专利号:US-8569452-B2 优先权日:2011-02-17 标题:Preparation of phalloidin and its derivatives 发明人:LIU BAOSHENG; ZHANG JIANHENG 权利人:LIU BAOSHENG; ZHANG JIANHENG; AMERICAN PEPTIDE COMPANY INC 摘要:The present invention relates to novel phalloidin derivatives and their fluorescent dye conjugates. These new compounds may be used in studies of actin dynamics in living systems. The present invention also relates to methods for preparing such compounds. The synthesis routes combine solid-phase and solution phase peptide synthesis, and has great advantage for efficient preparation of a diverse library of the phalloidin derivatives, especially for the synthesis of phalloidin.
专利号:US-2024287128-A1 优先权日:2020-11-17 标题:Extremely fast solid phase synthesis 发明人:GILON CHAIM; HUREVICH MATTAN; BENTOLILA MOSHE; ALSHANSKI ISRAEL; NAOUM JOHNNY 权利人:YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTD 摘要:The present disclosure generally relates to the field of solid phase synthesis and methods for synthesizing peptides and employing solid phase synthesis.
专利号:WO-2005102340-A1 优先权日:2003-05-30 标题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:JP-2008506633-A 优先权日:2004-04-22 标题 :Convergent synthesis of kahalalide compounds
专利号:US-6090912-A 优先权日:1993-05-27 标 题:Topologically segregated, encoded solid phase libraries comprising linkers having an enzymatically susceptible bond 发明人:LEBL MICHAL; LAM KIT S; SALMON SYDNEY E; KRCHNAK VICTOR; SEPETOV NIKOLAI; KOCIS PETER 权利人:SELECTIDE CORP 摘要:The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports. In particular, the invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. Each of the solid phase synthesis support beads contains a single type of synthetic test compound. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.
专利号:US-5840485-A 优先权日:1993-05-27 标题 :Topologically segregated, encoded solid phase libraries 发明人:LEBL MICHAL; LAM KIT S; SALMON SYDNEY E; KRCHNAK VICTOR; SEPETOV NIKOLAI; KOCIS PETER 权利人:SELECTIDE CORP 摘要:The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.
1: Wender, P.A., Rothbard, J.B., Jessop, T.C., et al. Oligocarbamate molecular transporters: Design, synthesis, and biological evaluation of a new class of transporters for drug delivery. J. Am. Chem. Soc. 124(45), 13382-13383 (2002). 2: Kumar, J., Yellepeddi, V.K., Davies, G.E., et al. Enhanced gene transfection efficiency by polyamidoamine (PAMAM) dendrimers modified with ornithine residues. Int. J. Pharm. 392(1-2), 294-303 (2010).
合成参考文献
参考文献:10.1055/s-0041-1737497 摘要:N-Propyl-1H-pyrazole-1-carboximidamide for the Synthesis of N ω-Propylarginine-Containing Dipeptides. Synfacts. 2021 Dec 17;18(01):0109. doi: 10.1055/s-0041-1737497.