L-色氨酸置于甲醇,氯化亚砜体系中,化学反应生成 L-色氨酸甲酯盐酸盐 参考文献: Spiro Compound,And Preparation Method Therefor And Use Thereof[fr] Composé Spiro,Son Procédé De Préparation Et Son Utilisation[zh] 一种螺环化合物及其制备方法与应用 标题: Spiro Compound,And Preparation Method Therefor And Use Thereof[fr] Composé Spiro,Son Procédé De Préparation Et Son Utilisation[zh] 一种螺环化合物及其制备方法与应用 摘要:本申请属于化学药物技术领域,涉及一种通式(I)所示的螺环化合物,或其异构体,或其消旋体,或其可药用的盐,作为一种3C样蛋白酶抑制剂以及使用其治疗多种特定疾病或病状的方法.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-9353112-B2 优先权日:2012-03-07 标 题 :Synthesis of polycyclic alkaloids 发明人:GOFF DANE; PAYAN DONALD G; BRASELMANN SYLVIA 权利人:RIGEL PHARMACEUTICALS INC 摘要:Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
专利号:US-2023220381-A1 优先权日:2020-06-30 标 题 :Dna-encoded functionalized aptamers 发明人:SLEIMAN HANADI; LACROIX DE VIMEUR DE ROCHAME DONATIEN PHILIPPE MARIE; MCKEAGUE MAUREEN; HIRKA SERHII; SALIBA DANIEL; ANDERSON SHAUN IAN 权利人:THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIV 摘要:It is provided the synthesis of an aptamer-like encoded oligomer (ALEnOmer), method of producing same and method of preparing a library of ALEnOmes. More particularly, the method of preparing ALEnOmer comprises coupling at least one phosphoramidite monomer with an orthogonal protecting group, and the ALEnOmer produces comprises a DNA coding strand covalently attached to an oligomer through a branching unit, wherein the oligomer has a degree of polymerization at least 5 and is an aptamer.
专利号:US-8703951-B2 优先权日:2011-07-15 标 题 :Synthesis of 4H-benzo[D]pyrrolo[1,2-A]thiazoles and indolizino[6,7-b]indole derivatives and their use as antitumor therapeutic agents 发明人:SU TSANN-LONG; CHOU TING-CHAO; LEE TE-CHANG 权利人:SU TSANN-LONG; CHOU TING-CHAO; LEE TE-CHANG; ACADEMIA SINICA 摘要:The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.
专利号:US-9422321-B2 优先权日:2010-09-07 标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments 发明人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE 权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU 摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
专利号:US-6495693-B2 优先权日:1996-11-22 标题:N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; PORTER WARREN J; THORSETT EUGENE D; WU JING 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 70.