CAS: 1086111-09-2; Thiazole-5-Boronic Acid Pinacol Ester

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1218791-01-5 1662682-33-8 1402166-32-8

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CAS号3034-55-7 5-溴噻唑 | CAS号73183-34-3 双戊酰二硼 | CAS号76-09-5 频哪醇 | CAS号79265-30-8 2-(三甲基硅基)噻唑 | CAS号1826-13-7 5-苯基噻唑

3,5-二甲基异恶唑-4-硼酸频哪醇酯置于正丁基锂体系中,用 四氢呋喃,1,4-二氧六环,正己烷 用作溶剂,化学反应 3.5H,反应生成5-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)噻唑
参考文献:(杂)芳基硼酸酯的原脱硼:直接与预水解途径和自/自催化
标题:(杂)芳基硼酸酯的原脱硼:直接与预水解途径和自/自催化
摘要:一系列硼酸酯的碱催化水解(arb(Or) 2-> Arb(Oh) 2)和原脱硼化(arb(Or) 2-> Arh)的动力学和机理,包括八种不同的多元醇和 10 种多氟芳基和杂芳基部分,已通过原位和停流 NMR 光谱(19 F,1 H 和11 B),Ph 速率依赖性,同位素夹带进行了研究,2H Kie 和 Ks-Dft 计算.该研究揭示了硼酸酯在碱性水-有机条件下的现象稳定性非常微妙.与通常的假设相反,与相应的硼酸相比,酯化不一定赋予更高的稳定性.此外,酯水解为硼酸可以是整个原脱硼过程的主要成分,当 Ph 值接近硼酸的 P K A时,自催化,自催化和氧化(酚类)催化作用增强酯.
Doi:10.1021/jacs.1C06863

专利信息

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-2023025807-A1
优先权日:2019-10-30
标题:Cd38 inhibitors
发明人：KULKARNI SANTOSH S; LAGU BHARAT; WU XINYUAN
权利人:MITOBRIDGE INC
摘要:The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD + or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).