📜(3-Fluoro-2-(Trifluoromethyl)Pyridin-4-yl)(1,4-Dioxa-8-Azaspiro[4,5]Decan-8-yl)Methanone置于盐酸,水,三乙胺体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 10.58H,反应生成Hy-16997 (Incb3911) 参考文献:Processes And Intermediates For Making A Jak Inhibitor 标题:Processes And Intermediates For Making A Jak Inhibitor 摘要:这项发明涉及制备{1-{1-[3-氟-2-(三氟甲基)异烟肼基]哌啶-4-基}-3-[4-(7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-基]氮杂环丙烯基}乙腈的过程和中间体,用于治疗与janus激酶(jak)活性相关的疾病,包括炎症性疾病,自身免疫性疾病,癌症和其他疾病.
专利号:US-9732097-B2 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor 发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI 权利人:INCYTE CORP 摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
专利号:US-2022259212-A1 优先权日:2019-07-11 标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase 发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-11267824-B2 优先权日:2017-08-17 标 题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase 发明人:BOSS CHRISTOPH; BUR DANIEL; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.
专利号:US-2016362426-A1 优先权日:2015-05-11 标题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor
1: Yiu ZZ, Warren RB. Novel Oral Therapies for Psoriasis and Psoriatic Arthritis. Am J Clin Dermatol. 2016 Jun;17(3):191-200. doi: 10.1007/s40257-016-0179-3. doi: 10.1124/dmd.114.060673. Epub 2015 Jan 20. doi: 10.1517/14656566.2014.913024. Epub 2014 Apr 25. Review. A process for the preparation of key intermediates towards the synthesis of fluorotrifluoromethylisonicotinoylpiperidinylpyrrolopyrimidinylpyrazolylazetidinylacetonitrile for use as a JAK inhibitor. U.S. Pat. Appl. Publ. (2014), US 20140256941 A1 20140911.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749