Abstract: The present invention relates to oral extended release composition, comprising memantine or its pharmaceutically acceptable salt as an active ingredient, resin complexation ingredient, release retardant, extended release coating system and the composition further comprising diluents, viscosity increasing agents, glidants, sweeteners, stabilizing agents, preservatives and other pharmaceutically acceptable excipients, wherein the drug-resin complex and drug-resin complex matrix particulates and coated drug-resin complex particulates have the specific particle size range. The present invention also relates to a process for the preparation of memantine or its salt oral extended release composition comprising the steps of drug-resin complexation, matrix resinate/particulates preparation process followed by extended release coating.

Abstract: The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

Abstract: The present disclosure relates to a method for delivering a mucoadhesive composition to the oral cavity of a subject. The mucoadhesive composition comprises one or more active agents, a mucoadhesive polymer, and water. The present disclosure is further related to a method for treating a disease, disorder, or condition, such as pharyngitis, aphthous stomatitis (canker sore), bacterial infection, radiation-induced mucositis, fibromyalgia, and diabetes, comprising administering the mucoadhesive composition to the oral cavity of a subject. The present disclosure is also related a mucoadhesive composition comprising one or more active agents, a mucoadhesive polymer, and water.

Abstract: Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.

Abstract: The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders.

Abstract: The present invention relates to a method for preparing 7?-methyl-19-aldehyde-4-androstene-3,17-dione by electrocatalytic oxidation. The method specifically includes: adopting an H-shaped electrolytic cell for reaction, in an anode chamber, using a metal oxide catalyst as a working electrode, using 7?-methyl-17,19-dihydroxy-4-androstene-3-one as a reaction substrate, and dissolving it in a mixed solvent to be used as an anolyte, and adding nitroxide radicals to be used as a medium; and in a cathode chamber, using a platinum sheet as a counter electrode, using a weakly alkaline solution as a catholyte, carrying out an electrocatalytic oxidation reaction in a constant temperature water bath, adding an organic solvent at the end of the reaction for extraction to obtain an organic extract liquor, and taking an organic layer and carrying out distilling under a reduced pressure to obtain 7?-methyl-19-aldehyde-4-androstene-3,17-dione.

Abstract: A small molecule compound IODVA1 has been found to have cellular inhibitory activity against several transformed cell lines including Ras-driven cells. IODVA1 decreases cell-cell and cell-extra cellular matrix interactions and reduces growth of Ras-driven tumors. Applicants also synthesized compound NIRA2 and showed in vitro and in vivo efficacy and potency against models of Ph+(BCR-ABL1) B-ALL and of colon adenocarcinoma xenografts.

Abstract: The invention provides compositions, formulations, and methods for treatment of malignancies via activation of an inflammatory response in the subject. Such compositions, formulations, and methods for are preferably used in conjunction with other therapies for the treatment and/or management of malignancies, e.g., chemotherapy and/or radiation. The invention also provides methods of monitoring immune activation in subjects with malignancies.

Abstract: Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.

Abstract: A method of treating Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: providing a subject with an effective amount of a modified tetracycline or derivative thereof to ameliorate or eliminate the AUD, SUD, tobacco use, pain, or proinflammatory disorder, and wherein the modified tetracycline or derivative thereof has reduced binding to a microbial ribosome and has the formula wherein R1 is acetyl, R2 is OH or acetyl, R3 is acetyl, R4 is H or acetyl, and R5 is acetyl.

Abstract: Disclosed herein are novel compounds and methods for the treatment of acute organ injury, including injuries resulting from ischemic events. The compounds may be used to treat organ including the brain, heart, or kidney, which have injured as a result of events such as stroke, cardiac arrest, traumatic brain injury, hemorrhagic shock, or subarachnoid hemorrhage.

Abstract: Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.

Abstract: The invention relates to compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.

Abstract: The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Abstract: The present invention relates to a composition comprising 2,4,6-trihydroxyacetophenone (THA) as an effective ingredient for prevention or treatment of prostate cancer. THA in the present invention is a main ingredient of Curcuma comosa. The composition of the present invention effectively inhibits the growth of prostate cancer by regulating in particular the activity of polo-like kinase 1 (PLK1) and thus is expected to find useful applications in use in the prevention, alleviation, and treatment of prostate cancer in future.

Abstract: The invention relates to the treatment of brain tumors, specifically to improved therapy for glioblastoma utilizing specific endocrine modulators and drug combinations. The compositions and uses thereof according to the invention employ androgen receptor (AR) inhibitors, either alone or in combination with receptor tyrosine kinase inhibitors and/or chemotherapeutic agents. According to certain advantageous embodiments, the use of the AR inhibitor enzalutamide, optionally in combination with epidermal growth factor receptor inhibitors such as erlotinib and alkylating agents such as carmustine and temozolomide, is contemplated.

Abstract: The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): wherein: , R1, R2, R3, R4, R5, R6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

Abstract: Neuroactive steroid anaesthetic agents, methods for their preparation and compositions comprising the same are disclosed. Also provided are scaled up and/or GMP methods for preparing neuroactive steroids, such as alfaxalone, alfadolone and alfadolone acetate.

Abstract: The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.