公开(公告)号：US20240336622A1

公开(公告)日：2024-10-10

申请号：US18260653

申请日：2022-01-08

Applicant: The Board of Regents of The University of Texas System

Inventor： Yonghao YU ,  Tian QIN ,  Yuanli ZHEN ,  Peng LI ,  Chiho KIM ,  Heping DENG ,  Hejun DENG

IPC: C07D493/06 ,  A61K31/365 ,  A61K31/443 ,  A61K45/06 ,  A61P35/00 ,  C07D307/77

CPC classification number: C07D493/06 ,  A61K31/365 ,  A61K31/443 ,  A61K45/06 ,  A61P35/00 ,  C07D307/77

Abstract: Disclosed herein are compounds of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of manufacturing and pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as PARP1 inhibitors. In some aspects, the present disclosure provides methods wherein the compounds and compositions described herein are used for the treatment of diseases and disorders, such as cancer.

公开(公告)号：US20220098196A1

公开(公告)日：2022-03-31

申请号：US17428605

申请日：2020-01-31

Applicant: The Board of Regents of the University of Texas System

Inventor： Yonghao YU ,  Chuo CHEN ,  Shuai WANG ,  Lei HAN ,  Lin YOU

IPC: C07D471/06 ,  C07D401/14 ,  C07D417/14 ,  C07D487/06 ,  A61K45/06

Abstract: The disclosure provides PARP PROTAC molecules comprising a PARP inhibitor linked to an E3 ligase binder, and their use in treating diseases caused by aberrant PARP activation. Such PROTAC molecules produce selective degradation of one or a specific set of PARP proteins with limited effects on the protein level of other PARPs.