专利号:US-6248891-B1 优先权日:1997-05-23 标题:Synthesis of acridine derivative multidrug-resistant inhibitors 发明人:SHARP MATTHEW JUDE; MADER CATHERINE J; STRACHAN CALUM 权利人:GLAXO WELLCOME INC 摘要:Synthesis of the MDRI of formula (I) from intermediates of acridone acid of formula (II) and aminophenethyl isoquinoline of formula (III), via steps including coupling and conversion to yield the MDRI of formula (I).
专利号:WO-2005103035-A1 优先权日:2004-04-23 标题:Modified fischer indole synthesis of eletriptan 发明人:ASHCROFT CHRISTOPHER PAUL 权利人:PFIZER LTD; ASHCROFT CHRISTOPHER PAUL; PFIZER 摘要:The present invention relates to a new process for the preparation of eletriptan (I), or its enantiomer comprising a modified Fischer indole synthesis, namely the reaction of a compound of formula (II), wherein R1 is a suitable hydrazine protecting group, with a compound of formula (III) wherein R2 is an aldehyde group (-CHO) or the functional equivalent thereof.
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-2016045626-A1 优先权日:2007-01-11 标题 :Methods and Compositions for Improved Labeling of Targeting Peptides 发明人: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 labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a therapeutic or diagnostic isotope, such as 61 Cu, 62 Cu, 64 Cu, 67 Cu, 18 F, 19 F, 66 Ga, 67 Ga, 68 Ga, 72 Ga, 111 In, 177 Lu, 44 Sc, 47 Sc, 86 Y, 88 Y, 90 Y, 45 Ti or 89 Zr, preferably 18 F or 19 F. More preferably, the targeting peptide is NOTA-octreotate, NOTA-MPAA-octreotate, pyridine-NOTA-octreotate or triazole-NOTA-octreotate. The labeled targeting peptides may be used for detection, diagnosis, imaging and/or treatment of sst 2 + tumors, such as neuroendocrine tumors.
专利号:US-9028800-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 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 labeled molecule may be used for imaging in a subject without purification after labeling.
专利号:WO-9852923-A1 优先权日:1997-05-23 标题:Synthesis of acridine derivative multidrug-resistant inhibitors
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合成参考文献
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