公开(公告)号：US11718620B2

公开(公告)日：2023-08-08

申请号：US17139452

申请日：2020-12-31

申请人： TransThera Sciences (Nanjing), Inc.

发明人： Frank Wu

IPC分类号： C07D471/14 ,  A61P35/02 ,  A61P35/00 ,  A61K31/551 ,  C07D487/04 ,  C07D491/08 ,  C07D519/00 ,  A61K45/06 ,  A61K31/5517

CPC分类号： C07D471/14 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  C07D487/04 ,  C07D491/08 ,  C07D519/00

摘要： The present invention relates to a method for treating a cancer mediated by abnormality of multi-kinases, comprising administrating a compound as represented by formula (I) or a pharmaceutically acceptable salt and stereoisomer thereof, wherein R1, R2, X, Y, P, W, and Ar are as defined in the description. Also provided is a method for treating a cancer mediated by abnormality of multi-kinases, comprising administrating a crystal form I of a compound 4-(5-(2-chlorophenyl)-3-methyl-2,10-dihydropyrazolo[4,3-b]pyrido[4,3-e][1,4]diazepin-8-yl)morpholine, wherein in an X-ray powder diffraction pattern of crystal form I, there are characteristic peaks at 7.4±0.2°, 17.9±0.2°, 18.9±0.2°, 19.4±0.2°, 21.5±0.2°, and 23.7±0.2°.

公开(公告)号：US20230129164A1

公开(公告)日：2023-04-27

申请号：US17791680

申请日：2021-02-23

申请人： TransThera Sciences (Nanjing), Inc.

发明人： Peng Peng ,  Xiaoyan Qiang ,  Frank Wu

IPC分类号： A61K31/5517 ,  A61P35/00

摘要： The present invention belongs to the technical field of medicines, relates to novel use of a multi-kinase inhibitor, and particularly relates to a compound of general formula (I) or a pharmaceutically acceptable salt, a stereoisomer and a crystal form thereof for use in the treatment of biliary tract cancer, a pharmaceutical composition comprising the compound, a method for treating biliary tract cancer by using the compound, use of the compound in the treatment of biliary tract cancer, and use of the compound in the preparation of a medicament for treating biliary tract cancer. The variables in the general formula are defined in the specification. Research shows that the multi-kinase inhibitor compound of general formula (I) or the pharmaceutically acceptable salt, the stereoisomer and the crystal form thereof have a treatment effect on biliary tract cancer, and especially on cholangiocarcinoma, so that the compound of the present invention has huge clinical application potential.

公开(公告)号：US20220160696A1

公开(公告)日：2022-05-26

申请号：US17436879

申请日：2020-03-06

申请人： TRANSTHERA SCIENCES (NANJING), INC.

发明人： Zejuan SHENG ,  Frank Wu

IPC分类号： A61K31/4545 ,  A61P9/04

摘要： Disclosed are uses of a compound represented by general formula (I) and pharmaceutically acceptable salts, isomers and deuterated compounds thereof in the preparation of a medicine for treating heart failure diseases. Experiments prove that the compound can improve the heart function of rats with heart failure, reverse myocardial remodeling caused by heart failure, and reduce fibrosis in the marginal zone of infarction.

公开(公告)号：US20240294542A1

公开(公告)日：2024-09-05

申请号：US18566865

申请日：2022-06-02

申请人： TransThera Sciences (Nanjing), Inc.

发明人： Lin Li ,  Frank Wu

IPC分类号： C07D495/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/34 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/18

CPC分类号： C07D495/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/34 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/18

摘要： The present invention belongs to the technical field of medicines, relates to an NLRP3 inflammasome inhibitor and use thereof, and particularly relates to a compound of general formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a tautomer thereof, wherein each group is defined in the specification. Researches show that the compound of general formula (I), or pharmaceutically acceptable salt, the stereoisomer or the tautomer thereof has relatively high biological activity on NLRP3 inflammasomes and has an important clinical development value for the treatment of NLRP3-associated diseases.

公开(公告)号：US20220089593A1

公开(公告)日：2022-03-24

申请号：US17424842

申请日：2020-01-20

申请人： TRANSTHERA SCIENCES (NANJING), INC.

发明人： Frank Wu

IPC分类号： C07D471/04 ,  C07D519/00

摘要： The present invention relates to the technical field of pharmaceuticals, and particularly to a PDE9 inhibitor compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a deuterated compound, a metabolite or a prodrug thereof. The present invention also relates to pharmaceutical formulations, pharmaceutical compositions and use thereof. X1, X2, X3, X4, R1, R2, ring A, L and m are as defined in the specification. The compound of the present invention can be used in the manufacture of a medicament for treating or preventing a PDE9-mediated related disease.