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.

Abstract: Provided is an alkynyl(hetero)aromatic compound having an inhibitory effect to protein tyrosine kinase, a pharmaceutical composition comprising same, preparation and usage thereof. Specifically, disclosed is an alkynyl(hetero)aromatic compound as shown in formula (I), wherein rings A, R1, R2, R3, R4, R5, L, and B are defined in the description, a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotopic variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases, such as anti-tumor.

Abstract: The present invention provides a diarylpyrazole compound, a composition comprising same, and a use thereof. The diarylpyrazole compound refers to the compound represented by a formula (I) or a tautomer, a stereoisomer, a prodrug, a crystalline form, a pharmaceutically acceptable salt thereof, a hydrate, or a solvent compound. The compound and the composition of the present invention can be used for treating BRAF kinase mutant proliferative diseases and have better pharmacokinetic properties.

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: An amino pyrimidine compound for inhibiting protein tyrosine kinase activity, a pharmaceutical composition thereof, preparation therefor, and an application thereof. Specifically, an amino pyrimidine compound represented by formula (I), R1, R2, L, Y, R6, W, A, m, and n being defined in the specification, and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound, a hydrate, a polymorphism, a prodrug, or an isotope variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases such as cell proliferative diseases, cancers, and immune diseases.

Abstract: Disclosed are alkynyl (hetero) aromatic ring compounds that inhibit protein tyrosine kinases, pharmaceutical compositions comprising same, preparations therefor and uses thereof. Specifically, disclosed are an alkynyl (hetero) aromatic ring compound represented by formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotope variant thereof. The disclosed compounds may be used in the treatment and/or prevention of diseases associated with protein tyrosine kinase, such as in preventing tumors.

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: 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.

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 di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation therefor 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 for using same, including methods for treating cancers, pain, neurological diseases, autoimmune diseases and inflammation.