专利号:US-2025282813-A1 优先权日:2021-04-09 标 题 :Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates 发明人:OKADA YOHEI; SUZUKI HIDEAKI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:A novel pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates are provided. The pseudo solid phase protecting group is represented by formula II wherein: * indicates the point of attachment to an oxygen atom of a hydroxyl moiety of the nucleoside, the nucleotide, the oligonucleotide, or of the conjugate of a nucleoside, a nucleotide or an oligonucleotide to be protected; c is 0 or 1; a is an integer of 1 to 12; R3 is H; R5 is O—R6 or H, where R6 is a C8-C40 aliphatic hydrocarbon group; each of R4 is independently O—R6, where R6 is at each occurrence independently a C8-C40 aliphatic hydrocarbon group; b is 1 to 3; with the proviso that if b is 1, at least one of R3 and R5 is not H; and with the further proviso that the sum of all carbon atoms contained in the R3, R4, and R5 moieties present is larger than 23 and smaller than 200.
专利号:WO-9600391-A1 优先权日:1994-06-23 标题:Methods for the synthesis of diketopiperazines 发明人:CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN 权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN 摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.
专利号:US-4212795-A 优先权日:1978-11-13 标题:Cyclization of peptides 发明人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing two cysteine moieties, each of which is protected by an n-alkylthio group, or when one of such moieties is in an amino terminal position, this one moiety may be protected by a cysteine group while the other is protected by an n-alkylthio group, and placing such intermediate peptide in a solution substantially free of oxygen and preferably at a pH of from 5 to 10 until rearrangement has taken place, to yield a cyclic disulfide peptide. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:US-4033940-A 优先权日:1975-11-12 标 题:Cyclization of peptides 发明人:HUGHES JOHN L; SEYLER JAY K; LIU ROBERT C 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing an amino terminal cystine residue and a cysteine residue located in a position within the amino acid sequence, to give a desired peptide, and placing such intermediate peptide in a solution substantially free of oxygen at a pH of from about 5 to 10 until rearrangement takes place to yield a cyclic disulfide peptide and to displace a molecule of cysteine from the amino terminal cysteine residue. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:WO-2022214692-A1 优先权日:2021-04-09 标题 :Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates
专利号:CN-114957258-A 优先权日:2021-02-25 标题 :Synthesis of a broad-spectrum serine β-lactamase inhibitor based on carbapenem structure and its application in the inhibition of drug-resistant bacteria