Abstract: A bi-functional, proteolysis-targeting chimera (PROTAC) agent is provided for the modulation of transcriptional factor FOXP3 and associated regulatory T cells. The agent contains an inhibitory peptide of FOXP3 covalently bound through a linker to a ubiquitin ligase binding moiety. The agent binds FOXP3 and recruits an E3 ubiquitin ligase, and thereby bringing FOXP3 in proximity to the E3 ubiquitin ligase for ubiquitination and degradation of the FOXP3. Methods of preparation and use of the agent are also provided.

Abstract: The present disclosure discloses a gradient single-crystal positive electrode material, which has a chemical formula of LiNixCoyA1-x-yO2@mLiaZbOc, wherein 0<x<1, 0<y<1, 0<x+y<1, 0<m<0.05, 0.3<a?10, 1?b<4, and 1?c<15, A is at least one of Mn, Zr, Sr, Ba, W, Ti, Al, Mg, Y, and Nb, and Z is at least one of B, Al, Co, W, Ti, Zr, and Si. The atomic ratio of the content of Co on the surface of the single-crystal positive electrode material particle to the content of Ni+Co+A on the surface is greater than 0.4 and less than 0.8, and the atomic ratio of Co at a depth 10% of the radius from the surface of the single crystal positive electrode material particle is not less than 0.3; and the single-crystal positive electrode material particle has a roundness of greater than 0.4, and is free from sharp corners.

Abstract: Provided are K-Ras mutant protein inhibitors of formula (I), a composition containing the same and the use thereof.

Abstract: A Compound of formula (I) or (II), a stereoisomer thereof, an atropisomer, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer, a pharmaceutically acceptable salt of the atropisomer, a prodrug thereof, a deuterated molecule thereof or a conjugated form thereof is disclosed:

Abstract: Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

Abstract: Provided are compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are pharmaceutical compositions comprising the compounds, methods of preparing the compounds and the use in the manufacture of medicaments for preventing or treating a disease or condition related to p53 mutants.

Abstract: Provided herein are salts of the compound 1 and new poly morph forms thereof, pharmaceutical composition including the compound 1 and new polymorph forms thereof, and methods of preparing them and using them.

Abstract: Provided herein is a compound of Formula (IB), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a prodrug thereof, a deuterated molecule thereof or a conjugated form thereof; composition containing the same and the use thereof.

Abstract: Provided are a compound of formula (I) that inhibit the activity of PARP7, a stereoisomer thereof, a deuterated derivative thereof, or a pharmaceutically acceptable salt thereof, an intermediate to prepare the compound, a process to prepare the compound, a composition comprising the same, and the methods of using the same.

Abstract: Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

Abstract: Compounds of general Formula S-1, S-2, S-3 and their pharmaceutically acceptable salts, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are synthesis, compositions, and uses of such compounds.

Abstract: Compounds of general Formula I, II, III, IV, V and their pharmaceutically acceptable salts, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are synthesis, compositions, and uses of such compounds.

Abstract: The present disclosure discloses a gradient single-crystal positive electrode material, which has a chemical formula of LiNixCoyA1-x-yO2@mLiaZbOc, wherein 0<x<1, 0<y<1, 0<x+y<1, 0<m<0.05, 0.3<a?10, 1?b<4, and 1?c<15, A is at least one of Mn, Zr, Sr, Ba, W, Ti, Al, Mg, Y, and Nb, and Z is at least one of B, Al, Co, W, Ti, Zr, and Si. The atomic ratio of the content of Co on the surface of the single-crystal positive electrode material particle to the content of Ni+Co+A on the surface is greater than 0.4 and less than 0.8, and the atomic ratio of Co at a depth 10% of the radius from the surface of the single crystal positive electrode material particle is not less than 0.3; and the single-crystal positive electrode material particle has a roundness of greater than 0.4, and is free from sharp corners.

Abstract: Tetrahydropyrido[3,4-d]pyrimidines compounds are provided that are potent HPK1 inhibitors. The compounds are useful to treat or prevent cancer and/or inflammatory and/or autoimmune diseases or symptoms thereof in mammals, particularly humans. The compounds have a chemical structure of the general Formula (I), (II), (III), (IV) or (V) or enantiomers or diastereomers or mixtures thereof or pharmaceutically acceptable salts thereof.

Abstract: An event processing method provided by an embodiment of the present disclosure determines M events, where each event is associated with a priority and a minimum working time, M is an integer greater than 1, and the minimum working time of each event is less than duration of a time slice; processes a first event within a first time slice, where the first event is an event having a highest priority among the M events; and in the case that processing duration of the first event reaches the minimum working time of the first event, determines to continue to process the first event within the first time slice, or determines to interrupt processing of the first event and processes a second event within the first time slice.

Abstract: The invention relates to novel glutamine analogs, a composition containing the glutamine analogs and the use thereof.

Abstract: The present invention provides recombinant bispecific antibodies designed to bind to a surface antigen on target cells and to an activating component on immune cells such as T cells. The bispecific antibodies comprise two polypeptide chains that contain Fv and Fab as antigen¬ binding fragments and a modified Fc region to facilitate heterodimer formation. In one embodiment, the bispecific antibodies further comprise protease cleavage sites and/or motifs that would cause steric occlusion of the antigen binding sites so that the antibodies would be activated only in a specific environment, e.g. in the vicinity of a tumor. In another embodiment, the bispecific antibodies comprise modified sequences that confer reduced binding affinity to CDS and/or cross-reactive binding to CDS on cells from different species.