CAS: 153559-49-0; 4-(1-(3,5,5,8,8-Pentamethyl-5,6,7,8-Tetrahydronaphthalen-2-yl)Vinyl)Benzoic Acid

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CAS号153559-48-9 蓓萨罗丁中间体6 | CAS号6683-48-3 1,1,4,4,6-五甲基-1... | CAS号153559-45-6 4-(3,5,5,8,8-五甲... | CAS号110-03-2 2,5-二甲基-2,5-己二醇 | CAS号1346970-00-0 bexarotene ethy... | CAS号6223-78-5 2,5-二氯-2,5-二甲基己烷 | CAS号119999-22-3 6-溴-1,1,4,4,7-五... | CAS号29020-85-7 2(1H)-Naphthale... | CAS号108-88-3 甲苯 | CAS号167958-79-4 1,1,4,4,6-penta...

4-[(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)羰基]苯甲酸甲酯置于氢氧化钾,Sodium Amide体系中,用 甲醇 用作溶剂,化学反应 1.67H,反应生成蓓萨罗丁
参考文献:Syntheses Of Isotopically Labeled 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-Tetrahydro-2-Naphthyl)Ethenyl]Benzoic Acid (Lgd1069),A Potent Retinoid X Receptor-Selective Ligand
标题:Syntheses Of Isotopically Labeled 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-Tetrahydro-2-Naphthyl)Ethenyl]Benzoic Acid (Lgd1069),A Potent Retinoid X Receptor-Selective Ligand
摘要:Lgd1069,4-[1-(3,5,5,8,8-五甲基-5,6,7,8-四氢-2-纳夫烯)乙烯基]苯甲酸,是首个进入临床试验的选择性维甲酸x受体(Rxr)维甲酸,用于治疗皮肤病和癌症.为了研究生物特性,如受体结合,代谢和生物利用度,需要使用[13C],[14C]和[3H]标记的lgd1069.本文描述了合成同位素标记lgd1069同系物的方法,以及[6,7-3H]-Lgd1069和[3H]-9-顺维甲酸与rxr活性维甲酸的竞争结合数据的比较.最终的放射性标记产物,[6,7-3H]-Lgd1069和3-[14C]-Lgd1069的特定活性分别为56 Ci/mmol和49 Mci/mmol.[6,7-3H]-Lgd1069的放射化学纯度为99.5%,而3-[14C]-Lgd1069的放射化学纯度为99.0%.3-[13Cd3]-Lgd1069的化学纯度为99.0%.与已知维甲酸进行的竞争结合研究显示,当使用[6,7-3H]-Lgd1069或[3H]-9-顺维甲酸作为放射性配体时,Kd值相似.
Doi:10.1002/jlcr.2580360712

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
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 disgnostic and therapeutic uses.

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.