N-甲基咪唑置于sodium Dihydrogenphosphate,二异丙胺体系中,用 四氢呋喃,水,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,以53%的收率获得1-甲基-1H-咪唑-2-甲醛 参考文献:Pyruvamide Compounds As Inhibitors Of Dust Mite Group 1 Peptidase Allergen And Their Use 标题:Pyruvamide Compounds As Inhibitors Of Dust Mite Group 1 Peptidase Allergen And Their Use 摘要:本发明一般涉及治疗化合物领域,更具体地涉及某些丙酮酰胺化合物的公式(x)(为方便起见,以下统称为"pva化合物"),该化合物在某些情况下抑制尘螨1组蛋白酶过敏原(例如der P 1,Der F 1,Eur M 1).本发明还涉及包含这种化合物的药物组合物,以及在体外和体内使用这种化合物和组合物来抑制尘螨1组蛋白酶过敏原,并用于治疗由尘螨1组蛋白酶过敏原介导的疾病和疾病,通过抑制尘螨1组蛋白酶过敏原而得到缓解的疾病和疾病;哮喘;鼻炎;过敏性结膜炎;特应性皮炎;由尘螨引发的过敏症状;由尘螨1组蛋白酶过敏原引发的过敏症状;以及犬类特应性.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-2006051291-A1 优先权日:2004-09-07 标题 :Synthesis of radiolabeled sugar metal complexes 发明人:ADAM MICHAEL J; FISHER CARA L; BAYLY SIMON R; ORVIG CHRISTOPHER; LIM NATHANIEL C; STORR TIMOTHY J; EWART CHARLES B 权利人:ADAM MICHAEL J; FISHER CARA L; BAYLY SIMON R; ORVIG CHRISTOPHER; LIM NATHANIEL C; STORR TIMOTHY J; EWART CHARLES B 摘要:The invention provides a method for manufacturing or preparing neutral, low molecular weight 99m Tc-labeled and 186 Re-labeled carbohydrate complexes with an improved radiochemical yield from a simple functionalized sugar, such as glucosamine. In particular the synthesis relies on single ligand transfer (SLT) or double ligand transfer (DLT) reactions for converting a ferrocene compound into a rhenium or technetium tricarbonyl complex. The ferrocene compound may be linked to a sugar through various functional groups including, for example, thio, amino and alcohol functionalities to provide a wide range of radiolabeled sugar complexes that include both water soluble and relatively water insoluble compounds.
专利号:US-7067622-B2 优先权日:2001-06-25 标题 :Method of the solid phase synthesis of pyrrole-imidazole polyamide 发明人:SUGIYAMA HIROSHI; IIDA HIROKAZU; SAITO ISAO; SAITO TAKASHI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.
专利号:US-8143423-B2 优先权日:2007-03-22 标 题 :N-heterocyclic carbene (NHC) catalyzed synthesis of hydroxamic acids 发明人:ZHANG YUGEN; YING JACKIE Y; SEAYAD JAYASREE; WONG FONG TIAN; PATRA PRANAB K 权利人:ZHANG YUGEN; YING JACKIE Y; SEAYAD JAYASREE; WONG FONG TIAN; PATRA PRANAB K; AGENCY SCIENCE TECH & RES 摘要:A process for preparing hydroxamic acids is provided. The process comprises reacting an aldehyde with a nitroso compound in the presence of a N-heterocyclic carbene (NHC) catalyst.
专利号:WO-2008115153-A1 优先权日:2007-03-22 标题:N-heterocyclic carbene (nhc) catalyzed synthesis of hydroxamic acids
专利号:US-10106572-B1 优先权日:2014-07-03 标 题:Supramolecular hacky sacks (SHS), method of synthesis and applications thereof 发明人:RIVERA JOSE M; NEGRON LUIS M 权利人:RIVERA JOSE M; NEGRON LUIS M; UNIV PUERTO RICO 摘要:The invention is directed to small molecules that self-assemble hierarchically to form NPs termed SHS (due to their architectural features). These SHS are composed by precise supramolecules known as Supramolecular G-Quadruplexes (SGQs) which are formed when amphiphilic guanosine (G) derivatives that self-assemble in presence of salt by non-covalent interactions. The resulting SGQs are made of amphiphilic guanosine (G) subunits (with precisely eight subunits at neutral pH (pH>5.7) or sixteen subunits at acidic pH (pH<5.7)). The SGQs are responsive entities that further self-assemble upon an external stimulus, such as an increase in temperature or a change in pH, leading to the formation of the aforementioned SHS.