Abstract: A di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation and the use thereof. Specifically, disclosed are a di(hetero)aryl macrocyclic compound represented by formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug or an active metabolite thereof, a pharmaceutical composition comprising said compound and the derivative thereof, and methods of using the same, including methods of treating cancers, pain, neurological diseases, autoimmune diseases and inflammation.

Abstract: Provided are a pharmaceutical composition of a substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound and the use thereof. The pyrazolo[1,5-a]pyrimidine macrocyclic compound is a compound as shown in formula (Aa), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvate, a crystal form, a stereoisomer or an isotopic variant thereof. The compound of the present invention is an inhibitor of the Trk kinase, and can be used for treating pain, cancers, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract: Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition including the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase, for preparing a plurality of drugs including an anti-tumour drug.

Abstract: A system for providing a persona-driven and artificially-intelligent avatar is disclosed. The avatar may be utilized to represent an artificially-intelligent virtual assistant that may perform actions on behalf of a user, such as actions related to an investment strategy for the user. Notably, the avatar may influence artificial intelligence algorithms supporting the functionality of the virtual assistant via quantifiable traits of a persona of the avatar. In particular, the quantifiable traits of the persona of the avatar may be utilized to range bound the controlling parameters of the algorithms such that the virtual assistant represented by the avatar performs actions that conform to the ranged-bounded controlling parameters. Metrics corresponding to the performance of the virtual assistant may be tracked, and the system may modify parameters of the virtual assistant based on the metrics so as to adjust future actions performed by the virtual assistant for the user.

Abstract: Provided are a substituted fused aromatic ring derivative, a composition containing the compound, and a use thereof. The substituted fused aromatic ring derivative is a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound and the composition can be used to treat various protein tyrosine kinase-mediated diseases or disorders.

Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention relates to an indazole compound for use in inhibiting kinase activity, and relates to a preparation and use thereof. Specifically disclosed in the present invention is an indazole compound represented by formula (I), or a crystal form, a prodrug, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a solvate or a hydrate thereof, or a pharmaceutical composition thereof. The compound of the present invention and the composition containing the compound have an excellent inhibitory effect on kinase proteins, and have better pharmacokinetic parameter characteristics, may increase the drug concentration of the compound in an animal, and improve the efficacy and safety of the drug.

Abstract: Provided are an aminopyrimidine compound as shown in formula (I), a polymorph, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotopic variant, a hydrate or a solvate thereof, and a pharmaceutical composition containing the same and the use thereof. The aminopyrimidine compound and the composition containing the same have excellent inhibition to protein kinases, and at the same time have better pharmacokinetic parameter characteristics, and can improve the drug concentration of the compound in animals, and thereby improve the efficacy and safety of the drug.

Abstract: The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: (I) where A, L, R1, R2, R3, and n are described herein.

Abstract: Disclosed are a dianilino pyrimidine compound having an inhibitory effect on protein tyrosine kinase, pharmaceutically acceptable salts, crystal forms, prodrugs, metabolites, hydrates, solvates, stereoisomers or isotopic derivatives thereof, a pharmaceutical composition containing these compounds, as well as preparation and use of these compounds. The compound has a structure as represented by formula (I), and may be used for treating ALK-mediated cancer-related symptoms, such as non-small cell lung cancer, breast cancer, nerve tumors, esophagus cancer, soft tissue cancer, lymphoma, or leukemia.

Abstract: The present invention relates to an aminopyrimidine compound having an inhibitory effect on the activity of protein kinase as well as the preparation and use thereof. Specifically, disclosed by the present invention is an aminopyrimidine compound represented by formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate or hydrate thereof, as well as a pharmaceutical composition comprising said compound and a use method therefor. The method comprises a method for treating cell proliferative diseases and conditions such as cancer and immune diseases.

Abstract: A breast diffusion optical tomography (DOT) device includes a light source, a detector, a mechanical driver and a contour acquisitor without using optical fiber and reduce the system complexity. The light source includes M1 number of multi-wavelength near-infrared light emitters for a continuous-wave mode and M2 number of laser diodes of different wavelengths for a frequency-domain mode. The detector includes N1 number of silicon photomultipliers for detecting near-infrared light in the continuous-wave mode and N2 number of silicon photomultipliers for detecting near-infrared light in the frequency-domain mode. The mechanical driver adjusts a distance between the light source and the detector. The contour acquisitor obtains the geometry of a patient's breast for reconstruction. The DOT device uses amplitude and phase information obtained in the frequency-domain mode to estimate initial optical parameters of tissues and then apply for reconstruction in the continuous-wave mode.

Abstract: A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation and use thereof are disclosed. In particular, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a polymorph, a prodrug or an isotopic variation thereof, as well as a pharmaceutical composition including the same are disclosed. As a selective irreversible inhibitor of Bruton's tyrosine kinase, the described compound can be used for preventing or treating diseases such as inflammation, autoimmune diseases (such as rheumatoid arthritis), xenogeneic immune diseases and cancers.

Abstract: The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: wherein A, L, R1, R2, R3, and n are described herein.

Abstract: Provided are a compound as represented by formula (D) and a preparation method therefor, where X2 is a halogen, Pg is selected from H and an amino protecting group, such as Cbz, Boc, Fmoc, Alloc, Teoc, methoxycarbonyl or ethoxycarbonyl. Also provided are a synthesized intermediate compound of the formula (D) compound and a preparation method for the intermediate compound.

Abstract: The present disclosure provides a substituted pyrazolo[1,5-a]pyridine compound, a composition including the same, and a use thereof. The substituted pyrazolo[1,5-a]pyridine compounds is a compound represented by formula (I) or the tautomers, stereoisomers, prodrugs, crystal forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compound of the present disclosure and composition thereof are useful for treating RET kinase-mediated diseases or conditions and have more excellent pharmacokinetic properties.

Abstract: A dihydroimidazopyrazinone compound, a composition including the same, and a use thereof. The dihydroimidazopyrazinone compound is a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate, or solvate thereof. The compound and the composition thereof can be used to treat a proliferative disease regulated by RAS/RAF/MEK/ERK kinase and have excellent pharmacokinetic properties.

Abstract: A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation, compositions, and uses thereof are disclosed. In particular, compounds of formula (I) and (II), or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a polymorph, a prodrug or an isotopic variation thereof, as well as a pharmaceutical composition including the same are disclosed. Compounds disclosed herein are substituted pyrrolo[3,2-d]pyrimidines and are selective irreversible inhibitors of Bruton's tyrosine kinase. The described compounds can therefore be used for preventing or treating diseases such as inflammation, autoimmune diseases (such as rheumatoid arthritis), xenogeneic immune diseases and cancers.

Abstract: Provided are a substituted oxadiazole chemical compound and composition containing said chemical compound and use thereof; said substituted oxadiazole chemical compound is the oxadiazole chemical compound as represented by formula (I), or its crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvent compound. The disclosed substituted oxadiazole chemical compound and composition containing said chemical compound are capable of inhibiting indoleamine 2,3-dioxygenase; it also has better pharmacokinetic parameter attributes and is capable of improving the drug concentration of the chemical compound in an animal body, thus improving the therapeutic efficacy and safety of the drug.