公开(公告)号：US10787666B2

公开(公告)日：2020-09-29

申请号：US16469816

申请日：2016-12-14

Applicant: ShanghaiTech University

Inventor： Haifan Lin ,  Zifeng Wang ,  Sanhong Liu ,  Shuo Shi

IPC: A61K48/00 ,  C07H21/04 ,  C12N15/113 ,  C12Q1/6886

Abstract: Provided methods for diagnosing and treating cancer by reducing the biological activity and/or expression of P-element induced wimpy testis-like protein 4 (PIWIL4), and related compositions and methods.

公开(公告)号：US11771709B2

公开(公告)日：2023-10-03

申请号：US16902172

申请日：2020-06-15

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Xiaoling Song ,  Haifan Lin ,  Ning Sun ,  Jinju Chen ,  Xing Qiu ,  Chaowei Ren ,  Ying Kong

IPC: A61K31/662 ,  A61P35/00 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06

CPC classification number: A61K31/662 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61P35/00 ,  A61K45/06

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.

公开(公告)号：US20200306273A1

公开(公告)日：2020-10-01

申请号：US16902172

申请日：2020-06-15

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Xiaoling Song ,  Haifan Lin ,  Ning Sun ,  Jinju Chen ,  Xing Qiu ,  Chaowei Ren ,  Ying Kong

IPC: A61K31/662 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/454 ,  A61K31/519 ,  A61K31/501 ,  A61P35/00

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.