专利号:WO-2024260325-A1 优先权日:2023-06-19 标题 :Synthesis of macrocyclic compound and medical use of macrocyclic compound 发明人:LU HONGFU; DING XIAO; REN FENG 权利人:INSILICO MEDICINE IP LTD 摘要:Provided in the present invention are the synthesis of a macrocyclic compound and the medical use of the macrocyclic compound. Specifically, provided in the present invention are a compound as show in formula (II), a stereoisomer thereof or a pharmaceutically acceptable salt thereof, which can be used as a CDK7 inhibitor.
专利号:US-2014135497-A1 优先权日:2012-11-13 标题 :Synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine 发明人:LIU LI; AKALAY DENIZ; DONG WEITONG; FENG JIANQING; HEMP CHRISTIAN WOLFGANG; LU JUN; XIE LE; YANG JINSONG 权利人:LIU LI; AKALAY DENIZ; DONG WEITONG; FENG JIANQING; HEMP CHRISTIAN WOLFGANG; LU JUN; XIE LE; YANG JINSONG; BOEHRINGER INGELHEIM INT 摘要:This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients.
专利号:US-7122670-B2 优先权日:2003-09-05 标题:Selective synthesis of CF3-substituted pyrimidines 发明人:KATH JOHN CHARLES; RICHTER DANIEL TYLER; LUZZIO MICHAEL JOSEPH 权利人:PFIZER 摘要:The present invention relates to a method of making a compound of the formula n nwherein X 1 , X 2 and R 3 —R 4 are as defined herein. The method includes reacting a compound of the formulan n nwith an amine of formula 3 (HNR 3 R 4 ) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4-diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the treatment of abnormal cell growth, such as cancer, in mammals.
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-2024059678-A1 优先权日:2021-01-18 标 题 :Synthesis Method for Aminopyrimidine FAK Inhibitor Compound 发明人:DU WU; LV HAIBIN; LI YU; KUANG TONGTAO; GENG XI 权利人:HINOVA PHARMACEUTICALS INC 摘要:A synthesis method for an aminopyrimidine FAK inhibitor compound, relating to the field of pharmaceutical synthesis. In the synthesis method, R1 is hydrogen or a carboxylic acid protecting group, R2 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl, R3 and R4 are each independently selected from hydrogen or deuterium, and R5 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl. The synthesis method is simple to operate, and has low costs. The product prepared can obtain a high total yield (≥66%) and a high purity (≥99%), and the product yield and purity are superior to those in the prior art (in the prior art, the total yield is about 11%, and the purity is 99%). The synthesis method achieves excellent effects, can also successfully prepare a final product on kilogram scale, and is suitable for industrial production, having a good application prospect.
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).