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CAS号128117-22-6 1-苄氧羰基-3-羟基氮杂环丁烷 | CAS号40320-60-3 1-二苯甲基氮杂环丁烷-3-酮 | CAS号501-53-1 氯甲酸苄酯 | CAS号67865-70-7 1-diazonio-3-(p... | CAS号1138-80-3 N-苄氧羰基甘氨酸 | CAS号55378-79-5 2-(((benzyloxy)... | CAS号934664-23-0 3-亚甲基氮杂环丁烷-1-羧酸苄酯 | CAS号934664-27-4 2-[3-羟基-1-[(苯基甲...

Ethoxycarbonyl 2-(Phenylmethoxycarbonylamino)Acetate置于dirhodium Tetraacetate体系中,用 四氢呋喃,乙醚,二氯甲烷 用作溶剂,化学反应 7.0H,反应生成1-苄氧羰基氮杂环丁烷-3-酮
参考文献:Serine And Threonine β-Lactones: A New Class Of Hepatitis A Virus 3C Cysteine Proteinase Inhibitors
标题:Serine And Threonine β-Lactones: A New Class Of Hepatitis A Virus 3C Cysteine Proteinase Inhibitors
摘要:Hepatitis A Virus (Hav) 3C Enzyme Is A Cysteine Proteinase Essential For Viral Replication And Infectivity And Represents A Target For The Development Of Antiviral Drugs. A Number Of Serine And Threonine Beta-Lactones Were Synthesized And Tested Against Hav 3C Proteinase. The D-N-Cbz-Serine Beta-Lactone 5A Displays Competitive Reversible Inhibition With A K-I Value Of 1.50 X 10(-6) M. Its Enantiomer,L-N-Cbz-Serine Beta-Lactone 5B Is An Irreversible Inactivator With 0.70 Min(-1),K,= 1.84 X 10(-4) M And K(Inact)/k-I = 3800 M-1 Min(-1). Mass Spectrometry And Hmqc NMR Studies Using C-13-Labeled 5B Show That Inactivation Of The Enzyme occurs By Nucleophilic Attack Of The Cysteine Thiol (Cys-172) At The Beta-Position Of The Oxetanone Ring. Although The N-Cbz-Serine Beta-Lactones 5A And 5B Display Potent Inhibition,Other Related Analogues With An N-Cbz Side Chain,Such As The Five-Membered Ring Homoserine Gamma-Lactones 14A And 14B,The Four-Membered Ring Beta-Lactam 33,2-Methylene Oxetane 34,Cyclobutanone 36,And 3-Azetidinone 39,Fail To Give Significant Inhibition Of Hav 3C Proteinase,Thus Demonstrating The Importance Of The Beta-Lactone Ring For Binding.
Doi:10.1021/jo0109016

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-9856241-B2
优先权日:2013-07-03
标 题:Substituted benzofuranyl and benzoxazolyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.