专利号:US-5665598-A 优先权日:1994-04-13 标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent 发明人:ABOOD NORMAN A; NOSAL ROGER A 权利人:SEARLE & CO 摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.
专利号:US-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
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-2025282825-A1 优先权日:2020-11-20 标 题 :Novel cyclic compounds, method for their preparation and the use of said cyclic compounds in cosmetic preparations 发明人:WIRTZ SEBASTIAN N; GROND STEPHANIE; SAUR JULIAN S; KRISMER BERNHARD; HEUER ANDREA; HUEPEDEN JENNIFER 权利人:UNIV EBERHARD KARLS TUEBINGEN 摘要:The present invention relates to novel cyclic compounds; a method for the solid phase synthesis of said novel cyclic compounds; novel thiazolidine and oxazolidine building blocks that can be directly incorporated into the solid phase synthesis of said novel cyclic compounds, and a novel method for the synthesis of said thiazolidine and oxazolidine building blocks; and cosmetic compositions containing said novel cyclic compounds.
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.
摘要:Hall, M.; Faber, K.; Tasnádi, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 305. 摘要:Agrahari, A. K.; Mishra, A.; Tiwari, V. K., Science of Synthesis, (2021) , 136.