专利号:US-6177409-B1 优先权日:1996-07-05 标 题 :Method for the site specific synthesis of novel 3-hydroxypyridin-4(1H)ons derivatives from aminomonosaccharides or aminoitols, products obtained by this method and their applications 发明人:VANLEMMENS PIERRE PAUL; POSTEL DENIS GHISLAIN; GERMAIN PIERIG EMMANUEL; JULIEN RENE JEAN-MARIE; PETIT JEAN-PIERRE CONSTANT; RONCO GINO LINO; VILLA PIERRE JOSEPH 权利人:INST BIOCHIMICO PAVESE PHARMA 摘要:Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula:in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue. It also regards the products obtained by this process, as well as their applications, namely as medicaments for the treatment of toxic overloads of FeIII.
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-2012095058-A1 优先权日:2003-12-03 标 题 :Method of preventing survival of retrovirally cells and of inhibiting formation of infectious retroviruses 发明人:HANAUSKE-ABEL H M; PALUMBO PAUL; CRACCHIOLO B M; PARK MYUNG-HEE; WOLFF EDITH; HANAUSKE AXEL-RAINER; MATHEWS MICHAEL B; SAXENA DEEPTI; HOQUE MAINUL 权利人:HANAUSKE-ABEL H M; PALUMBO PAUL; CRACCHIOLO B M; PARK MYUNG-HEE; WOLFF EDITH; HANAUSKE AXEL-RAINER; MATHEWS MICHAEL B; SAXENA DEEPTI; HOQUE MAINUL 摘要:The present invention discloses compounds and pharmaceutical compositions which are highly effective at inhibiting the accumulation of spliced and unspliced viral transcripts and their utilization for viral protein synthesis at cellular ribosomes, and at inhibiting the formation of the hypusine residue in cellular eIF-5A precursor proteins, the cellular cofactors that render spliced and unspliced viral transcripts translatable at the ribosomes of infectled cells. The invention further relates to methods of using such compounds and pharmaceutical compositions therefrom for inhibiting or preventing viral protein synthesis. Such inhibition cause a dose-dependent release from the virally induced arrest of the otherwise genetically preprogrammed apoptosis of virally infected cells, and in consequence, triggers their apoptotic ablation and the eradication of the chronic infection-mediating provirus integrated into their genome.
专利号:US-9382462-B2 优先权日:2013-03-15 标 题:Metal ligand-containing prepolymers, methods of synthesis, and compositions thereof 发明人:RAO CHANDRA; DENG JUN; LIN RENHE 权利人:PRC DESOTO INT INC 摘要:Metal ligand-containing prepolymers, compositions containing metal ligand-containing prepolymers, methods of synthesizing metal ligand-containing prepolymers and the use of metal ligand-containing prepolymers in aerospace sealant applications are disclosed. The metal ligand-containing prepolymers have metal ligands incorporated into the backbone of the prepolymer. Cured sealant compositions comprising the metal ligand-containing prepolymers exhibit enhanced properties suitable for aerospace sealant applications.
专利号:WO-9801458-A1 优先权日:1996-07-05 标 题:Method for the site specific synthesis of novel 3-hydroxypyridin-4(1h)-ons derivatives from aminomonosaccharides or aminoitols, products obtained by this method and their applications
专利号:EP-1021457-B1 优先权日:1996-07-05 标题 :Method for the site specific synthesis of novel 3-hydroxypyridin-4(1h)-ones derivatives from aminoitols, products obtained by this method and their applications
参考文献:10.1007/s10637-019-00809-0 摘要:Kyriakou S, Mitsiogianni M, Mantso T, Cheung W, Todryk S, Veuger S, Pappa A, Tetard D, Panayiotidis MI. Anticancer activity of a novel methylated analogue of L-mimosine against an in vitro model of human malignant melanoma. Investigational New Drugs. 2019 Jun 26;38(3):621–33. doi: 10.1007/s10637-019-00809-0. 参考文献:10.1021/jm00030a005 摘要:el-Jammal A, Howell PL, Turner MA, Li N, Templeton DM. Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies. J Med Chem. 1994 Feb 18;37(4):461–6. doi: 10.1021/jm00030a005.