专利号:US-2008242866-A1 优先权日:2007-03-30 标 题 :Synthesis of anthranilamides 发明人:SCHMEES NORBERT; PETROV ORLIN 权利人:SCHMEES NORBERT; PETROV ORLIN 摘要:The present invention relates to a novel method of preparing anthranilamides of formula I: n n n n n n n n n n in which R 1 , R 2 , R 3 , A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.
专利号:US-2025222120-A1 优先权日:2024-01-09 标题 :Synthesis of novel small molecule carm1 degraders, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; XU WEI; XIE HAIBO; BACABAC MEGAN 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Provided herein are CARM1 PROTACs comprising a binding molecule of CARM1 with an optimized linker attached to an E3 ubiquitin ligase ligand that recruits the E3 ubiquitin ligase to CARM1. The PROTACs find use, e.g., for selectively targeted degradation of CARM1 protein in cancer cells. Also provided herein are compositions comprising the PROTACs, as well as methods of using the PROTACs.
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:EP-3070087-B1 优先权日:2011-08-05 标题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:EP-3070087-A1 优先权日:2011-08-05 标 题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:ES-2733096-T3 优先权日:2011-08-05 标题:Intermediaries for the synthesis of cyclic P1 linkers as XIA factor inhibitors