Abstract: The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49).

Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.

Abstract: Provided herein are stable amlodipine oral liquid formulations. Also provided herein are methods of using amlodipine oral liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).

Abstract: A method for treating AR+ breast cancer in a subject comprising administering to the subject an AR agonist (e.g., SARMs such as RAD140), or in combination with one or more therapeutic agents selected from the group consisting of cdk4/6 inhibitors, m-TOR inhibitors, PI3k inhibitors, PARP inhibitors, BCL-2 inhibitors, and MCL-1 inhibitors.

Abstract: The present invention relates to a preparation method and application of a micelle preparation containing thymol and a derivative thereof. The micelle preparation contains thymol, a thymol derivative, a derivative (CST) formed by vitamin E and chondroitin sulfate, a derivative (TPGS) formed by vitamin E and polyethylene glycol, and water. On the one hand, the thymol is transformed into its derivative, so that the pungency degree of the thymol is effectively reduced, and the gasoline smell of the thymol is masked; on the other hand, the thymol and the derivative of the thymol are encapsulated by the vitamin E derivative to form micelles, so that the two components are effectively solubilized, and the biological adhesion of the micelle preparation is greatly enhanced. The micelle preparation can be used for oral ulcer treatment, oral care and correction of related oral cavity abnormalities.

Abstract: Disclosed is a method for improving the sensorial properties of an oil-in-water type emulsion for topical application, including, for 100% of its mass, 5% to 30% by weight of glycerol, characterised in that the oil-in-water type emulsion for topical application includes an effective quantity of a mixture of saturated cyclic or acyclic, linear or branched hydrocarbons, of which at least 95% by weight have between fifteen and nineteen carbon atoms. Also disclosed is a new oil-in-water type emulsion for topical use, including the mixture, and to the use of same in cosmetics.

Abstract: Disclosed is a method for improving the sensorial properties of an oil-in-water type emulsion for topical application, including, for 100% of its mass, 1% to 30% by weight of glycerol, characterised in that the oil-in-water type emulsion for topical application includes an effective quantity of a mixture of saturated cyclic or acyclic, linear or branched hydrocarbons, of which at least 95% by weight have between fifteen and nineteen carbon atoms. Also disclosed is a new oil-in-water type emulsion for topical use, including the mixture, and to the use of same in cosmetics.

Abstract: Disclosed are a nitrogen-containing fused heterocyclic SHP2 inhibitor compound, a preparation method, and use. The nitrogen-containing fused heterocyclic SHP2 inhibitor compound is represented by formula I below. The compound has high inhibitory activity for an SHP2 enzyme and tumor cell proliferation, and has good druggability.

Abstract: This document relates to materials and methods for treating fibrosis (e.g., pulmonary fibrosis). For example, this document provides methods for using one or more fatty acid synthase (FASN) inhibitors to treat a mammal having fibrosis (e.g., pulmonary fibrosis), and/or a complication associated with fibrosis (e.g., hypoxia caused by pulmonary fibrosis).

Abstract: The present disclosure relates to compositions including a phenylbutyrate compound and a bile acid, and methods of processing such compositions.

Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.

Abstract: The present invention provides methods of treating Restless Legs Syndrome (RLS) including administering to a subject an effective amount of a dopamine D1 receptor antagonist. Compositions and kits useful for treating RLS are also provided.

Abstract: The present invention provides a method of treating patients with long acting injectable paliperidone palmitate formulations.

Abstract: The invention provides methods for treating or preventing developmental disorders associated with mutations in the OCD1 gene.

Abstract: The present disclosure provides compounds represented by Formula I: wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are EED inhibitors. EED inhibitors are useful for the treatment of cancer and other diseases.

Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.

Abstract: The present invention provides methods and compositions for treating epithelioid cell tumors (such as a PEComa) by administering a composition comprising nanoparticles comprising an mTOR inhibitor and an albumin.

Abstract: The present invention relates to injectable pharmaceutical compositions comprising therapeutically effective amount of succinylcholine chloride, one or more pharmaceutically acceptable aqueous solvents, and one or more stabilizing agents selected from aliphatic polyols; lower alkyl alcohols; amino acids having at least one additional amino, carboxyl or hydroxyl group; amino alcohols; and aliphatic dicarboxylic acids having at least one hydroxyl or amino group, or ?-? unsaturation. The compositions are stable at room temperature for at least 30 days. Methods of manufacturing the injectable pharmaceutical compositions are also provided. The composition may be provided in a sealed container, e.g., an ampoule, vial and pre-filled syringe, and are suitable for subcutaneous, intravenous or intramuscular administration as an adjunct to general anesthesia, to facilitate tracheal intubation, and/or to provide skeletal muscle relaxation during surgery or mechanical ventilation.

Abstract: Aspects of the disclosure relate to compositions, kits, and methods for the treatment of cancer that utilize a selective histone deacetylase 3 (HDAC3) inhibitor. In some aspects, the compositions, kits, and methods relate to use of a selective HDAC3 inhibitor in combination with an immunotherapy agent (e.g., an immune checkpoint inhibitor).

Abstract: The present invention relates to a pharmaceutical composition containing ?-lapachone as an active ingredient for prevention or treatment of cholestatic liver disease, and can provide agents for effectively preventing and treating cholestatic liver disease.