📜5-(Methoxycarbonyl)-2-Methylpyridine 1-Oxide置于manganese(Iv) Oxide,三氟乙酸酐体系中,用 二氯甲烷 用作溶剂,化学反应 6.0H,反应生成6-甲酰基烟酸甲酯 参考文献: Btk Inhibitors[fr] Inhibiteurs De Btk 标题: Btk Inhibitors[fr] Inhibiteurs De Btk 摘要:根据公式i提供了bruton'S酪氨酸激酶(btk)抑制剂化合物,或其药学上可接受的盐,或包含这些化合物的药物组合物,并且这些化合物在治疗中的用途.特别提供了使用公式i的btk抑制剂化合物来治疗btk介导的疾病.
专利信息
专利号:US-11225655-B2 优先权日:2010-04-16 标题:Bi-functional complexes and methods for making and using such complexes 发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK 权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS 摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.
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-8709382-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.
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 320. 摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 398.