Abstract: The present invention provides methods for treating a cancer in a subject and for inhibiting tumor growth, metastasis or a dihydrorotate oxygenase enzyme activity of a tumor or cancer cell. At least one trisubstituted benzotriazole derivative with the formula (I) is administered to the subject or is contacted with the cancer cell. Compounds of formula (I) have substituents R1, R2 and R3 which have the meanings given in the specification, and pharmaceutically acceptable salts thereof.

Abstract: Described herein are compounds having Formula I or Formula II: wherein each dashed line independently represents a saturated or unsaturated bond; R1 and R?1 are aryl or heteroaryl as defined herein; and R2 and R?2 are as defined herein. Further described is a method of inhibiting nuclear translocation of ERK1/2 in a cell, by contacting the cell with a compound having Formula I or Formula II. The compounds may also be for use in treating a disease or disorder associated with nuclear translocation of ERK1/2.

Abstract: A method of treating cancer that includes administering a therapeutically effective amount of an organoselenium benzimidazole compound of Formula (I), where R is at least one selected from the group consisting of an alkyl group having 1 to 6 carbon atoms, an unsubstituted benzyl group, a para halo-substituted benzyl group, and an allyl group.

Abstract: The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.

Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl) pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.

Abstract: This invention, in at least some embodiments, relates to an inventive molecule, compositions comprising same, and methods of use thereof for treatment of a neurological disorder.

Abstract: Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

Abstract: Disclosed herein are compositions and methods for topical delivery of mTOR inhibitors. In one embodiment, an anhydrous composition includes one or more mTOR inhibitors, one or more solvents, one or more gelling agents, and one or more antioxidants. Also disclosed herein are methods to treat skin disorders using such compositions.

Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.

Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: The present invention discloses an oxime ether compound with novel structure. The structure is shown in general formula I. The definition of each substituent in the formula is provided in the description. The compound of general formula I has excellent microbicidal 1 activity, and has good control effects on plant bacterial diseases and fungal diseases. The present invention comprises an application of the compound of the general formula I as a microbicide in agriculture and other fields.

Abstract: This document discloses a novel class of compounds for inhibiting bacterial growth and treating bacterial infection. The compounds target a key step of the futalosine pathway and therefore are effective for the selective inhibition of certain bacterial species and genera with reduced side effect in comparison with conventional antibiotics.

Abstract: The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface asialoglycoprotein receptor (ASGPR). The cell surface ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided herein methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.

Abstract: A method for cytotoxically treating cancer cells includes contacting the cancer cells with a composition comprising a compound of Formula I. The compound of Formula I is contacted with the cancer cells in an amount effective to reduce the number of cancer cells by at least 50%. A method for preparing the compound of Formula I.

Abstract: Provided herein is a process for the preparation of (R)—N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide, intermediates thereof, and salts of the foregoing.

Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.

Abstract: The present disclosure pertains to a pharmaceutical composition comprising fursultiamine or a salt thereof for prevention or treatment of macular degeneration. Fursultiamine decreases the upregulated expression of HIF-1? in retinal pigment epithelial cells and suppresses the growth of choroidal vascular endothelial cells. The pharmaceutical composition comprising fursultiamine or salts thereof according to the present disclosure can be used as a therapeutic agent for various neovascular ocular diseases.

Abstract: The present invention provides pharmaceutically acceptable salts of compounds of Formula I that are potent EP4 receptor antagonists and can be used for treating cancer or inflammatory diseases alone or in combination with antibody therapy, radiation therapy, anti-metabolite chemotherapy to a subject in need thereof.

Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amount of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.