Abstract: Disclosed in the present invention are a crystal form of monomethanesulfonate of a deuterated 3-(4,5-substituted aminopyrimidine)phenyl compound as represented by formula I, and a preparation method therefor. The crystal form is highly stable, can be used for treatment or prevention of diseases or conditions by means of epidermal growth factor receptors (EGFRs) in some mutation forms, can effectively inhibit the growth of a variety of tumor cells, and have an inhibiting effect on other proteases of EGFR and Her families, and thus can be used for preparing antitumor drugs.

Abstract: The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the invention.

Abstract: Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD).

Abstract: The present application provides detectable compounds useful for identifying compounds that bind (e.g., inhibit) MmpL3. Methods of identifying compounds that bind and/or inhibit MmpL3 are also provided.

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Abstract: In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.

Abstract: A composition may include a compound, a film may include the composition, an organic layer of an organic sensor and/or photoelectric diode may include the compound, and the film, organic sensor, and/or photoelectric diode may be included in an electronic device.

Abstract: The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: An organic EL device is provided, including at least an anode, a hole transport layer, a light-emitting layer, an electron transport layer, and a cathode in this order, wherein the hole transport layer contains an arylamine compound represented by the following formula (1), wherein Ar1 to Ar8 and n1 are defined in the specification, and the electron transport layer contains a compound having a benzoazole ring structure represented by the following formula (2), wherein Ar9, Ar10, X, Y1, Z1 and Z2 are defined in the specification.

Abstract: Provided are a novel compound having CDK8 and/or CDK19 inhibitory activity, and a production method for Tregs. The treatment of T cells with a CDK8 and/or CDK19 inhibitor induces Foxp3 in the T cells. Foxp3+ T cells can be induced by treating Foxp3? T cells with the CDK8 and/or CDK19 inhibitor in vitro. Thus, Tregs can be induced.

Abstract: The present invention relates to a pharmaceutical combination comprising: (a) a PPAR agonist; (b) a p38 kinase inhibitor; and optionally (c) one or more pharmaceutically acceptable diluents, excipients or carriers for use in a method of preventing or treating ophthalmic diseases or disorders in a subject.

Abstract: The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents.

Abstract: Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.

Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: The present disclosure provides an organic compound represented by general formula [1] below. In formula [1], Ar1 and Ar2 each represent an alkyl group having 1 to 8 carbon atoms, an aromatic hydrocarbon group having 6 to 18 carbon atoms, or a heteroaromatic group having 3 to 17 carbon atoms. Ar1 and Ar2 may be the same or different. Ar3 and Ar4 are each a substituent having a carbazolyl group. Ar3 and Ar4 may be the same or different. Ar1 to Ar4 may be substituted. At least one of Ar1 to Ar4 has a tert-butyl group. The total number of tert-butyl groups in one molecule of the organic compound is 2 or more.

Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

Abstract: Provided are a tricyclic compound as shown in formula (I) as a CRTH2 inhibitor, or a pharmaceutically acceptable salt, a tautomer, a stereoisomer or a solvate thereof, and the use thereof in treating diseases related to CRTH2 receptors.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(1,1?-biphe-1H-benzo[d]imidazole derivatives. The invention further provides compositions comprising the compounds and the compounds for use in methods of medical treatment.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: Provided herein piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction. Also provided methods of treatment of diseases associated with said processes, e.g. Alzheimer's and Parkinson's diseases.