CAS: 118-42-3; 2-((4-((7-Chloroquinolin-4-yl)Amino)Pentyl)(Ethyl)Amino)Ethanol

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CAS号86-98-6 4,7-二氯喹啉

📜硫酸羟基氯喹置于氨体系中,用 氯仿 用作溶剂,化学反应 1.0H,以90%的收率获得硫酸羟氯喹
参考文献:羟基氯喹双作用前药与芳基乙酸nsaid的新型药物递送:设计,动力学和药理研究.
标题:羟基氯喹双作用前药与芳基乙酸nsaid的新型药物递送:设计,动力学和药理研究.
摘要:类风湿关节炎(ra)是一种慢性自身免疫性疾病,其特征是手,脚,肘,膝盖和颈部的关节活动受限,但主要是滑膜关节.尽管病因病理学尚不完全清楚,但治疗范式正在发展以提供对症状和疾病进展的更严格控制.当前的趋势是在早期阶段引入疾病改良抗类风湿药(dmard).羟氯喹(hcq)和非甾体抗炎药(nsaids)是广泛用于ra治疗的两种机制上不同的机制,其中前者可阻止疾病进展,而后者可缓解症状.目前的工作旨在通过设计互酯前药来最大程度地减少非目标部位hcq的缓慢发作和积累以及对nsaid局部胃不耐受的问题.1 H-NMR,13C-NMR,质谱和元素分析.前药在胃的酸性环境中抵抗水解,但在小肠中显示出明显的释放.给大鼠口服前药后,在8.5-10 H的血液中可回收40.5-49%hcq和53.4-66.8%的nsaid.在24小时内收集的尿液和粪便样品分别显示hcq的2.3-3.5%和0.75-0.9%,而没
Doi:10.1007/s13346-017-0420-5

专利信息

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-11672829-B2
优先权日:2015-09-10
标 题:Genetically engineered coronavirus-specific effector cells for in situ synthesis of antiviral proteins
发明人：BHATNAGAR PARIJAT; SSEMADAALI MARVIN A
权利人:STANFORD RES INST INT
摘要:An example genetically engineered effector cell comprises an exogenous polynucleotide sequence that includes a receptor element, an actuator element, and an effector element. The receptor element encodes a chimeric antigen receptor (CAR) comprising an extracellular antigen binding domain operably linked to a transmembrane domain, and an intracellular signaling domain, wherein the extracellular antigen binding domain recognizes an antigen on a surface of a Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2)-infected cell. The actuator element encodes a transcription factor binding site that upregulates synthesis of an antiviral protein. The effector element encodes the antiviral protein operably linked to a signal peptide, wherein, in response to the antigen binding domain of the CAR binding to the antigen of SARS-CoV-2-infected cell, the engineered effector cell is configured to activate and, to synthesize and secrete the antiviral protein.

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.