Abstract: A compound represented by formula (I) or an optical isomer, a pharmaceutically acceptable salt, a hydrate or a solvate thereof are provided. In formula (I), R1-R17 are each independently selected from hydrogen and deuterium, R18 and R19 are hydrogen, and R1-R19 are not simultaneously hydrogen. The deuterated compound and the salt, hydrate or solvate thereof have excellent metabolic stability and pharmacokinetic properties, and can be used in the manufacture of tubulin inhibitors, anti-cancer drugs, antiviral drugs, and drugs for the treatment of novel coronavirus pneumonia.

Abstract: A combination drug for treating triple-negative breast cancer. Androgen receptor-targeting degraders (including PROTACs) can effectively prevent and/or treat triple negative breast cancer (including androgen receptor-positive triple negative breast cancer). The combined use of an androgen receptor degrader and a targeting drug (including PI3K? inhibitors and PARP inhibitors), immunotherapy drug or chemotherapy drug can effectively prevent and/or treat triple negative breast cancer.

Abstract: Provided is a drug for treating triple negative breast cancer. Provided is use of an androgen receptor (AR) degrader (including PROTAC) in the preparation of a drug for preventing and/or treating triple negative breast cancer (including androgen receptor positive triple negative breast cancer). Provided is use of an AR degrader in combination with a targeting drug (comprising a PI3K? inhibitor and a PARP inhibitor), an immunotherapy drug or a chemotherapeutic drug in the preparation of a drug for preventing and/or treating triple negative breast cancer.

Abstract: A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines.

Abstract: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.

Abstract: A high-precision multi-pole magnetoelectric encoder includes a mounting seat, a rotating shaft, a single-pole magnet ring, a single-pole signal processing board, a shielding shell, an n-pole magnet ring, an n-pole signal processing board, a housing, a conductive rubber pad, an aviation plug, bearings, copper columns, Hall components, and assembly screws. The magnetoelectric encoder improves the environmental adaptability and replaceability of the high-precision multi-pole magnetoelectric encoder by redesigning the structure of the multi-pole encoder. It eliminates errors caused by changes in the position of magnets and Hall sensors during the replacement process, reduces interference caused by the multi-pole magnet encircling the single-pole magnet, enhances resistance to electromagnetic interference, thereby increasing the detection accuracy of the magnetoelectric encoder, and improves the performance and competitiveness of the product.

Abstract: The compound of formula (I) has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound of formula (I) can not only be used independently to prepare an antineoplastic agent but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.

Abstract: A synthesis and an application of a phosphatase degrader are provided. The phosphatase degrader is a compound represented by formula I, or a salt thereof, or a deuterated compound thereof, or a stereoisomer thereof, or a solvate thereof, or a hydrate thereof, or a prodrug thereof. The compound can be used as a phosphatase degrader, especially as an SHP2 protein degrader, can treat malignant diseases such as tumors, and has good application prospects.

Abstract: A pharmaceutical composition for the treatment of cancer and a use thereof are provided. The pharmaceutical composition consists of an FAK inhibitor and a CD44 inhibitor. Also provided is a drug combination of an FAK inhibitor and a CD44 inhibitor for the treatment of cancer. The CD44 inhibitor and FAK inhibitor drug combination can have synergistic effects, significantly improving tumor inhibition effects, reducing toxic side effects, and overcoming tumor drug resistance.

Abstract: This patent document provides a sustained-release formulation comprising 1-40 parts of a quinoline compound, 100-300 parts of a filler, 50-200 parts of a sustained-release material and optionally 0.5-4 parts of a lubricant. Also provided are methods of treating diseases with the sustained-release formulation.

Abstract: The present disclosure provides techniques for implementing a hierarchical and partitional integer motion estimation search (IMES) architecture using a search engine that is configurable based on a content of a plurality of frames in a video sequence. For example, the techniques include identifying, based on the plurality of frames, one or more search parameters for the hierarchical and partitional motion estimation, where the one or more search parameters are based on a content indicative of motion features tracked across the video sequence. The hierarchical and partitional motion estimation, which includes at least one decimated motion estimation search followed by a full-pixel level search, is performed based on the one or more identified search parameters to determine an integer (or pixel-level) motion vector.

Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.

Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I), R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.

Abstract: A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R4—NH—R5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.

Abstract: Bifunctional chimeric heterocyclic compounds of formula (I) is effective for targeted degradation of androgen receptors and use thereof. The compound of formula (I) also has an isotopic compound, an optical isomer, a tautomer, pharmacologically acceptable salt, a prodrug thereof, or a solvate. In formula (I), ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.

Abstract: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.

Abstract: Disclosed is a BRD4 inhibitor as shown in formula I, belonging to the field of compound drugs. The compound provided has a good inhibitory effect on prostate cancer cell proliferation, and can be used for preparing a drug combatting tumors, autoimmune or inflammatory diseases and viral infection, and in particular an anti-prostate cancer drug.

Abstract: An EP300/CBP inhibitor, specifically provided is a compound as shown in formula I, or a deuterated product thereof, or a salt thereof, or a conformational isomer thereof, or a crystal form thereof, or a solvate thereof. The compound is highly selective for EP300/CBP, and can effectively inhibit the activity of EP300/CBP; in addition, the compound has an excellent inhibitory effect on various tumor cells including prostate cancer cells, leukemia cells, breast cancer cells and multiple myeloma cells. The compound has broad application prospects in the preparation of an EP300/CBP inhibitor, and drugs for preventing and/or treating tumors, myeloid hematopoietic stem/progenitor cells malignant disease, and regulating regulatory T cells.

Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.

Abstract: Provided is a compound represented by formula (I). Also provided are a pharmaceutical composition containing the compound of formula (I) and use of the compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for preparing drugs for preventing and/or treating diseases having pathological features of IDO-mediated tryptophan metabolic pathways.