CAS: 163042-96-4; (2S,3S,4R,5R)-5-(2-Chloro-6-((3-Iodobenzyl)Amino)-9H-Purin-9-yl)-3,4-Dihydroxy-N-Methyltetrahydrofuran-2-Carboxamide

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CAS号3718-88-5 3-碘苄胺盐酸盐 | CAS号5451-40-1 2,6-二氯嘌呤 | CAS号120046-86-8 2-chloro-N-6-(3... | CAS号152918-18-8 匹利诺生

📜2-Chloro-N6-(3-Iodobenzyl)-Adenine置于ammonium Sulfate,三氟甲磺酸三甲基硅酯,氨体系中,用 1,2-二氯乙烷 用作溶剂,化学反应 83.0H,反应生成1-[2-氯-6-[[(3-碘苯基)甲基]氨基]-9H-嘌呤-9-基]-1-脱氧-N-甲基-Beta-D-呋喃核糖酰胺
参考文献:N6-苄基腺苷-5'-糖醛酰胺的 2-取代增强了对 A3 腺苷受体的选择性.
标题:N6-苄基腺苷-5'-糖醛酰胺的 2-取代增强了对 A3 腺苷受体的选择性.
摘要:合成了带有 N6-(3-碘苄基) 基团的腺苷衍生物,据报道可增强腺苷-5'-糖醛酰胺类似物作为 A3 腺苷受体激动剂的亲和力 (J. Med. Chem. 1994,37,636-646)从甲基β-D-呋喃核苷开始,分10步.比较了大鼠脑膜中 A1 和 A2A 受体以及来自稳定转染的 Cho 细胞的克隆大鼠 A3 受体的结合亲和力. N6-(3-碘苄基)腺苷对 A3 受体的选择性是 A1 或 A2A 受体的 2 倍;因此,它是第一个具有任何 A3 选择性的单取代腺苷类似物.探索了 2-取代与 N6-和 5'-位修饰相结合的效果. 2-氯-N6-(3-碘苄基)腺苷的 Ki 值为 1.4 Nm,对 A3 受体具有中等选择性. 2-Chloro-N6-(3-Iodobenzyl)Adenosine-5'-N-Methyluronamide 的 Ki 值为 0.33 Nm,对 A3 和 A1 和
Doi:10.1021/jm00047A018

专利信息

专利号:US-9018371-B2
优先权日:2007-03-07
标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient
发明人：JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH
权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO
摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.

专利号:US-2024368164-A1
优先权日:2021-04-28
标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof
发明人：RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH
权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH
摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

专利号:US-12358903-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-11739065-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-2023271983-A1
优先权日:2020-07-29
标题 :Functionalized isonitriles and products, preparation and uses thereof
发明人：SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
权利人:UNIV SANTIAGO COMPOSTELA
摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

专利号:WO-2024256496-A1
优先权日:2023-06-14
标题 :[1,2,4]-triazolo[4,3-b]pyridazine derivatives useful as a medicament
发明人：ELIE JONATHAN; GEORGE PASCAL; MIEGE FRÉDÉRIC; MEIJER LAURENT
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) or any of its pharmaceutically acceptable salt. The present invention further relates to a synthesis process for manufacturing compound of formula (I) or any of its pharmaceutically acceptable salts, comprising at least a step of reacting a compound of formula (II) with an amine of formula (IV) NHR5R6 for example in a molar ratio ranging from 1 to 20 eq, with respect to the compound of formula (II), in an aprotic solvent or without solvent or else in a protic solvent.