CAS: 1232416-25-9; 5-(4-(Isopropylsulfonyl)Phenyl)-3-(3-(4-((Methylamino)Methyl)Phenyl)Isoxazol-5-yl)Pyrazin-2-Amine

上下游产品

5-(4-(isopropylsulfonyl)phenyl)pyrazin-2-amine 3-bromo-5-(4-(isopropylsulfonyl)phenyl)pyrazin-2-amine 5-(4-isopropylsulfonylphenyl)-3-(2-trimethylsilylethynyl)pyrazin-2-amine tert-butyl N-tert-butoxycarbonyl-N-[5-(4-isopropylsulfonylphenyl)-3-(2-trimethylsilylethynyl)pyrazin-2-yl]carbamate

📜5-(4-(Isopropylsulfonyl)Phenyl)Pyrazin-2-Amine置于4-二甲氨基吡啶,N-溴代丁二酰亚胺(Nbs),Copper(L) Iodide,四(三苯基膦)钯,偶氮二异丁腈,Sodium Carbonate,三乙胺,三氟乙酸体系中,用 四氢呋喃,甲醇,乙醇,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 26.0H,反应生成3-[3-[4-[(甲基氨基)甲基]苯基]-5-异恶唑基]-5-[4-[异丙磺酰基]苯基]-2-吡嗪胺
参考文献:Rational Design Of 5-(4-(Isopropylsulfonyl)Phenyl)-3-(3-(4-((Methylamino)Methyl)Phenyl)Isoxazol-5-yl)Pyrazin-2-Amine (Vx-970,M6620): Optimization Of Intra-And Intermolecular Polar Interactions Of A New Ataxia Telangiectasia Mutated And Rad3-Related (Atr) Kinase Inhibitor
标题:Rational Design Of 5-(4-(Isopropylsulfonyl)Phenyl)-3-(3-(4-((Methylamino)Methyl)Phenyl)Isoxazol-5-yl)Pyrazin-2-Amine (Vx-970,M6620): Optimization Of Intra-And Intermolecular Polar Interactions Of A New Ataxia Telangiectasia Mutated And Rad3-Related (Atr) Kinase Inhibitor
摘要:The Dna Damage Response (Ddr) Is A Dna Damage Surveillance And Repair Mechanism That Can Limit The Effectiveness Of Radiotherapy And Dna-Damaging Chemotherapy,Commonly Used Treatment Modalities In Cancer. Two Related Kinases,Ataxia Telangiectasia Mutated (Atm) And Atm And Rad3-Related Kinase (Atr),Work Together As Apical Proteins In The Ddr To Maintain Genome Stability And Cell Survival In The Face Of Potentially Lethal Forms Of Dna Damage. However,Compromised Atm Signaling Is A Common Characteristic Of Tumor Cells,Which Places Greater Reliance On Atr To Mediate The Ddr. In Such Circumstances,Atr Inhibition Has Been Shown To Enhance The Toxicity Of Dna Damaging Chemotherapy To Many Cancer Cells In Multiple Preclinical Studies,While Healthy Tissue With Functional Atm Can Tolerate Atr Inhibition. Atr Therefore Represents A Very Attractive Anticancer Target. Herein We Describe The Discovery Of Vx-970/m6620,The First Atr Inhibitor To Enter Clinical Studies,Which Is Based On A 2-Aminopyrazine Core First Reported By Charrier Et Al. (J. Med. Chem. 2011,54,2320-2330,Doi: ).
Doi:10.1021/acs.Jmedchem.9B00426

专利信息

专利号:US-11801232-B2
优先权日:2019-11-27
标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
发明人：HUANG GLORIA
权利人:UNIV YALE
摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.

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).