Abstract: The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: where R1, R2, R3, R3?, R4, R5, X1, X2, X3, X4, and n are described herein.

Abstract: Provided herein are solid forms comprising a compound of formula (I), or a stereoisomer, or a mixture of stereoisomers thereof, or a pharmaceutically acceptable salt thereof. Also provided herein are methods of synthesizing a compound of formula (I), pharmaceutical compositions comprising the same, and methods of treating, preventing, and managing various disorders using the compositions provided herein.

Abstract: Disclosed are covalent inhibitors of enhancer zeste homolog 2 (EZH2) which may be utilized as EZH2 targeting agents. The disclosed compounds may be characterized as substituted 3-amino-5-phenylbenzamide compounds. The disclosed compounds may be utilized as covalent inhibitors of EZH2 and further may be derivatized to form proteolysis-targeting chimeric molecules (PROTACs) that target EZH2 for degradation. The disclosed compounds and PROTACs may be used in pharmaceutical compositions and methods for treating cell proliferative disorders associated with EZH2 activity, such as cancer.

Abstract: The present disclosure relates to compounds of Formula (P) or (II?-0): (Formulae (I?), (II?-0)), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

Abstract: Provided is an effective method for using an orally administrable compound having an excellent Aurora A selective inhibitory effect, and a microtubule-targeting drug in combination. The present invention provides a method for treatment of malignant tumor by a combination of 1-(2,3-dichlorobenzoyl)-4-[5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl]methyl-4-piperidinecarboxylic acid (compound I) or a salt thereof and a microtubule-targeting drug, wherein the following administration schedule thereof is performed: one cycle involves 7 days; the microtubule-targeting drug is administered once; and the compound I or the salt thereof is administered for 3 consecutive days with cessation of the drug for remaining 4 days.

Abstract: The invention provides a method of treating a subject afflicted with a drug-induced movement disorder including levodopa-induced dyskinesia comprising periodically administering to the subject in need thereof an amount of pridopidine or pharmaceutically acceptable salt thereof effective to treat the subject. The invention further provides a method of treating a subject at risk of developing a drug-induced movement disorder, including levodopa-induced dyskinesia.

Abstract: The present application provides, inter alia, a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Y, Ar, X1, X2, X3, R1, R2, R3, R4, R5, and R6 are as described herein. Methods of making these compounds and methods of using these compound for treating diseases such as cancer are also provided.

Abstract: The present application discloses compounds having the following formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.

Abstract: Disclosed are a class of macrocyclic derivatives, a preparation method therefor, a pharmaceutical composition containing the derivatives, and the use thereof as therapeutic agents, particularly as XIa factor inhibitors and in the preparation of a drug for treating and preventing thromboembolisms and other diseases. Particularly disclosed are compounds shown by formula (I), an isomer thereof and a pharmaceutically acceptable salt thereof.

Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

Abstract: The inventors have found that the compounds of formula (I) protect cardiomyocytes. Accordingly, the disclosure provides a pharmaceutical composition for protecting a cardiomyocyte comprising a compound of formula (I) or an ester, oxide, pharmaceutically acceptable salt or solvate thereof. The pharmaceutical composition may be used for treating or preventing a disease associated with cardiomyocyte death, such as myocardial infarction, chronic heart failure, hypertensive heart failure, or dilated cardiomyopathy, especially for treating myocardial infarction.

Abstract: Provided herein are novel synthetic compounds having the structure of formula (1), wherein X is a substituted or unsubstituted aromatic or heteroaromatic mono- or polycyclic ring system; and Y is substituted or unsubstituted C5-C10 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions. The compounds and pharmaceutical compositions are useful for inhibiting growth of a bacterium.

Abstract: A compound 1-(morpholin-4-yl)-3-(naphthalen-2-yloxy)propan-2-ol, its synthesis, insecticidal compositions containing the same, and its use as an insecticidal agent.

Abstract: The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising the compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular to modulate CFTR protein or ABC protein activities.

Abstract: The present disclosure relates to methods for treating lupus nephritis 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. 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 (INS1007).

Abstract: The present disclosure relates to a pharmaceutical composition for treating brain cancer containing an aldehyde inhibitor and an anticancer drug. Since there are many types of brain cancer and the boundary between brain cells and tumor cells in brain cancer is not clear, brain cancer is particularly difficult to treat. The pharmaceutical composition of the present disclosure may further contain a biguanide-based compound as needed, wherein the compound is preferably phenformin. The pharmaceutical composition of the present disclosure is very effective for the treatment and improvement of prognosis of brain cancer, and has remarkable effects of killing cancer cells and inhibiting cancer stem cell characteristics, compared to when each of the active ingredients is administered alone. Thus, it is expected that the pharmaceutical composition of the present disclosure will be widely used in the field of brain cancer treatment.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis, ankylosing spondylitis, and psoriatic arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3?: a C1-C6 alkyl group or the like].

Abstract: Preparation of phosphorus fine chemicals from phosphate sources is described.

Abstract: The present disclosure is directed to a method of combatting opioid dependence in a subject who is misusing alcohol or susceptible to alcohol misuse. The method comprises treating the subject with an opioid agonist whilst managing their alcohol consumption using a step-wise interactive process, particularly where the process involves virtual cognitive behavioral therapy comprising a program for self-treatment. The self-treatment program could be embodied as a mobile medical application.