CAS: 1160295-21-5; ((1S,2S,4R)-4-(4-(((S)-2,3-Dihydro-1H-Inden-1-yl)Amino)-7H-Pyrrolo[2,3-D]Pyrimidin-7-yl)-2-Hydroxycyclopentyl)Methyl Sulfamate Hydrochloride

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上下游产品

((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)-methyl sulfamate 4-chloro-1H-pyrrolo[2,3-d]pyrimidine (1S,2S,4R)-4-{4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-(hydroxymethyl)-cyclopentanol (1,4-diazabicyclo[2.2.2]°Ctan-1-ium-1-ylsulfonyl)(tert-butoxycarbonyl)amide

合成工艺路线路线简述

    📜氨基磺酸 [(1S,2S,4R)-4-[4-[[(1S)-2,3-二氢-1H-茚-1-基]氨基]-7H-吡咯并[2,3-D]嘧啶-7-基]-2-羟基环戊基]甲基酯置于盐酸体系中,用 乙醇 用作溶剂,化学反应生成氨基磺酸[(1S,2S,4R)-4-[4-[[(1S)-2,3-二氢-1H-茚-1-基]氨基]-7H-吡咯并[2,3-D]嘧啶-7-基]-2-羟基环戊基]甲基酯盐酸盐
    参考文献: Hydrochloride Salt Of ((1S,2S,4R)-4-{4-[(1S)-2,3-Dihydro-1H-Inden-1-Ylamino]-7H-Pyrrolo [2,3-D]Pyrimidin-7-Yl}-2-Hydroxycyclopentyl)Methyl Sulfamate[fr] Sel De Chlorhydrate De ((1S,2S,4R)-4-{4-[(1S)-2,3-Dihydro-1H-Indèn-1-Ylamino]-7H-Pyrrolo [2,3-D] Pyrimidin-7-Yle}-2-Hydroxycyclopentyle) Méthylsulfamate
    标题: Hydrochloride Salt Of ((1S,2S,4R)-4-{4-[(1S)-2,3-Dihydro-1H-Inden-1-Ylamino]-7H-Pyrrolo [2,3-D]Pyrimidin-7-Yl}-2-Hydroxycyclopentyl)Methyl Sulfamate[fr] Sel De Chlorhydrate De ((1S,2S,4R)-4-{4-[(1S)-2,3-Dihydro-1H-Indèn-1-Ylamino]-7H-Pyrrolo [2,3-D] Pyrimidin-7-Yle}-2-Hydroxycyclopentyle) Méthylsulfamate
    摘要:本发明公开了一种化合物(I);其晶体形式和溶剂化物;含有化合物(I)或其晶体形式或溶剂化物的药物组合物,以及药学上有效量的化合物(I)或其晶体形式或溶剂化物和药学上可接受的载体或稀释剂;以及使用化合物(I)或其晶体形式或溶剂化物治疗患有或有可能通过抑制el激活酶(特别是nae)改善病理状况的患者,包括癌症.

    海关参考信息

    专利信息


    专利号:US-2024261416-A1
    优先权日:2023-01-31
    标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them
    发明人:TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.

    专利号:US-2025222120-A1
    优先权日:2024-01-09
    标题 :Synthesis of novel small molecule carm1 degraders, compounds formed thereby, and pharmaceutical compositions containing them
    发明人:TANG WEIPING; XU WEI; XIE HAIBO; BACABAC MEGAN
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:Provided herein are CARM1 PROTACs comprising a binding molecule of CARM1 with an optimized linker attached to an E3 ubiquitin ligase ligand that recruits the E3 ubiquitin ligase to CARM1. The PROTACs find use, e.g., for selectively targeted degradation of CARM1 protein in cancer cells. Also provided herein are compositions comprising the PROTACs, as well as methods of using the PROTACs.

    专利号:WO-2025076501-A1
    优先权日:2023-10-06
    标题:High throughput parallel synthesis of small molecule degraders
    发明人:SHAUM JAMIE; ERB MICHAEL A; STEEN ERICA
    权利人:SCRIPPS RESEARCH INST
    摘要:Disclosed herein are high throughput synthetic methods for the deliberate and prospective discovery of molecular glues which can be used to form composite protein-ligand surfaces that facilitate interfacial binding to other proteins over dispersed surfaces. In particular, this application discloses a high throughput approach using sulfur(VI) fluoride exchange (SuFEx) transformations and N-hydroxysuccinimide (NHS)-ester derived amide couplings to prospectively repurpose known ligands for a prolein-of-interest into degraders and compounds capable of inducing proximity to other proteins. Disclosed herein are methods of developing known ligands of a target protein into degraders of the target proteins. Further disclosed are methods of developing novel small molecule chromatin-competitive inhibitors of the eleven nineteen leukemia (ENL) YEATS domain into effective degraders of ENL.

    专利号:US-12054512-B2
    优先权日:2017-11-10
    标 题 :Sting modulator compounds, and methods of making and using
    发明人:VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.

    专利号:US-2022143183-A1
    优先权日:2019-02-23
    标题:Photoswitchable protacs and synthesis and uses thereof
    发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE
    权利人:UNIV NEW YORK
    摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.

    专利号:US-2023310400-A9
    优先权日:2018-07-23
    标题 :Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Paiva C, Godbersen JC, Berger A, Brown JR, Danilov AV. Targeting neddylation induces DNA damage and checkpoint activation and sensitizes chronic lymphocytic leukemia B cells to alkylating agents. Cell Death Dis. 2015 Jul 9;6:e1807. doi: 10.1038/cddis.2015.161.

    合成参考文献


    参考文献:10.1128/mcb.05746-11
    摘要:Tan MM, Lim H, Harper JW. SCFFBXO22 Regulates Histone H3 Lysine 9 and 36 Methylation Levels by Targeting Histone Demethylase KDM4A for Ubiquitin-Mediated Proteasomal Degradation. Molecular and Cellular Biology. 2011 Sep 01;31(18):3687–99. doi: 10.1128/mcb.05746-11.
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