专利号:US-6177564-B1 优先权日:1998-09-11 标题:Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one 发明人:NELSON TODD D; BHUPATHY MAHADEVAN 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula:This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-6046325-A 优先权日:1998-09-11 标 题:Chemical synthesis of 1,4-oxazin-2-ones 发明人:ASHWOOD MICHAEL STEWART; BISHOP BRIAN CHRISTOPHER; COTTRELL IAN FRANK 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R 1 is a C 1-6 alkyl or arylC 1-4 alkyl group; and R 2 is a hydrogen atom, a halogen atom, or a group selected from C 1-6 alkyl, CF 3 or C 1-6 alkoxy substituted by C 1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-2025084410-A1 优先权日:2015-01-12 标 题:Incorporation of unnatural nucleotides and methods thereof 发明人:PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E 权利人:SYNTHORX INC 摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.
专利号:US-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
1: Li YX, Yang JY, Alcantara M, Abelian G, Kulkarni A, Staubli U, Foster AC. Inhibitors of the Neutral Amino Acid Transporters ASCT1 and ASCT2 Are Effective in In Vivo Models of Schizophrenia and Visual Dysfunction. J Pharmacol Exp Ther. 2018 Nov;367(2):292-301. doi: 10.1124/jpet.118.251116. Epub 2018 Aug 31.
合成参考文献
参考文献:10.1007/s11244-022-01770-8 摘要:Batool I, Iqbal A, Imran M, Ramzan M, Anwar A. Design and Applications of Enzyme-Linked Nanostructured Materials for Efficient Bio-catalysis. Top Catal. 2023 Jan 03;66(9-12):649–75. doi: 10.1007/s11244-022-01770-8.