专利号:US-12076715-B1 优先权日:2021-04-15 标 题:Synthesis and characterization of air-stable iron-based catalysts for Suzuki-Miyaura cross-coupling reactions of alkyl halides and aryl boronic esters 发明人:WONG ALEXANDER; BYERS JEFFERY 权利人:THE TRUSTEES OF BOSTON COLLEGE 摘要:This disclosure relates to novel catalysts for Suzuki-Miyaura cross-coupling reactions, the use thereof, and the methods of making the same.
专利号:US-12319691-B2 优先权日:2020-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI 权利人:AMGEN INC; VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-12428442-B2 优先权日:2017-06-21 标题 :Compounds, compositions and methods for synthesis 发明人:BUTLER DAVID CHARLES DONNELL; HENCKEN CHRISTOPHER P; IWAMOTO NAOKI; KANDASAMY PACHAMUTHU; LANAO ALVARO ANDRES; LU GENLIANG; SHIMIZU MAMORU; DIVAKARAMENON SETHUMADHAVAN; VARGEESE CHANDRA; BOMMINENI GOPAL REDDY; MARAPPAN SUBRAMANIAN 权利人:WAVE LIFE SCIENCES LTD 摘要:The present disclosure, among other things, provides technologies for synthesis, including reagents and methods for stereoselective synthesis. In some embodiments, the present disclosure provides compounds useful as chiral auxiliaries. In some embodiments, the present disclosure provides reagents and methods for oligonucleotide synthesis. In some embodiments, the present disclosure provides reagents and methods for chirally controlled preparation of oligonucleotides. In some embodiments, technologies of the present disclosure are particularly useful for constructing challenging internucleotidic linkages, providing high yields and stereoselectivity.
专利号:WO-2023131254-A1 优先权日:2022-01-06 标 题 :Pseudouridine modified at n1 position and use thereof in mrna synthesis 发明人:LI SONG; GUO CHUANXIN; CAI XIAORU; QIAN QIJUN 权利人:MAXIRNA SHANGHAI PHARMACEUTICAL CO LTD; MAXIRNA ZHEJIANG TECH CO LTD 摘要:Provided in the present invention are a pseudouridine modified at an N1 position and the use thereof in mRNA synthesis. Specifically, the compound of the present invention comprises compounds represented by formula I and formula II, and the definition of each group in the formula is as described herein. The compound of the present invention can be used for preparing mRNA to reduce the autoimmunogenicity of the mRNA, improve the stability of the mRNA itself, and/or enhance the expression time and expression efficiency of the mRNA in a target cell.
专利号:US-2016319312-A1 优先权日:2013-07-29 标 题 :Synthesis method for l-cyclic alkyl amino acid and pharmaceutical composition having thereof 发明人:HONG HAO; ZHENG CHANGSHENG; GUO LINA 权利人:ASYMCHEM LABORATORIES (TIANJIN) CO LTD; ASYMCHEM LIFE SCIENCE (TIANJIN) CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LABORATORIES (FUXIN) CO LTD; JILIN ASYMCHEM LABORATORIES CO LTD 摘要:A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD + , and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is n n n n n n n n n n where n 1 ≧1, m 1 ≧0 and the M 1 is H or a monovalent cation; the Structural Formula (II) is n n n n n n n n n n where n 2 ≧0, m 2 ≧0, the M 2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.
专利号:US-2024335442-A1 优先权日:2021-08-02 标 题:N-acylhydrazone compounds capable of inhibiting nav1.7 and/or nav1.8, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits 发明人:BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; GAMBA LUIS EDUARDO REINA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA; LIMA LÃ?DIA MOREIRA 权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO UFRJ 摘要:N-acylhydrazone compounds that are Nav 1.7 and/or Nav 1.8 inhibitors, including N-acylhydrazone compounds of Formula (I), wherein the substituents R1 to R6 are independently selected from the groups defined in the specification, as well as to the processes for the preparation thereof, compositions comprising at least one of said compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits, and which are applicable in the fields of medicinal chemistry and organic synthesis, as well as in the treatment of pain-related disorders.
[参考文献]: Yi Liu, Et Al. Photodissociation Of Cyclobutyl Bromide At 234 Nm Studied Using Velocity Map Imaging. J Phys Chem A. 2006 Apr 27;110(16):5379-85. [参考文献]: Zhen Li, Et Al. Discovery Of Potent 3,5-Diphenyl-1,2,4-Oxadiazole Sphingosine-1-Phosphate-1 (S1P1) Receptor Agonists With Exceptional Selectivity Against S1P2 And S1P3. J Med Chem. 2005 Oct 6;48(20):6169-73.
合成参考文献
摘要:Kostikov, R.; Baird, M. S., Science of Synthesis, (2009) 48, 638. 摘要:Shi, L., Science of Synthesis: Knowledge Updates, (2024) 1, 13.