专利号:US-2023248849-A1 优先权日:2020-07-27 标 题:Contrast agents for detection of enzyme activities based on melanin synthesis 发明人:PAGEL MARK D 权利人:UNIV TEXAS 摘要:We disclose a composition, comprising a compound, comprising a melanin precursor that spontaneously synthesizes a melanin when in free form in vivo, and a peptide directly covalently bonded to or indirectly linked to the melanin precursor, wherein the direct covalent bond or indirect link of the peptide to the melanin precursor blocks spontaneous synthesis of the melanin in vivo in the absence of protease activity. We also disclose methods of tumor imaging, tumor detection, diagnosis, and treatment, including methods comprising administering, to a patient suffering from a tumor, the composition; and either surgically resecting the tumor or thermally ablating the tumor, wherein the surgical resection is guided at least in part by contrast imparted by, or the thermally ablating targets cells containing, the melanin, wherein the melanin is spontaneously synthesized in the tumor after administering the composition.
专利号:US-2013004979-A1 优先权日:2010-06-11 标 题 :Glycosyltransferase reversibility for sugar nucleotide synthesis and microscale scanning 发明人:THORSON JON S; GANTT RICHARD W; PELTIER-PAIN PAULINE MARIE JEANNE 权利人:WISCONSIN ALUMNI RES FOUND; THORSON JON S; GANTT RICHARD W; PELTIER-PAIN PAULINE MARIE JEANNE 摘要:The present invention generally relates to materials and methods for exploiting glycosyltransferase reversibility for nucleotide diphosphate (NDP) sugar synthesis. The present invention provides engineered glycosyltransferase enzymes characterized by improved reaction reversibility and expanded sugar donor specificity as compared to corresponding non-mutated glycosyltransferase enzymes. Such reagents provide advantageous routes to NDP sugars for subsequent use in a variety of biomedical applications, including enzymatic and chemo-enzymatic glycorandomization.
专利号:US-8372380-B2 优先权日:2007-03-30 标 题:In vivo imaging of sulfotransferases 发明人:BARRIO JORGE R; KEPE VLADIMIR; SMALL GARY W; SATYAMURTHY NAGICHETTIAR 权利人:UNIV CALIFORNIA; BARRIO JORGE R; KEPE VLADIMIR; SMALL GARY W; SATYAMURTHY NAGICHETTIAR 摘要:Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18 F, 123 I, 124 I, 125 I, or 11 C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.
专利号:US-5756834-A 优先权日:1995-11-11 标 题:Process for preparing fluorinated aromatics 发明人:PASENOK SERGEJ; APPEL WOLFGANG 权利人:HOECHST AG 摘要:It is known to prepare fluorinated aromatic compounds of the formula I in which X, Y and Z can have the meaning specified in the description, by reacting aromatic compounds of the formula II in which X, Y and Z have the meaning specified for formula I, with fluorine in a reaction medium. According to the invention, the direct fluorination is carried out in a reaction medium containing polyfluoroalkanesulfonic acids of the formula IIICFnH3-n(CFY)m-SO3H(III)in which m, n and Y have the meaning specified in the description. By this means, it is possible, particularly advantageously to provide a process, which improves the known processes not only with regard to the selectivity and the yield, but also with respect to the quality of the resulting products of the process in a manner not readily predictable. Fluorinated aromatic compounds of the formula I as intermediates for active compound synthesis.
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合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 240. 参考文献:10.1016/j.mri.2006.04.003 摘要:Kodibagkar VD, Yu J, Liu L, Hetherington HP, Mason RP. Imaging beta-galactosidase activity using 19F chemical shift imaging of LacZ gene-reporter molecule 2-fluoro-4-nitrophenol-beta-D-galactopyranoside. Magn Reson Imaging. 2006 Sep;24(7):959–62. doi: 10.1016/j.mri.2006.04.003.