CAS: 17180-93-7; 4-Chloropyrimidine

上下游产品

pyrimidine-4(3H)-one Pyrimidin-4-ol PYRIMIDINE 4-(4-chloro-2-fluoro-5-methoxyphenyl)-5-cyano-6-difluoro-methylpyrimidine Methyl 2-chloro-5-(5-cyano-6-methylpyrimidin-4-yl)-4-fluorobenzoate 4-(2,4-dichlorophenyl)-5-cyano-6-methoxypyrimidine

📜4(3H)-嘧啶酮置于三氯氧磷体系中,化学反应 1.0H,以23%的收率获得4-氯嘧啶
参考文献:通过分子简化设计的半胱氨酸蛋白酶cruzain和rhodesain潜在抑制剂的合成和生物学评估.
标题:通过分子简化设计的半胱氨酸蛋白酶cruzain和rhodesain潜在抑制剂的合成和生物学评估.
摘要:使用分子简化策略合成了已知的克鲁萨因抑制剂8-氯-N-(3-吗啉代丙基)-5H-嘧啶[5,4-B]吲哚-4-胺1的类似物.获得了五个系列的类似物:吲哚,嘧啶,喹啉,苯胺和吡咯衍生物.评估了该化合物对克鲁萨因和罗得沙星酶以及克鲁斯锥虫锥虫和锥虫鞭虫形式的活性.4-氨基喹啉衍生物对两种酶均显示出有希望的活性,Ic50值为15至125µm.这些衍生物是寄生蛋白酶的选择性抑制剂,不能抑制哺乳动物组织蛋白酶b和s.抗克鲁萨因活性最高的化合物(化合物5A; Ic50 = 15µm)比1具有更强的合成可及性,同时保留了其配体效率.如对原始铅所观测到的,化合物5A被证明是竞争性酶抑制剂.此外,它还对克氏锥虫具有活性(ic50 = 67.7µm).有趣的是,嘧啶衍生物4B虽然在酶促测定中没有活性,但与未感染的成纤维细胞相比,它对克鲁斯锥虫(ic50 = 3.1µm)具有很高的选择性指数(si = 128),
Doi:10.1016/j.Bmc.2017.02.009

专利信息

专利号:US-6818633-B2
优先权日:2001-06-29
标题:Antiviral compounds and methods for synthesis and therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

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-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-7115592-B2
优先权日:2003-06-16
标题:Phosphonate substituted pyrimidine compounds and methods for therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN; HOCKOVA DANA
权利人:BIOCHEMISTRY OF THE ACADEMY OF
摘要:Novel compounds are provided having formula (I) n nwheren n R 1 , R 2 , R 3 , R 4 , Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

专利号:US-12054512-B2
优先权日:2017-11-10
标 题 :Sting modulator compounds, and methods of making and using
发明人：VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI
权利人:TAKEDA PHARMACEUTICALS CO
摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.

专利号:US-2004116453-A1
优先权日:2001-07-17
标 题 :Synthesis and methods of use pyrimidine analogues and derivatives
发明人：FICK DAVID B; FOREMAN MARK M; GLASKY ALVIN J
摘要:A pyrimidine derivative or analogue comprises an amino-substituted six-membered heterocyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )-D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption, or promotes blood-brain barrier penetration of the derivative or analogue. The moiety A can have two or three nitrogen atoms in the ring; typically, the moiety A is a pyrimidine moiety, with two nitrogen atoms in the ring. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.