专利号:US-9115172-B2 优先权日:2007-01-11 标 题 :Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:D SOUZA CHRISTOPHER A; MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 18 F- or 19 F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18 F- or 19 F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.
专利号:US-7999090-B2 优先权日:2000-07-07 标 题:Fungal cell wall synthesis gene 发明人:TSUKAHARA KAPPEI; HATA KATSURA; SAGANE KOJI; NAKAMOTO KAZUTAKA; TSUCHIYA MAMIKO; WATANABE NAOAKI; OHBA FUMINORI; TSUKADA ITARU; UEDA NORIHIRO; TANAKA KEIGO; KAI JUNKO 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides isolated DNA encoding a GWT1 protein having activity to confer resistance of a fungus against a compound of formula Ia, and wherein a defect of a function of the GWT1 protein leads to a decrease in the amount of a glycosylphosphatidylinositol (GPI)-anchored protein in the cell wall of a fungus.
专利号:US-4746659-A 优先权日:1985-12-30 标题:Diastereomers of 10-alkyl-10-deazaminopterins and process for preparing the same 发明人:DEGRAW JOSEPH I; CHRISTIE PAMELA H; SIROTNAK FRANCIS M 权利人:STANFORD RES INST INT; SLOAN KETTERING INST CANCER 摘要:Diastereomers of 10-alkyl-10-deazaminopterins are provided, as well as a synthesis for their preparation as the individual d,L. and l,L.-diastereomers, the d,L-10-ethyl diastereomer being three times as potent against L1210 cells as the l,L-10-ethyl diastereomer, and the l,L-10-ethyl diastereomer being approximately one-half as toxic as the d,L-10-ethyl diastereomer.
专利号:CN-1472189-A 优先权日:2003-06-26 标 题 :Synthesis of trans-4-alkyl cyclohexyl formic acid
专利号:US-9175357-B2 优先权日:2011-02-04 标 题:Fragment ligated inhibitors selective for the polo box domain of PLK1 发明人:MCINNES CAMPBELL; FARAG DOAA BOSHRA 权利人:MCINNES CAMPBELL; FARAG DOAA BOSHRA; UNIV SOUTH CAROLINA 摘要:Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.