Abstract: Disclosed is a BCL-2 protein apoptosis inducer, and further disclosed are the uses of the compound and a pharmaceutical composition comprising the compound in the preparation of a drug for treating diseases related to anti-apoptotic protein BCL-2. The compound has potent BCL-2/BAK blocking activity, and can be used for treating diseases such as infectious diseases, immune diseases, inflammatory diseases or cell proliferation abnormalities that benefit from the inhibition of anti-apoptotic protein BCL-2.

Abstract: Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof; or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

Abstract: Disclosed in the present invention is a compound having a structure shown in general formula I, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvate thereof. Further disclosed in the present invention are a composition comprising the compound, a preparation and an application. The compound of the present invention has a significant activation effect on KCNQ2/3 potassium ions, and can be used for treating diseases related to potassium channel ion flow, especially for treating central nervous system diseases.

Abstract: The present disclosure discloses a crystal form of a casein kinase 1? inhibitor and a preparation method and use of the crystal form. Specifically, the present disclosure relates to a crystal form of the compound (S)-2-(1-(4-amino-3-(2,3-difluoro-4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-3-phenylquinazoline-4(3H)one methanesulfonate and a preparation method and use of the crystal form. The crystal form of the casein kinase 1? inhibitor compound of the present disclosure has good water solubility and oral absorption, and can be better used for the treatment of malignant tumors and autoimmune diseases that benefit from the inhibition of casein kinase 1? activity.

Abstract: Disclosed is a novel substituted pyrazolopyrimidine compound that inhibits the activity of casein kinase 1? (CK1?) and a stereoisomer or stereoisomer mixture thereof, or a pharmaceutically acceptable salt or solvate thereof, and an application thereof in preparation of drugs for treating diseases, disorders or conditions that benefit from the inhibition of the activity of the casein kinase 1? (CK1?). The compound of the present invention has an inhibitory activity on CK1? kinase, OCI-LY10 cells and Karpas299 cells, shows good anti-tumor activity in an OCI-LY10 subcutaneous xenogeneic model and shows excellent synergistic anti-tumor activity in combination with BTK inhibitors. The compound of the present invention has good pharmacokinetics properties and may be used alone or in combination with other drugs to treat diseases, disorders or conditions that benefit from the inhibition of the activity of the casein kinase 1?, the diseases, disorders or conditions comprising tumors, autoimmune diseases, etc.

Abstract: The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug. The compound of the present invention has a structure of Formula II or Formula II?: or their optical isomers, or pharmaceutically acceptable salts or solvates; where each Rg is independently H, halogen, —CF2H, —CF3, —CN, C1-C3 alkyl, or C1-C3 alkoxy; n is selected from 0, 1 and 2; Rd is selected from Re is selected from H, CH3, C2-C6 alkyl, C1-C6 azaalkyl, and C1-C6 oxaalkyl, wherein CH3, C2-C6 alkyl, C1-C6 azaalkyl and C1-C6 oxaalkyl are further substituted with amino, hydroxyl, and C1-C3 alkyl; Y1, Y2, Y3 and Y4 are independently selected from C(Rf) and N, and at least one of Y1, Y2, Y3 and Y4 is N, wherein Rf is selected from H, halogen, C1-C3 alkyl, —CF3, and —CF2H.

Abstract: The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug for treating diseases, disorders or conditions benez,fiting from the inhibition of Bruton's tyrosine kinase activity. The compound of the present invention has anti-proliferation and inhibitory effects on tumor cell strains such as A549, MINO, OCI-LY10 and TMD-8, and shows an excellent anti-tumor activity in tumor models such as Mino subcutaneous xenografts, and can be applied in drugs for treating solid tumors or leukemia associated with cell proliferation in humans or animals. The compound of the present invention has good pharmacokinetic properties, and can be applied to the oral treatment of solid tumors or leukemia associated with the cell proliferation in humans or animals or autoimmune diseases. The compound of the present invention has the property of a low hERG channel blockade.