📜Carbamic Acid,N-[(1S)-2-[[(1S)-1-Cyclohexyl-2-[(2S)-2-[4-(4-Fluorobenzoyl)-2-Thiazolyl]-1-Pyrrolidinyl]-2-Oxoethyl]Amino]-1-Methyl-2-Oxoethyl]-N-Methyl-,1,1-Dimethylethyl Ester 以99的收率获得lcl161,凋亡蛋白抑制因子抑制剂 参考文献:Smac Peptidometics Useful As Iap Inhibitors 标题:Smac Peptidometics Useful As Iap Inhibitors 摘要:本发明涉及以下式的化合物:或其药学上可接受的盐,并且利用这种化合物治疗哺乳动物的增殖性疾病,例如癌症.
专利信息
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2024066133-A1 优先权日:2020-03-06 标 题 :Therapeutic agents and conjugates thereof 发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.
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合成参考文献
参考文献:10.1038/ncomms14278 摘要:Beug ST, Beauregard CE, Healy C, Sanda T, St-Jean M, Chabot J, Walker DE, Mohan A, Earl N, Lun X, Senger DL, Robbins SM, Staeheli P, Forsyth PA, Alain T, LaCasse EC, Korneluk RG. Smac mimetics synergize with immune checkpoint inhibitors to promote tumour immunity against glioblastoma. Nature Communications. 2017 Feb 15;8(1):14278. doi: 10.1038/ncomms14278. 参考文献:10.1038/s41419-020-02879-y 摘要:Miles MA, Hawkins CJ. In vitro analysis reveals necroptotic signaling does not provoke DNA damage or HPRT mutations. Cell Death & Disease. 2020 Aug 13;11(8):680. doi: 10.1038/s41419-020-02879-y. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749