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:CA-2394414-A1 优先权日:1999-12-16 标 题 :Moss genes from physcomitrella patens encoding proteins involved in the synthesis of tocopherols carotenoids
专利号:WO-0063184-A1 优先权日:1999-04-16 标 题:Method for producing 2-(alkylthio)-4-chloropyrimidines 发明人:RODUIT JEAN-PAUL 权利人:LONZA AG; RODUIT JEAN PAUL 摘要:The invention relates to 2- (alkylthio) -4- chloropyrimidines of general formula (I), wherein R<1> represents C1-6 alkyl and R<2> and R<3> are, independently of each other, hydrogen or C1-6 alkyl. Said chloropyrimidines are produced from the corresponding 4- hydroxy-2- mercaptopyrimidines which are reacted with a C1-6 alkyl halide to produce the corresponding 2- (alkylthio) -4- hydroxypyrimidine. The reaction product is subsequently chlorinated with phosgene. The 2- (alkylthio) -4- chlorpyrimidines are intermediate products in the synthesis of fungicides and beta-blockers.
专利号:WO-2013163159-A2 优先权日:2012-04-24 标 题:Design and synthesis of novel inhibitors of isoprenoid biosynthesis
专利号:SU-1738088-A3 优先权日:1987-07-17 标 题 :Method for synthesis of cis-derivatives of n-(3-hydroxy-4-piperidinyl)-benzamide
专利号:WO-2018218006-A1 优先权日:2017-05-24 标 题 :Enzymatic dna synthesis using the terminal transferase activity of template-dependent dna polymerases