异胞嘧啶置于氯磺酸,三氯氧磷,Ammonium Hydroxide体系中,用 水 用作溶剂,以92%的收率获得2-氨基-4-氯嘧啶 参考文献: Alkynyl Alcohols As Kinase Inhibitors[fr] Alcools D'Alcynyle Utilisés Comme Inhibiteurs De Kinases 标题: Alkynyl Alcohols As Kinase Inhibitors[fr] Alcools D'Alcynyle Utilisés Comme Inhibiteurs De Kinases 摘要:选定的化合物对预防和治疗炎症和炎症性疾病,如nik介导的疾病,具有有效性.该发明涵盖了新颖的化合物,类似物,前药及其药用可接受的盐,以及用于预防和治疗涉及炎症等疾病和其他疾病或病症的药物组合物和方法.
专利信息
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2002040032-A1 优先权日:2000-07-07 标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system 发明人:GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R 摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.
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-8895747-B2 优先权日:2009-07-27 标 题 :Method and substances for preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL 权利人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
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:WO-2011050245-A1 优先权日:2009-10-23 标 题:Bicyclic heteroaryls as kinase inhibitors 发明人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
[参考文献]: Adam Littke, Et Al. Mild And General Methods For The Palladium-Catalyzed Cyanation Of Aryl And Heteroaryl Chlorides. Org Lett. 2007 Apr 26;9(9):1711-4.
合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 411. 参考文献:10.1021/jm011095y 摘要:Holý A, Votruba I, Masojídková M, Andrei G, Snoeck R, Naesens L, De Clercq E, Balzarini J. 6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activity. J Med Chem. 2002 Apr 25;45(9):1918–29. doi: 10.1021/jm011095y.