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.

公开(公告)号：EP4442685A1

公开(公告)日：2024-10-09

申请号：EP22903465.7

申请日：2022-12-06

申请人： Hangzhou HealZen Therapeutics Co., Ltd. ,  Guangdong Hongye Pharmaceutical Co., Ltd.

发明人： LIU, Xingguo ,  SU, Mingbo ,  WU, Yizhe ,  GAO, Anhui ,  ZHOU, Xinglu ,  ZHONG, Li ,  HU, Miao ,  HUANG, Jinglai ,  JING, Hanghui ,  ZHU, Jianrong

IPC分类号： C07D403/12 ,  C07D471/04 ,  C07D498/14 ,  A61K31/496 ,  A61K31/437 ,  A61K31/499 ,  A61P35/00

CPC分类号： Y02P20/55 ,  A61K31/437 ,  A61K31/438 ,  A61K31/496 ,  A61K31/499 ,  A61K31/635 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D403/12 ,  C07D471/04 ,  C07D498/14

摘要： Disclosed is a BCL-2 protein apoptosis inducer, and further disclosed are the uses of the compound and a pharmaceutical composition comprising the compound in the preparation of a drug for treating diseases related to anti-apoptotic protein BCL-2. The compound has potent BCL-2BAK blocking activity, and can be used for treating diseases such as infectious diseases, immune diseases, inflammatory diseases or cell proliferation abnormalities that benefit from the inhibition of anti-apoptotic protein BCL-2.

公开(公告)号：EP4269412A1

公开(公告)日：2023-11-01

申请号：EP21909408.3

申请日：2021-12-21

申请人： Hangzhou Healzen Therapeutics Co., Ltd.

发明人： ZHOU, Xinglu ,  LIU, Xingguo ,  HU, Miao ,  ZHU, Jianrong ,  WU, Yizhe

IPC分类号： C07D487/04 ,  A61P35/00

摘要： The present disclosure discloses a crystal form of a casein kinase 1ε inhibitor and a preparation method and use of the crystal form. Specifically, the present disclosure relates to a crystal form of the compound ( S )-2-(1-(4-amino-3-(2,3-difluoro-4-methoxyphenyl)-1 H -pyrazolo[3,4- d ]pyrimidin-1-yl)ethyl)-5 -chloro-3-phenylquinazoline-4(3 H )one methanesulfonate and a preparation method and use of the crystal form. The crystal form of the casein kinase 1ε inhibitor compound of the present disclosure has good water solubility and oral absorption, and can be better used for the treatment of malignant tumors and autoimmune diseases that benefit from the inhibition of casein kinase 1ε activity.

公开(公告)号：EP3964512A1

公开(公告)日：2022-03-09

申请号：EP20830639.9

申请日：2020-06-23

申请人： Hangzhou Healzen Therapeutics Co., Ltd.

发明人： ZHOU, Xinglu ,  LIU, Xingguo ,  HU, Miao

IPC分类号： C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  A61P37/00 ,  A61P11/00

摘要： Disclosed in the present invention is a novel substituted pyrazolopyrimidine compound that inhibits the activity of casein kinase 1ε (CK1ε) and a stereoisomer or stereoisomer mixture thereof, or a pharmaceutically acceptable salt or solvate thereof, and an application thereof in preparation of drugs for treating diseases, disorders or conditions that benefit from the inhibition of the activity of the casein kinase 1ε (CK1ε). The compound of the present invention has an inhibitory activity on CK1ε kinase, OCI-LY10 cells and Karpas299 cells, shows good anti-tumor activity in an OCI-LY10 subcutaneous xenogeneic model and shows excellent synergistic anti-tumor activity in combination with BTK inhibitors. The compound of the present invention has good pharmacokinetics properties and may be used alone or in combination with other drugs to treat diseases, disorders or conditions that benefit from the inhibition of the activity of the casein kinase 1ε, the diseases, disorders or conditions comprising tumors, autoimmune diseases, etc.