2-氨基-6-氯烟酸置于四(三苯基膦)钯,氯化亚砜,氨,N,N-二异丙基乙胺,三氯氧磷体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基乙酰胺,甲苯 用作溶剂,化学反应生成[5-[2,4-二((3S)-3-甲基吗啉-4-基)吡啶并[2,3-D]嘧啶-7-基]-2-甲氧基苯基]甲醇 参考文献:Optimization Of Potent And Selective Dual Mtorc1 And Mtorc2 Inhibitors: The Discovery Of Azd8055 And Azd2014 标题:Optimization Of Potent And Selective Dual Mtorc1 And Mtorc2 Inhibitors: The Discovery Of Azd8055 And Azd2014 摘要:The Optimization Of A Potent And Highly Selective Series Of Dual Mtorc1 And Mtorc2 Inhibitors Is Described. An Initial Focus On Improving Cellular Potency Whilst Maintaining Or Improving Other Key Parameters,Such As Aqueous Solubility And Margins Over Herg Ic50,Led To The Discovery Of The Clinical Candidate Azd8055 (14). Further Optimization,Particularly Aimed At Reducing The Rate Of Metabolism In Human Hepatocyte Incubations,Resulted In The Discovery Of The Clinical Candidate Azd2014 (21). (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2013.01.019
专利号:US-2023295162-A1 优先权日:2020-08-06 标 题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity 发明人:CSÃ?MPAI ANTAL; BÃ?RÃ?NY PÉTER; CZUCZI TAMÃ?S; Kovács Imre; ADAMIS BÃ?LINT; NÉMETH ZSÓFIA; MURÃ?NYI JÓZSEF; OLÃ?HNÉ SZABÓ RITA; BOSZE SZILVIA; MEZO GÃ?BOR; KOHIDAI LÃ?SZLÓ; LAJKÓ ESZTER; TAKÃ?CS ANGÉLA; Láng Orsolya; MEZO DIÃ?NA 权利人:EOETVOES LORAND TUDOMANYEGYETEM; SEMMELWEIS EGYETEM 摘要:The present invention relates to compounds of formula (I) (I) or pharmaceutically acceptable salts, and stereoisomers thereof, including enantiomers, racemic mixtures, mixtures of enantiomers, or combinations thereof, which are applicable for use in treating cancer diseases. The present invention further relates to a pharmaceutical composition comprising the above compounds.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
专利号:EP-4192467-A1 优先权日:2020-08-06 标题 :Synthesis of novel imipridone derivatives and their evaluation for their anticancer activity
专利号:US-2022047711-A1 优先权日:2018-12-10 标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins 发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA 权利人:GENENTECH INC 摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.
专利号:CN-116437925-A 优先权日:2020-08-06 标题 :Synthesis of novel elmidone derivatives and evaluation of anticancer activity thereof
1: Holt SV, Logie A, Davies BR, Alferez D, Runswick S, Fenton S, Chresta CM, Gu Y, Zhang J, Wu YL, Wilkinson RW, Guichard S, Smith PD. Enhanced apoptosis and tumor growth suppression elicited by combination of MEK and mTOR kinase inhibitors. Cancer Res. 2012 Jan 23. [Epub ahead of print] Epub 2011 Sep 23. 5: Shao H, Gao C, Tang H, Zhang H, Roberts LR, Hylander BL, Repasky EA, Ma WW, Qiu J, Adjei AA, Dy GK, Yu C. Dual targeting of mTORC1/C2 complexes enhances histone deacetylase inhibitor-mediated anti-tumor efficacy in primary HCC cancer in vitro and in vivo. J Hepatol. 2012 Jan;56(1):176-83. Epub 2011 Aug 9. 7: Jiang Q, Weiss JM, Back T, Chan T, Ortaldo JR, Guichard S, Wiltrout RH. mTOR kinase inhibitor AZD8055 enhances the immunotherapeutic activity of an agonist CD40 antibody in cancer treatment. Cancer Res. 2011 Jun 15;71(12):4074-84. Epub 2011 May 3.
合成参考文献
参考文献:10.1158/0008-5472.can-09-1751 摘要:Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res. 2010 Jan 01;70(1):288–98. doi: 10.1158/0008-5472.can-09-1751. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749