公开(公告)号：US20250064837A1

公开(公告)日：2025-02-27

申请号：US18923448

申请日：2024-10-22

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Renhong Sun ,  Chaowei Ren ,  Ning Sun ,  Ying Kong ,  Yan Li ,  Jinju Chen ,  Qianqian Yin ,  Xiaoling Song ,  Quanju Zhao ,  Xing Qiu

IPC: A61K31/675 ,  A61K31/138 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5517 ,  A61K45/06 ,  A61K47/54 ,  A61K47/60 ,  A61P35/00

Abstract: The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), 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.

公开(公告)号：US12226424B2

公开(公告)日：2025-02-18

申请号：US17046690

申请日：2019-04-09

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Renhong Sun ,  Chaowei Ren ,  Ning Sun ,  Ying Kong ,  Yan Li ,  Jinju Chen ,  Qianqian Yin ,  Xiaoling Song ,  Quanju Zhao ,  Xing Qiu

IPC: A61K31/675 ,  A61K31/138 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5517 ,  A61K45/06 ,  A61K47/54 ,  A61K47/60 ,  A61P35/00

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.

公开(公告)号：US11639343B2

公开(公告)日：2023-05-02

申请号：US17015319

申请日：2020-09-09

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Qianqian Yin ,  Jinju Chen ,  Quanju Zhao ,  Chaowei Ren ,  Renhong Sun ,  Ning Sun ,  Xing Qiu ,  Ying Kong ,  Yan Li ,  Linyi Liu

IPC: C07D401/14 ,  C07D417/14 ,  A61P35/02 ,  A61K45/06

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.

公开(公告)号：US20220117982A1

公开(公告)日：2022-04-21

申请号：US17046690

申请日：2019-04-09

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Renhong Sun ,  Chaowei Ren ,  Ning Sun ,  Ying Kong ,  Yan Li ,  Jinju Chen ,  Qianqian Yin ,  Xiaoling Song ,  Quanju Zhao ,  Xing Qiu

IPC: A61K31/675 ,  A61K45/06 ,  A61K47/54 ,  A61K47/60 ,  A61K31/506 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/138 ,  A61K31/5517 ,  A61K31/519 ,  A61K31/454 ,  A61P35/00

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.