专利号:US-2024082435-A1 优先权日:2021-02-26 标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents 发明人:PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS 权利人:TELIX INT INNOVATIONS PTY LTD 摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
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:WO-2022178592-A1 优先权日:2021-02-26 标题 :Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agents
专利号:EP-4297804-A1 优先权日:2021-02-26 标题 :Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agents
专利号:CN-117355343-A 优先权日:2021-02-26 标题:Solid-phase synthesis of glutamate-urea-lysine-derived (GUL-derived) conjugates targeting prostate-specific membrane antigen (PSMA) and their use as precursors to therapeutic and/or diagnostic agents
专利号:US-7732628-B2 优先权日:2000-03-22 标题 :Functional biopolymer modification reagents and uses thereof 发明人:SCHWARTZ DAVID A; HOGREFE RICHARD I 权利人:SOLULINK INC 摘要:Hydrazino, oxyamino and carbonyl-based reagents and methods for incorporation into oligonucleotides during their solid phase synthesis are provided. Modified oligonucleotides are provided that incorporate the reagents provided herein. Immobilized oligonucleotides and oligonucleotide conjugates that contain covalent hydrazone or oxime linkages are provided. Methods for preparation of surface bound oligonucleotides are provided. Methods for the preparation of oligonucleotide conjugates are also provided.
参考文献:10.3390/ijms130810067 摘要:Szymański P, Lázničková A, Lázniček M, Bajda M, Malawska B, Markowicz M, Mikiciuk-Olasik E. 2,3-dihydro-1H-cyclopenta[b]quinoline derivatives as acetylcholinesterase inhibitors-synthesis, radiolabeling and biodistribution. Int J Mol Sci. 2012;13(8):10067–90.