CAS: 122536-77-0; (R)-Tert-Butyl Pyrrolidin-3-Ylcarbamate

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(3R)-(+)-1-苄基-3-(叔丁氧羰基氨基)吡咯烷置于palladium Dihydroxide 氢气体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 24.0H,以100%的收率获得(R)-3-叔丁氧羰基氨基吡咯烷
参考文献:Novel Angular Benzophenazines: Dual Topoisomerase I And Topoisomerase Ii Inhibitors As Potential Anticancer Agents
标题:Novel Angular Benzophenazines: Dual Topoisomerase I And Topoisomerase Ii Inhibitors As Potential Anticancer Agents
摘要:A Series Of Substituted Angular Benzophenazines Were Prepared Using A New Synthetic Route Via A Novel Regiocontrolled Condensation Of 1,2-Naphthoquinones And 2,3-Diaminobenzoic Acids. The Synthesis And Biological Activity Of This New Series Of Substituted 8,9-Benzo[a]Phenazine Carboxamide Systems Are Described. The Analogues Were Evaluated Against The H69 Parental Human Small Cell Lung Carcinoma Cell Line And H69/lx4 Resistant Cell Line Which Overexpresses P-Glycoprotein. Selected Analogues Were Evaluated Against The Cor-L23-Parental Human Non Small Cell Lung Carcinoma Cell Line And The Cor-L23/r Resistant Cell Line Which Overexpresses Multidrug Resistance Protein. This Series Of Novel Angular Benzophenazines Were Potent Cytotoxic Agents In These Cell Lines And May Be Able To Circumvent Multidrug Resistance Mechanisms Which Result In The Lack Of Efficacy Of Many Drugs In Cancer Chemotherapy. These Compounds Show Dual Inhibition Of Topoisomerase I And Topoisomerase Ii And Thus Target Two Key Enzymes Responsible For The Topology Of Dna That Are Active At Different Points In The Cell Cycle. The Introduction Of Chirality Into The Carboxamide Side Chain Of These Novel Benzophenazine Carboxamides Has Resulted In The Discovery Of A Potent Enantiospecific Series Of Cytotoxic Agents,Exemplified By 4-Methoxy-Benzo[a]Phenazine-11-Carboxylic Acid (2-(Dimethylamino)-1-(R)Methyl-Ethyl)-Amide,Xr11576 ((R)-4J"). In Vivo Activity Has Been Demonstrated For 4-Methoxy-Benzo[a]Phenazine-11-Carboxylic Acid (2-(Dimethylamino)-1-(R)-Methyl-Ethyl)-Amide,Xr11576,After Intravenous Administration To Female Mice,And This Compound Has Been Selected As A Development Candidate For Further Evaluation.
Doi:10.1021/jm010329A

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-6255315-B1
优先权日:1997-06-18
标题:Alpha 1a adrenergic receptor antagonists
发明人：PATANE MICHAEL A; SELNICK HAROLD G; BOCK MARK G
权利人:MERCK & CO INC
摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha relductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.