CAS: 182133-25-1; Arzoxifene

上下游产品

4'-Bromo-4'-Desmethoxyarzoxifene 943439-50-7
[6-Benzyloxy-3-[4-[2-(1-Piperidinyl)Ethoxy]Phenoxy]-2-(4-Methoxyphenyl)]-Benzo[b]Thiophene 182133-23-9
Diethyl-Carbamic Acid 2-(4-Methoxy-Phenyl)-3-[4-(2-Piperidin-1-Yl-Ethoxy)-Phenoxy]-Benzo[b]Thiophen-6-Yl Ester

📜3-甲氧基苯硫酚置于copper(L) Iodide,乙酸乙酯 盐酸,氢氧化钾,双氧水,Sodium Hydride,三氟乙酸,N-溴代乙酰胺体系中,用 甲醇,乙醚,乙醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 33.83H,反应生成阿佐昔芬
参考文献:具有调节的氧化活性和受体亲和力的苯并噻吩选择性雌激素受体调节剂.
标题:具有调节的氧化活性和受体亲和力的苯并噻吩选择性雌激素受体调节剂.
摘要:选择性雌激素受体调节剂(serm)的雌激素和抗雌激素作用的调节被认为是其临床应用的基础.大多数serm是易氧化为醌的氧化代谢的聚芳族苯酚,被认为具有遗传毒性.相反,Serms的氧化还原反应性可能有助于抗氧化剂和化学预防机制,为改善serms的治疗性能提供了一种新方法.开发了改进的合成策略以产生苯并噻吩serm家族.使用计算建模方法和抗氧化剂活性和雌激素受体(er)配体结合的测量结果,表明该serm家族既可提供1.2-67倍的eralpha / Erbeta选择性,又可提供一定范围的氧化还原活性.通过改变远离oh基团的取代基可以成功地调节抗氧化活性.抗氧化能力的来源.报道了一种有效的合成方法,该方法产生了苯并噻吩serm,其中氧化还原活性和er亲和力得到调节.
Doi:10.1021/jm070079J

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-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-8828984-B2
优先权日:2012-11-19
标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
发明人：CHE CHI MING; ZOU TAOTAO
权利人:UNIV HONG KONG; UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

专利号:US-10577387-B1
优先权日:2018-08-09
标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
发明人：CHE CHI MING; Fung Sin Ki; Chen tian feng
权利人:UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-11286271-B2
优先权日:2018-07-31
标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
发明人：CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
权利人:UNIV HONG KONG
摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.