专利号:US-2009318627-A1 优先权日:2006-02-07 标题:Solid phase synthesis of acridinium derivatives 发明人:NATRAJAN ANAND; SHARPE DAVID; COSTELLO JIM; JIANG QINGPING 权利人:SIEMENS HEALTHCARE DIAGNOSTICS 摘要:Acridinium-functionalized solid-phase supports and methods for making acridinium-functionalized solid-phase supports are disclosed. The acridinium-functionalized solid-phase supports comprise a solid phase support linked to a chemiluminescent substituted acridinium compound through a linker group covalently attached to the nitrogen atom of the acridinium nucleus and the solid phase support as exemplified in FIG. 1.
专利号:US-8912323-B2 优先权日:2009-10-30 标题 :Multifunctional small molecules 发明人:BAKER JR JAMES R; ZONG HONG; THOMAS THOMMEY P 权利人:BAKER JR JAMES R; ZONG HONG; THOMAS THOMMEY P; UNIV MICHIGAN 摘要:The present invention relates to dendrimer synthesis. Specifically, the present invention relates to triazine scaffolds capable of click chemistry for one-step synthesis of functionalized dendrimers, and methods of making and using the same.
专利号:US-9481678-B2 优先权日:2015-02-09 标题 :Substituted pyrrolo[2,3-D]dipyrimidines for selectively targeting tumor cells with FR-alpha and FR-beta type receptors 发明人:GANGJEE ALEEM; MATHERLY LARRY H 权利人:DUQUESNE UNIV OF THE HOLY GHOST; UNIV WAYNE STATE 摘要:Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.
专利号:US-12133900-B2 优先权日:2013-03-15 标 题:Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors 发明人:LOW PHILIP STEWART; KULARATNE SUMITH A; MAHALINGAM SAKKARAPALAYAM M 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds. The disclosure also relates to compositions for incorporating the compounds as used for the targeted imaging of tumors. Conjugation of the amino acid linking groups increase specificity and detection of the compound. Methods and compositions for use thereof in diagnostic imaging are contemplated.
专利号:US-2003181635-A1 优先权日:2002-03-22 标 题:Process for coupling amino acids to an antifolate scaffold 发明人:KOCHAT HARRY; WU YE 摘要:A synthetic process is disclosed for coupling amino acids to a substrate. The process involves dissolving the amino acid and the scaffold in a non-polar aprotic solvent, and agitating the resulting mixture for a predetermined time. The process is specially suited to the synthesis of antifolate compounds having useful applications in the medical fields of oncology, inflammatory diseases and others.
专利号:US-2011251138-A1 优先权日:2010-04-08 标题:Lipoic acid metabolite conjugate: preparation and their therapeutic effect 发明人:SEETHARAMA RAVIKUMAR KABYADI 权利人:SEETHARAMA RAVIKUMAR KABYADI 摘要:The present invention is a design and synthesis of a series of therapeutic conjugates which consists of tautomers of lipoic acid metabolites, with small molecule, vitamin, carbohydrates, peptides, chemotherapeutic agent wherein or not the conjugate possesses dual binding ability. The present invention can be used to therapeutics and diagnostics in vitro for cancer and other diseases associated with altered metabolic enzymes. The invention can also be used for the controlled release of more stable form of lipoic acid in its salt form with the minerals or vitamins.
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合成参考文献
参考文献:10.1016/0076-6879(80)66522-7 摘要:Scott JM. Preparation and purification of pteroic acid from pteroylglutamic acid (folic acid). Methods Enzymol. 1980;66():657–60. doi: 10.1016/0076-6879(80)66522-7. 参考文献:10.1007/s00259-006-0111-9 摘要:Müller C, Hohn A, Schubiger PA, Schibli R. Preclinical evaluation of novel organometallic 99mTc-folate and 99mTc-pteroate radiotracers for folate receptor-positive tumour targeting. European Journal of Nuclear Medicine and Molecular Imaging. 2006 Jun 09;33(9):1007–16. doi: 10.1007/s00259-006-0111-9.