专利号:WO-9000622-A1 优先权日:1988-07-08 标题 :Oligonucleotide hybridization probes and means for the synthesis of the most preferred probes 发明人:KWIATKOWSKI MAREK; SUND CHRISTIAN; HURSKAINEN PERTTI 权利人:WALLAC OY; PHARMACIA AB 摘要:Oligonucleotide probe labeled at one of its teminal positions with a non-linear branched polymer carrying a plurality of negatively charged groups, preferably phosphodiester groups, and optionally also analytically indicatable groups covalently linked to terminal ends of the branches of said polymer. The preferred indicatable groups are lanthanide chelates. A compound that can be used for the synthesis of the probe is also disclosed. The compound has formula (I), where R1 and R2 are lower alkyl; R3 is lower alkyl (C1-C7), or aryl each of which optionally being provided with electron-withdrawing substituents; and A1, A2 and A3 are hydrogen, A'-O-B, A''-O-B or A'''-O-B, at most one of A1-3 being hydrogen and A', A'' and A''' being a hydrocarbon chain providing a distance of 5-9 atoms between the phosphorous atom and the oxygen directly bound to B, and B being a protecting group. In the preferred compound at least two of A1-3 are identical while the other is hydrogen.
专利号:US-8975427-B2 优先权日:2010-04-28 标题 :Synthesis of alkyl cyclopentadiene compounds 发明人:HARLAN C JEFF; CAO XIANYI; RIX FRANCIS C 权利人:HARLAN C JEFF; CAO XIANYI; RIX FRANCIS C; UNIVATION TECH LLC 摘要:A method of synthesizing an alkyl cyclopentadiene compound is disclosed. The method includes contacting at least one cyclopentadienyl anion source and at least one alkyl group source to form at least one alkyl cyclopentadiene compound. The method further includes extracting the alkyl cyclopentadiene compound with a hydrocarbon solvent. The alkyl cyclopentadiene compound may be converted to a metallocene catalyst compound.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-5936128-A 优先权日:1993-11-19 标题:5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND LEE; LUNNEY ELIZABETH; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
专利号:US-2024175005-A1 优先权日:2021-03-31 标题 :PURIFICATION AND RECYCLING OF mRNA NUCLEOTIDE CAPS 发明人:BEAUDOIN JENNIFER; DIETER LANCE; VIK KAELYN 权利人:MODERNATX INC 摘要:This disclosure relates to purification and recycling nucleotide messenger RNA (mRNA) caps from the preparation of mRNA, which comprises isolating and purifying excess nucleotide mRNA caps from mRNA synthesis.
专利号:US-5510375-A 优先权日:1993-11-19 标 题 :Coumarin derivatives as protease inhibitors and antiviral agents 发明人:DOMAGALA JOHN M; HAGEN SUSAN E; LUNNEY ELIZABETH; TAIT BRADLEY D 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.
[参考文献]: Son T Nguyen, Et Al. Structure-Activity Relationships Of A Novel Pyranopyridine Series Of Gram-Negative Bacterial Efflux Pump Inhibitors. Bioorg Med Chem. 2015 May 1;23(9):2024-34.
合成参考文献
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