CAS: 50264-69-2; 1-(2,4-Dichlorobenzyl)-1H-Indazole-3-Carboxylic Acid

上下游产品

CAS号94-99-5 2,4-二氯氯苄 | CAS号43120-28-1 1H-吲唑-3-羧酸甲酯 | CAS号874110-84-6 1-[(2,4-dichlor...

(1-(2,4-Dichlorobenzyl)-1H-Indazol-3-yl)Methanol置于chromium(Vi) Oxide,硫酸体系中,用 丙酮 作为反应溶剂,化学反应 24.0H,以84%的收率获得产物氯尼达明
参考文献:铜(i)介导的邻卤代芳基n-甲苯磺酰hydr的环化反应:吲唑的高效合成
标题:铜(i)介导的邻卤代芳基n-甲苯磺酰hydr的环化反应:吲唑的高效合成
摘要:从邻卤代芳基n-甲苯磺酰基hydr的易获得的e / Z混合物中开发了吲唑的有效合成方法.讨论了n-甲苯磺酰hydr的热诱导异构化.以高收率制备了一系列有价值的吲唑衍生物,该方法已成功地用于生物活性化合物的合成,如:Lonidamine,Af-2785,Axitinib,Yc-1和yd-3.
DOI:10.1002/adsc.201500953

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人：GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人：HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:WO-2023008461-A1
优先权日:2021-07-27
标题:Medicament for treatment and/or prevention of cancer
发明人：KUME MASAHIKO; OKANO FUMIYOSHI; SAITO TAKANORI
权利人:TORAY INDUSTRIES
摘要:The present invention relates to a medicament for the treatment and/or prevention of cancer, the medicament being characterized by comprising an antibody having an immunological reactivity with CAPRIN-1 protein or a fragment of the antibody and a drug capable of inhibiting the N-glycoside-linked sugar chain synthesis of a glycoprotein which are combined with each other in a blended or separated form.