专利号:US-11370736-B2 优先权日:2019-04-01 标 题:Synthesis of fluoro hemiacetals via transition metal-catalyzed fluoro ester and carboxamide hydrogenation 发明人:DUB PAVEL A; BATRICE RAMI J; GORDON JOHN C 权利人:TRIAD NAT SECURITY LLC 摘要:This application is directed to use of transition metal-ligand complexes to hydrogenate fluorinated esters and carboxamides into fluorinated hemiacetals. Methods for synthesis of certain ligands are also provided.
专利号:US-12172982-B2 优先权日:2020-08-12 标 题:Synthesis of quinazoline compounds 发明人:LIM NGIAP-KIE; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BIGLER RAPHAEL; CLAGG KYLE BRADLEY PASCUAL; DIPASQUALE ANTONIO GIOVANNI; GOSSELIN FRANCIS; ORCEL UGO JONATHAN; MEIER ROLAND CHRISTOPH 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
专利号:US-7312250-B2 优先权日:2002-03-12 标题 :Fluorine-substituted alkyl phenol compounds and their uses 发明人:BAKER MAX T; NAGUIB MOHAMED 权利人:UNIV IOWA RES FOUND 摘要:The present invention relates to the synthesis of fluorinated forms of alkyl phenol compounds and their subsequent use as pharmaceutical agents. More specifically, alkyl phenol compounds are fluorinated to increase compound volatility such that the compound may be administered to a mammal, such as a human being, by inhalation. The invention also provides an inhaler (or vaporizer), that can be used for administration of the volatile derivatives of fluorine-substituted alkyl phenol compound. Further, different derivatives of fluorine-substituted alkyl phenol compound can be also administered by other routes as described in this document.
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:US-6723715-B1 优先权日:1999-12-08 标 题:14, 15-cyclopropanosteroids of the 19-norandrostane series, method for producing said compounds and pharmaceutical preparation containing said compounds 发明人:RING SVEN; ELGER WALTER; KAUFMANN GUENTER 权利人:SCHERING AG 摘要:The invention relates to the new 14,15-cyclopropanoandrosteroids of the 19-norandrostane series of the general formula (I) n their synthesis and to pharmaceutical compositions containing these compounds. n The compounds of formula (I) have an interesting, mixed androgen/gestagen profile, the androgenic or gestagenic activity predominating, depending on the substitution.
专利号:WO-2022035790-A1 优先权日:2020-08-12 标题:Synthesis of quinazoline compounds
[参考文献]: David Orr, Et Al. Evaluating The Thermal Vinylcyclopropane Rearrangement (Vcpr) As A Practical Method For The Synthesis Of Difluorinated Cyclopentenes: Experimental And Computational Studies Of Rearrangement Stereospecificity. Chemistry. 2014 Oct 27;20(44):14305-16.
合成参考文献
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