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:US-11555047-B2 优先权日:2019-10-31 标题:One-step synthesis of phosphate-based inhibitors and applications thereof 发明人:D'ANTONIO EDWARD; PIERCE JOSHUA 权利人:UNIV SOUTH CAROLINA; UNIV NORTH CAROLINA STATE 摘要:One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such as T. cruzi ribose 5-phosphate isomerase type B and D-ribulose-5-phosphate 3-epimerase enzymes. Methods can be used in forming pharmaceutical compositions for use in treatment of disease caused by kinetoplastid parasites including T. cruzi, T. brucei, and Leishmania spp.
专利号:US-5843682-A 优先权日:1995-11-20 标题 :N-1-carboxyalkyl derivatives of LSD 发明人:SIGLER GERALD F; ROUHANI RIAZ; DAVOUDZAHEH DAVID 权利人:BOEHRINGER MANNHEIM CORP 摘要:Novel derivatives of LSD having the formula wherein R1 is an alkyl, cycloalkyl or aryl group having 1 to 10 carbon atoms, preferably an alkyl group having 1 carbon atom; R2 is a bond or wherein R3 is alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms, preferably an alkyl group having 2 or 5 carbon atoms; Z is an immunogenic carrier substance, an enzyme donor polypeptide or a label selected from the group consisting of an enzyme, a substance having fluorescent or luminescent properties and a radioactive substance; and n is 1 to p where p equals MW of Z/1000. The derivatives include maleimide conjugates of an immunogenic poly(amino acid), an enzyme donor polypeptide or a labeling substance such as an enzyme, a fluorescent substance or a radioactive substance. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and their conjugate derivatives are also disclosed.
专利号:US-5525474-A 优先权日:1994-01-31 标 题 :Piperidine analogs and conjugates of procainamide and NAPA 发明人:SIGLER GERALD F; WALTER CHARLES F; GLANCY TODD; HUBER ERASMUS; KLEIN FRANK E 权利人:BOEHRINGER MANNHEIM CORP 摘要:Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: wherein: X=hydrogen or acetyl; n=1 to p where p=MW of Z/1000; Z=a poly(amino acid) or polysaccharide; and R3=a bond or aving 2 to 10 carbon atoms. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.
专利号:US-5439798-A 优先权日:1993-12-17 标 题:Maleimide adduct conjugates of procainamide and NAPA 发明人:SIGLER GERALD F; WALTER CHARLES F; DURANT CHARLES E; GLANCY TODD; KLEIN FRANK E; DORN ALLAN R 权利人:BOEHRINGER MANNHEIM CORP 摘要:Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: +TR wherein: X=hydrogen or acetyl; R1=an alkyl group having 1 to 3 carbon atoms; m=an integer from 2 to 10; R2=an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms; Z=a poly(amino acid); and n=1 to p where p=MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.
专利号:US-2005250765-A1 优先权日:2000-08-16 标题 :Diazepinones as antiviral agents 发明人:CHO HIDETSURA; GOGLIOTTI ROCCO D; HAMILTON HARRIET W; KRASUTSKY ALEXEI; NAKAMURA TAKESHI; TADA HIROKI; WEBER PETER C 权利人:CHO HIDETSURA; GOGLIOTTI ROCCO D; HAMILTON HARRIET W; KRASUTSKY ALEXEI; NAKAMURA TAKESHI; TADA HIROKI; WEBER PETER C 摘要:The invention is novel compounds of formula n nwhich exhibit an improved therapeutic index and improved metabolic stability which are useful in the treatment and/or prevention of herpes viral infections. Novel intermediates useful in the synthesis of the final compounds are also part of the invention.
1: Sicard, C., Shek, N., White, D., et al. A rapid and sensitive fluorimetric β-galactosidase assay for coliform detection using chlorophenol red-β-ᴅ-galactopyranoside. Anal. Bioanal. Chem. 406(22), 5395-5403 (2014). 2: Jendresen, C., Daws, M.R., and Nilsson, L.N.G. An improved CPRG colorimetric ligand-receptor signal transduction assay based on beta-galactosidase activity in mammalian BWZ-reporter cells. J. Pharmacol. Toxicol. Methods 90, 67-75 (2018).
合成参考文献
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