Abstract: This disclosure relates to certain compounds that are effective in the treatment of a Rac-GTPase mediated disorder (e.g., acute lymphoblastic or chronic myelogenous leukemia), as well as methods for the manufacture of and the use of these compounds (e.g., for treating a Rac-GTPase mediated disorder).

Abstract: The subject matter disclosed herein is directed to novel She inhibitors of Formula (II). These compounds are useful for treating impaired insulin sensitivity, glucose tolerance, obesity, diabetes, metabolic syndrome, NAFLD, NASH, PSC, PBC, or other metabolic syndrome component conditions.

Abstract: A crystal form of a pyrazin-2(1H)-one compound and a preparation method therefor. The present invention specifically related to a compound of formula (II) and a preparation method for a crystal form of the compound.

Abstract: This disclosure is in the field of medicinal chemistry, and relates to a new class of small-molecules having the Formula I, or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof, wherein the variables Ring A, X, R1a, R1b, R2, R3, R4, m, n, and p are described herein, which function as dual inhibitors of EGFR proteins and PI3K proteins. The disclosure further relates to the use of the compounds described herein as therapeutics for the treatment of diseases and conditions mediated by EGFR proteins and/or PI3K proteins, such as cancer and other diseases.

Abstract: Disclosed herein are compounds of Formula I?. Compounds of Formula I? inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

Abstract: The invention provides compounds that inhibit human MLKL, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.

Abstract: The present disclosure provides a crystal form of a compound and fumaric acid, an active pharmaceutical ingredient and a pharmaceutical composition containing the same, and a method for treating coronavirus-induced diseases a using the same. In particular, the crystal form of the present disclosure comprises the compound of Formula (I) and fumaric acid, and the X-ray powder diffraction pattern of the crystal form obtained using Cu-K? radiation includes at least three peaks selected from the group consisting of: 0.94°±0.2° 2?, 19.06°±0.2° 2?, 23.50°±0.2° 2?, and 24.66°±0.2° 2?. The crystal form of the present disclosure has a high purity, good stability, and a high melting point.

Abstract: Disclosed herein are novel compounds for degrading Tau protein aggregates, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof. Also disclosed herein are uses of the compounds, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof in manufacture a medicament for treating a tauopathy, as well as method for aiding in the treatment of a tauopathy or treating a tauopathy in a subject.

Abstract: The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.

Abstract: A compound represented by the following general formula (I) [the symbol in the formula are as defined in the description], a salt thereof, or the like is a RET inhibitor or RET tyrosine kinase inhibitor that can he used as an agent for the prevention or treatment of disorders including cancers and cancer metastasis having mutations in RET.

Abstract: A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester.

Abstract: An oral gel composition suitable for the treatment of oral leukoplakia comprising a combination of diclofenac with hyaluronic acid and methods of administering the oral gel that may include a device that prolongs contact time of the oral gel with the areas of the mucosa that are affected by oral leukoplakia.

Abstract: The present disclosure provides a therapeutic drug that is useful for the treatment of motor fluctuations (e.g., wearing-off) in Parkinson's disease. In particular, the present disclosure provides a composition and method for treating, improving, suppressing the progression, or preventing motor complications in Parkinson's disease, especially motor fluctuation, comprising tandospirone or a pharmaceutically acceptable salt thereof, wherein the tandospirone or a pharmaceutically acceptable salt thereof is parenterally administered.

Abstract: The present invention relates to: novel selenopsammaplin A and a derivative thereof, which have anticancer activity; a preparation method therefor; and a pharmaceutical composition containing the same as active ingredients and, more specifically, to: a novel compound selenopsammaplin A and a derivative thereof which exhibit more excellent anticancer activity since a disulfide moiety thereof is substituted with diselenide according to research on the structural activity of psammaplin A, which is known to have an effect of inhibiting the growth of cancer cells; a preparation method therefor; and a composition for preventing or treating cancer, containing the same as active ingredients. According to the present invention, the novel selenopsammaplin A and the derivative thereof exhibit excellent anticancer activity on various human cancer cell lines so as to be expected to be effectively usable in a pharmaceutical composition for cancer prevention and treatment.

Abstract: A first aspect of the invention relates to novel compounds and more precisely to novel bifunctional prodrugs and drugs. An additional aspect of the invention relates to antibody compound conjugates, wherein the compound is a claimed compound, and to pharmaceutical compositions containing the compound or antibody compound conjugate. The invention lastly relates to the use of this compound or antibody compound conjugates according to the invention in order to treat tumour diseases, particularly in mammals.

Abstract: A method for treating cancer is disclosed. The method comprises administering to a subject in need thereof, an effective amount of a pharmaceutical composition comprising monoethanolamine, its prodrug or hybrid molecule or a pharmaceutically acceptable salt thereof, and a pharmaceutically effective carrier. Also disclosed is a composition comprising monoethanolamine or a pharmaceutically acceptable salt thereof and a pharmaceutically effective carrier, wherein the pharmaceutical composition is formulated for oral, intravenous, intraperitoneal, subcutaneous, dermal, or intranasal administration.

Abstract: The present invention disclosed a crystal form of pyrazine-2(1H)-ketone compound and a preparation method therefor. Specifically disclosed is a method for preparing a compound of formula (II) and a crystal form thereof.

Abstract: A method of lowering cholesterol and/or PCSK9 levels in a subject in need thereof includes administering to the subject an ADH inhibitor, AKR inhibitor, and/or SNO-CoAR inhibitor at an amount(s) effective to reduce serum cholesterol and/or PCSK9 levels.

Abstract: Antifibrinolytic agents/drugs are applied to the concussive area of a patient's brain to counter the activation of a fibrinolytic process in the concussive area. Various techniques are described for administering the antifibrinolytic agent.