, (1) a first agent which is an ALK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof. The invention further relates the use of such combination in the treatment or prevention of proliferative diseases.

Abstract: The present invention provides the use of protein kinase inhibitors, in particular JAK2 inhibitors of formula (I), as set forth in the specification, in the treatment of solid organ transplant rejection and graft versus host disease (GvHD). Also provided are combination therapies for the treatment of solid organ transplant rejection and graft versus host disease.

Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.

Abstract: The disclosed subject matter provides pyrazolone derivative compounds, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.

Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof that are useful as antibacterial agents. The compounds are useful as inhibitors of bacterial gyrase activity and of bacterial infections, and have the structure of Formula (I): as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.

Abstract: Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.

Abstract: The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.

Abstract: To provide a pharmaceutical agent or an antitumor agent useful for the treatment and/or prevention of gastrointestinal cancer, leukemia, pituitary tumor, small cell lung cancer, thyroid cancer, and neuroastrocytoma. The antitumor agent containing, as an active ingredient, a 1,5-benzodiazepine derivative represented by the following formula (1): (wherein R1 represents a C1-6 alkyl group; R2 represents a phenyl group or a cyclohexyl group; and Y represents a single bond or a C1-4 alkylene group) or a pharmaceutically acceptable salt thereof.

Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.