Abstract: Provided herein are novel piperazine compounds and pharmaceutical compositions thereof comprising the piperazine compounds for inhibiting serotonin reuptake and/or acting as 5-HT1A receptor agonists. Also provided herein are methods for preparing the novel piperazine compounds and pharmaceutical compositions thereof, and uses of them in treating central nervous system (CNS) dysfunction.

Abstract: Provided are methods and compositions for the treatment of depression and anxiety. The compositions contain scopolamine, or an analog thereof, and can optionally include one or more psychoactive agents. Further provided is an inhaler containing scopolamine, or an analog thereof, in a pharmaceutically acceptable carrier.

Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.

Abstract: Analogs of PPAR5 and analogs of 20-OH-PGE2, which are PPAR5 agonists and 20-OH-PGE2 antagonists, respectively, and methods of using the same for inducing osteogenesis or chondrogenesis, are disclosed.

Abstract: A cancer chemotherapeutic agent that is particularly kinase suppressing and/or any other signaling pathway interfering agents and pharmaceutical formulations/compositions involving the same and its process of manufacture is provided. A potential the cancer chemotherapeutic agent is provided which apart from stated anticancer activity as a proven kinase suppressing and/or any other signaling pathway interfering agent could also involve specific potential binding affinity towards the intramolecular G-Quadruplex DNA structure and/or other potential quadruplex forming sequences over duplex DNA structures favors further diverse end use and application including but not limited to antiaging, antiangiogenic, antiproliferative, antitumor, antibiotic, antiviral, antifungal and multiple anticancer therapeutics, and also possesses favorable cytotoxicity values towards uncontrollably proliferative cells by inducing apoptosis irrespective of cells' p53 status, without being cytotoxic to normal cells.

Abstract: Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), as well as therapeutic methods for use of such compounds to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia. Examples of compounds include thiadiazole, isoxazole, 1,2,4-triazole, thiazole, indole, pyrazole, and pyrrolinone derivatives.

Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I); in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

Abstract: Compounds having the following formula (I): or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN? by acting on Tyk-2 to cause signal transduction inhibition.

Abstract: Described are ROR? modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.

Abstract: Patients which are treated with stimulants (e.g., CNS stimulants, sympathomimetic amine, or anorectic/anorexigenic), such as patients being treated for attention deficit/hyperactivity disorder or obesity, often are at risk in developing high blood pressure. Similarly, patients which are treated with analgesics such as non-steroidal anti-inflammatory drugs (NSAIDs) over an extended period of time risk developing high blood pressure. These and other iatrogenic therapies (therapies which inadvertently cause an increase in, e.g., blood pressure) are addressed by providing the patient with one or more antihypertensive drugs, most preferably calcium channel blockers, during the treatment period. The CNS or NSAIDs can be provided separately or together with the antihypertensive drugs or as part of a combined composition. The adjunctive therapy can prevent or reduces cardiovascular disease and other complications of high blood pressure attendant with these iatrogenic therapies.

Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.

Abstract: A solid supplement comprising the following components (A) and (B): (A) sphingomyelin in an amount of from 0.15 to 7% by mass; and (B) phosphatidyl inositol or a salt thereof, wherein the mass ratio of the content of phosphatidyl inositol or the salt thereof (B) in terms of phosphatidyl inositol content to the content of sphingomyelin (A) in the solid supplement, i.e., [(B)/(A)], is from 0.05 to 3.

Abstract: A composition for treating ear infections in animals includes an antifungal agent, an antibiotic agent, a steroidal anti-inflammatory agent, and an acid dissolved to form a liquid. The acid aids in keeping the steroidal anti-inflammatory agent in solution, and enhances the bactericidal effect of the composition. The method of preparing such composition includes dissolving the antifungal agent, steroidal anti-inflammatory agent, and acid in dehydrated alcohol, dissolving the antibiotic agent in propylene glycol, combining the two solutions together, heating the combination and then cooling the composition. Several drops of the composition are applied at least twice per day to the affected area of the animal's ear.

Abstract: This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Abstract: Compounds are provided having agonistic activity against G protein-coupled receptor 35 (GPR35). The compounds are useful for providing antinociception, providing neuroprotection in case of stroke or ischemia, or treating gastric inflammation.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: Topoisomerase II alpha (topo II?) is exported from the cell nucleus in human myeloma cells by a chromosome-maintenance protein-1 (CRM1)-dependent mechanism, resulting in topo II inhibitor resistance. The nuclear export signal (NES) of topo II? is unique, making it a potential target for small molecule inhibitors. Small molecules NES inhibitors were identified, which inhibited binding of topo II? to the export receptor CRM1. Inhibition was specific to topo II? as p53 trafficking was unaffected along with topo II? protein expression and function (decatenation). These topo II?-specific nuclear export inhibitors may potentially lead to a new approach in circumventing drug resistance in multiple myeloma. The compounds provide a protocol for treating multiple myeloma or an oncogenic disease. Further, the topoisomerase II nuclear export signal inhibitor may be combined with a topoisomerase II inhibitor.

Abstract: Certain embodiments are directed to methods of treating respiratory infection by administering an H2S donor.

Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.