CAS: 517905-93-0; (R)-3-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-(2-Nitrophenyl)Propanoic Acid

该化合物是一种合成化合物,具有以氟氧基碳基(Fmoc)保护群体为特征的复杂结构,通常用于peptide合成以保护氨基组.该化合物含有一个硝基化合物,因其电子提取特性而闻名,影响分子的再活性和极性.丙酸运动的存在表明,该化合物具有酸性,可以与各种化学反应和生物相互作用有关.(R)指出,该化合物具有特定的空间安排,可影响其生物活动和与其他分子的相互作用.

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合成工艺路线路线简述

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    专利号:US-8147799-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:MCBRIDE WILLIAM J; GOLDENBERG DAVID M
    权利人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M; IMMUNOMEDICS INC
    摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.

    专利号:US-8153100-B2
    优先权日:2007-01-11
    标题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
    发明人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
    权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; 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 or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18 F- or 19 F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18 F or 19 F bound to the metal. 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 18 F or 19 F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.

    专利号:US-8147800-B2
    优先权日:2007-01-11
    标 题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
    发明人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
    权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC
    摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.

    专利号:US-8343460-B2
    优先权日:2007-01-11
    标题:Methods and compositions for F-18 labeling of proteins, peptides and molecules
    发明人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M
    权利人:IMMUNOMEDICS INC; MCBRIDE WILLIAM J; GOLDENBERG DAVID M
    摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use in PET imaging. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules may be labeled and utilized. Preferably, the F-18 is attached to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. In other embodiments, the metal may first be attached to the chelating group and subsequently the F-18 bound to the metal. More preferably, the F-18 label moiety may be attached to a targetable conjugate that is used for pretargeting in combination with a bispecific or multispecific antibody. The F-18-metal labeled molecules are stable in human serum at 37° C.

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