专利号:US-12319691-B2 优先权日:2020-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI 权利人:AMGEN INC; VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-12428425-B2 优先权日:2020-05-04 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; PANTELEEV JANE; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:AMGEN INC; VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:WO-2025128873-A1 优先权日:2023-12-12 标题:Heterocyclic pyridinone compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
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:CN-111909140-A 优先权日:2019-04-12 标题:Heterocyclic compounds as TYK2 inhibitors and methods of synthesis and use
专利号:CN-119101020-A 优先权日:2024-09-04 标 题 :Synthesis method of 3-oxetane carbonitrile
摘要:Hagen, T. J.; Helgren, T. R., Science of Synthesis Knowledge Updates, (2015) 2, 147. 摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 419. 摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 422.