Abstract: A compound of formula (I) and its antitumor application are disclosed. The compounds of formula (I) have degradation and inhibitory effects on ALK target proteins. They are mainly composed of four parts: the first part, ALK-TKI, being compounds with ALK tyrosine kinase inhibitory activity; the second part, LIN, being different kinds of linker (Linker); the third part, the ULM, being a small molecule ligand (ULM, ubiquitin ligase binding moiety) with ubiquitination of VHL, CRBN or other proteases; and the fourth part, the group A, being a carbonyl group or absent, which covalently bond ALK-TKI to LIN, wherein LIN and ULM are covalently bonded. A series of compounds designed and synthesized by the present disclosure have wide pharmacological activities, have functions of degrading ALK protein and inhibiting ALK activity, and can be used for related tumor treatment.

Abstract: The present disclosure provides compounds of formula (I) or salts, enantiomers, stereoisomers, solvates, or polymorphs thereof, and applications thereof, and pharmaceutical compositions comprising, as an active ingredient, the compound of Formula (I) or a salt, enantiomer, stereoisomer, solvate, or polymorph thereof, and applications of the pharmaceutical compositions. The compounds can effectively prevent and/or treat diseases or disorders associated with TNF-?.

Abstract: The present disclosure relates to compounds of Formula (I) or salts, enantiomers, stereoisomers, solvates, or polymorphs thereof, and uses thereof. The present disclosure also relates to pharmaceutical compositions comprising, as an active ingredient, the compound of Formula (I) or a salt, enantiomer, stereoisomer, solvate, or polymorph thereof, and use thereof. A series of compounds designed and synthesized by the present disclosure can effectively prevent and/or treat diseases or disorders associated with TNF-a.

Abstract: The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.

Abstract: The present disclosure relates to glutarimide skeleton-based compounds of Formula (I) or a salt, an enantiomer, a stereoisomer, a solvate, or a polymorph thereof, and uses thereof. The present disclosure further relates to a pharmaceutical composition comprising, as an active ingredient, the glutarimide skeleton-based compounds of Formula (I), or a salt, an enantiomer, a stereoisomer, a solvate, or a polymorph thereof, and uses thereof. The series of compounds designed and synthesized in the present disclosure can effectively prevent and/or treat a tumor.

Abstract: A bifunctional compound, or a pharmaceutically acceptable salt, an isomer, a prodrug, a polymorphic substance or a solvate thereof. The chemical structural formula of the bifunctional compound is represented as formula I, and the bifunctional compound can be used for preventing or treating cancers.

Abstract: A compound of general formula (I), a compound of general formula (III) and anti-tumor applications thereof. A series of compounds designed and synthesized have a wide range of pharmacological activities, have the function of degrading specific proteins and/or inhibiting activity, and can be used in related tumor and cancer treatments.

Abstract: The present disclosure relates to a compound of Formula (I) or a salt, a solvate, an isotopically enriched analog, a tautomer, a polymorph, a stereoisomer thereof, or a mixture of stereoisomers thereof, and their use for treating a tumor. The present disclosure also relates to a compound of Formula (I?) or a pharmaceutically acceptable salt, a solvate, an isotopically enriched analog, a tautomer, a polymorph, a stereoisomer thereof, or a mixture of stereoisomers thereof, and their use for treating a tumor.

Abstract: The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), intermediates of formula (IV), and uses of the intermediates. The compound of formula (I) has a degrading effect on a specific target protein, which is mainly composed of three parts. The first part is a small molecule compound (SMBP, Small Molecules Binding Protein) that can bind to a protein, the second part LIN is a linker, and the three-part ULM is a ubiquitin ligand (ULM, Ubiquitin Ligase Binding Moiety), wherein SMBP is covalently bound to LIN, and LIN is covalently bound to ULM. A series of compounds designed and synthesized in the present disclosure have a wide range of pharmacological activities, including the functions of degrading specific proteins and/or inhibiting activities of specific proteins, and thus can be used in related tumor treatments.

Abstract: The present disclosure relates to an ER protein regulator compound represented by formula (I) and use thereof. LIN in the compound represented by formula (I) is a linker; ULM is a small-molecule ligand of VHL or CRBN protease having a ubiquitylation function; and group X is CH2, O or NH, and group X is covalently linked to ULM by means of the linker LIN. The designed and synthesized compounds of the present disclosure have wide pharmacological activity, has the function of regulating ER protein and inhibiting the activity of tumors, and can be used for preventing and/or treating diseases and disorders associated with estrogen receptors, or related tumor treatment.

Abstract: The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.

Abstract: A compound of formula (I) and its antitumor application are disclosed. The compounds of formula (I) have degradation and inhibitory effects on ALK target proteins. They are mainly composed of four parts: the first part, ALK-TKI, being compounds with ALK tyrosine kinase inhibitory activity; the second part, LIN, being different kinds of linker (Linker); the third part, the ULM, being a small molecule ligand (ULM, ubiquitin ligase binding moiety) with ubiquitination of VHL, CRBN or other proteases; and the fourth part, the group A, being a carbonyl group or absent, which covalently bond ALK-TKI to LIN, wherein LIN and ULM are covalently bonded. A series of compounds designed and synthesized by the present disclosure have wide pharmacological activities, have functions of degrading ALK protein and inhibiting ALK activity, and can be used for related tumor treatment.