专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-6348616-B1 优先权日:1996-07-26 标题 :Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of the formula:is particularly effective in the treatment of HIV.
专利号:WO-2015058868-A1 优先权日:2013-10-25 标题 :Compositions and methods for the treatment of cancer 发明人:JIMENO DOÑAQUE JOSÉ Mª 权利人:PANGAEA BIOTECH S L 摘要:The invention relates to anti-tumor compounds which have been designed to functionally disrupt the cross-talk between AEG-1 and the p65 subunit of NF-κB. Therefore, the invention relates to methods and compositions for the treatment of cancer using the compounds identified in the present invention, as well as compositions adequate for sustained release of the compounds of the invention to be administered to the surgical site after resection of the tumor. The invention also provides methods for the synthesis of the compounds of the invention.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-8846898-B2 优先权日:2000-10-17 标题:Phosphinoamidite carboxylates and analogs thereof in the synthesis of oligonucleotide having reduced internucleotide charge 发明人:DELLINGER DOUGLAS J 权利人:DELLINGER DOUGLAS J; Lieure Cornu LLC 摘要:Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) n nwherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH 2 , azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R 11 and R 12 is a blocking group and the other is (IV) or (VI)n n nin which W, X, Y, Z, R 1 and n are as defined herein.
专利号:WO-2024163852-A1 优先权日:2023-02-03 标题:Histidine kinase inhibitors as antibacterial agents 发明人:CARLSON ERIN ELIZABETH; GOSWAMI MANIBARSHA; ESPINASSE ADELINE; JI YINDUO 权利人:UNIV MINNESOTA 摘要:The invention provides maleimide derivative compounds of Formula I, as histidine kinase inhibitors, useful for inhibiting bacterial histidine kinases, such as HK853 and AirS, for treating S. aureus bacterial infections, in particular methicillin-resistant S. aureus (MRSA). The invention further provides methods of treating bacterial infection with the. compounds of Formula I, either used alone or in combination with other agents in a therapeutic regimen. Further disclosed is the synthesis of the compounds of Formula I.
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合成参考文献
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