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: Disclosed are compounds of Formula (I) and (Ia): or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer or a deuterated analog thereof, wherein R4, R5, R6, and R7 are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.

Abstract: Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.

Abstract: A zirconium metal-organic framework, which is a coordination product formed between zirconium ion clusters and a linker that links together adjacent zirconium ion clusters, wherein the linker is of formula (I) wherein R1 to R4 are independently hydrogen, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted arylalkyl, an optionally substituted alkoxy, a hydroxyl, a carboxyl, a halo, a nitro, or a cyano, R5 is hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an amino, a hydroxyl, a carboxyl, a halo, a nitro, or a cyano, and R6 and R7 are independently a hydrogen or an optionally substituted alkyl group having 1 to 4 carbon atoms. A method of detecting copper cations and/or chromate anions in a fluid sample with zirconium metal-organic framework.

Abstract: 12(S)-hydroxyeicosatrienoic acid (12(S)-HETrE) compounds and compositions comprising the same are disclosed. Methods of using the compounds in the prevention and treatment of thrombosis and thrombotic disorders are also disclosed.

Abstract: The compound 2-(4-tert-Butylphenyl)-1H-benzo[d]imidazol-5-ol: and its use are disclosed. The compound activates Ppargc1a and, as a consequence, is useful for treating neuroinflammation and for treating a variety of neurodegenerative diseases.

Abstract: The present invention provides novel derivative of ?-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

Abstract: Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of USP7 activity.

Abstract: The disclosed subject matter provides methods of using nitroxyl donating compounds and pharmaceutical compositions comprising such compounds in a dose escalation regimen.

Abstract: The invention provides modulators of indoleamine 2,3-dioxygenase (IDO1) and their use in the prophylaxis and/or treatment of IDO1-mediated diseases. Specifically, the present invention provides compounds according to Formula (I) an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof.

Abstract: Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple.

Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, Rx, X1, n, n1, and q are as defined herein, and methods of making and using same.

Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

Abstract: Provided herein are compounds of Formulae (RL), (I), (II), (III), (IV), and (V), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, prodrugs, and isotopically labeled derivatives thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of metabolic disorders (e.g., diabetes, hyperglycemia, impaired glucose tolerance, insulin resistance, obesity). The compound are useful as substrate selective inhibitors of insulin-degrading enzyme (IDE).

Abstract: Disclosed herein are inhibitors of the GGDPS enzyme, and methods for their use in treating or preventing diseases, such as multiple myeloma. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are described.

Abstract: Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

Abstract: Provided herein are pharmaceutical compositions comprising deuterated derivatives of psilocybin. The provided compositions may be useful for treating and/or preventing various diseases and conditions, such as mood or psychiatric disorders.

Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

Abstract: The present technology provides compounds according to Formula I or Formula III as well as compositions including such compounds useful for the treatment of metastatic cancer and/or glaucoma.

Abstract: It is an object of the present invention to provide a novel and advantageous process for commercially preparing of 2-cyanoimidazole compounds. More particularly, it relates to an efficient method of preparation of cyazofamid synthetic precursor by simultaneous conversion of aldoxime group to the corresponding cyano-derivative and reducing of N-oxygenated-imidazole ring to imidazole under mild conditions using reducing agent selected from the group consisting of metal salts of sulfur-containing derivatives in the presence of a polar organic solvent.