公开(公告)号：EP4342892A1

公开(公告)日：2024-03-27

申请号：EP22832202.0

申请日：2022-06-30

申请人： Hangzhou Healzen Therapeutics Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： ZHOU, Xinglu ,  LI, Jia ,  LIU, Xingguo ,  ZHOU, Yubo ,  HU, Miao ,  LUO, Xiaomin ,  XIE, Jiangfeng ,  KAN, Weijuan ,  SU, Mingbo ,  WU, Yizhe

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61P35/00 ,  A61K31/4427

摘要： Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof, or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

公开(公告)号：EP4434980A1

公开(公告)日：2024-09-25

申请号：EP22895006.9

申请日：2022-11-22

申请人： Hangzhou HealZen Therapeutics Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： ZHOU, Xinglu ,  LI, Jia ,  LIU, Xingguo ,  ZHOU, Yubo ,  HU, Miao ,  LUO, Xiaomin ,  XIE, Jiangfeng ,  KAN, Weijuan ,  WU, Yizhe ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4427 ,  A61P35/00 ,  A61P37/00

CPC分类号： A61K31/4427 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

摘要： Disclosed in the present invention are a Bruton's tyrosine kinase degrading agent, which has a structure represented by general formula 1, or a stereoisomer, a mixture of stereoisomers, or a pharmaceutically acceptable salt and a prodrug thereof, Further disclosed are the uses of the compound and a pharmaceutical composition containing same in the preparation of a drug for treating Bruton's tyrosine kinase-related diseases such as B cell or plasma cell proliferative diseases, The compound of the present invention has potent cell proliferation inhibitory activity, effectively degrades Bruton's tyrosine kinase, and has a good liver particle metabolism stability and good oral absorption properties. The compound can be used alone in drugs or in combination with other drugs for treating a disease, disorder or condition that benefits from the inhibition of the Bruton's tyrosine kinase activity or degradation of the Bruton's tyrosine kinase.