CAS: 5909-24-0; Ethyl 4-Chloro-2-(Methylthio)Pyrimidine-5-Carboxylate

上下游产品

ethyl 3,4-dihydro-2-methylthio-4-oxopyrimidine-5-carboxylate ethyl 4-hydroxy-2-(methylthio)pyrimidine-5-carboxylate diethyl 2-ethoxymethylenemalonate2-methanesulfanyl-4-phenylamino-pyrimidine-5-carboxylic acid ethyl ester ethyl 2-(methylthio)-4-morpholinopyrimidine-5-carboxylate H-pyrimido[4,5-e][1,4]oxazepin-5-one9-benzyl-2-methylsulfanyl-8,9-dihydro-7H-pyrimido[4,5-e][1,4]oxazepin-5-one 4-ethylamino-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester

1,4-二氢-2-甲巯基-4-氧代-5-嘧啶甲酸乙酯置于三氯氧磷体系中,化学反应 3.0H,反应生成 4-氯-2-甲硫基嘧啶-5-羧酸乙酯
参考文献:基于儿茶酰嘧啶的新型 Pde4 抑制剂治疗特应性皮炎的设计,合成和生物学评价
标题:基于儿茶酰嘧啶的新型 Pde4 抑制剂治疗特应性皮炎的设计,合成和生物学评价
摘要:磷酸二酯酶 (pde) 4B 的选择性抑制有利地抑制炎性细胞因子的合成,随后通过调节细胞内 Camp 水平来阻止特应性皮炎的发展.考虑到皮质类固醇的副作用,选择性 Pde4 抑制可能构成治疗特应性皮炎 (ad) 的有效替代疗法.在本研究中,合成了一系列以嘧啶为核心的新型儿茶酚基化合物,并筛选了 Pde4 抑制特性.研发了活性化合物相对于其他 Pde 的 Pde4 选择性.带有嘧啶核心的化合物 23 与儿茶酚,吡啶和三氟甲基官能团化,可有效抑制 Pde4B,Ic50 值在纳摩尔范围内 (ic50 = 15 +/-0.4 Nm).化合物 23 对 Pde4B 的选择性是 Pde4D 的 7 倍.分子对接研究证实了它对 Pde4B 催化结构域的亲和力更强.体内分析证实,化合物 23 通过抑制 Tnf-α 和 Ig-E 等炎症介质的合成,有效缓解了 Dncb 处理的 Balb/c 小鼠的特应性皮炎症状.综上所述,本研究提示化合物
DOI:10.1016/j.Ejmech.2017.12.069

专利信息

专利号:US-11629150-B2
优先权日:2016-07-01
标题:Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines
发明人：SMITH ALEXANDER; WHITE HANNAH S; TAVARES FRANCIS XAVIER; KRASUTSKY SERGIY; CHEN JIAN-XIE; DORROW ROBERTA L; ZHONG HUA
权利人:G1 THERAPEUTICS INC
摘要:This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

专利号:US-7897762-B2
优先权日:2006-09-14
标 题:Kinase inhibitors useful for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:DECIPHERA PHARMACEUTICALS LLC
摘要:The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-11339145-B2
优先权日:2018-05-04
标题 :Synthesis of cerdulatinib
发明人：PANDEY ANJALI; SRAN ARVINDER; CHEN YING; POGGIALI DANIELE; FUMAGALLI TIZIANO
权利人:ALEXION PHARMA INC
摘要:The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I:or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.

专利号:US-2019337930-A1
优先权日:2018-05-04
标 题 :Synthesis of cerdulatinib

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).