专利号:US-12129222-B2 优先权日:2016-08-11 标题:Production of bitter principle derivatives 发明人:WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS 权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV 摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.
专利号:US-8617518-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; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 68 Ga, 18 F or 19 F labeled molecules of use in PET or MRI 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 chelating moiety, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 68 Ga, 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. In more preferred embodiments, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment.
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-2009221019-A1 优先权日:2005-06-22 标 题:Core-Modified Terpene Trilactones From Ginkgo Biloba Extract and Biological Evaluation Thereof 发明人:NAKANISHI KOJI; DZYUBA SERGEI; ISHII HIDEKI 权利人:NAKANISHI KOJI; DZYUBA SERGEI; ISHII HIDEKI 摘要:Lactone-rings of ginkgolides are converted into the corresponding tetrahydrofuran moieties via DIBAL-H reduction followed by deoxygenation of the formed lactols with Et 3 SiH/BF 3 Et 2 O producing a series of lactol-free ginkgolides. The present invention also relates to synthesis of hydroxyl-free, or hydroxyl-free and lactone-free, ginkgolides and bilobalides.
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.
专利号:US-8808665-B2 优先权日:2007-01-11 标 题:In vivo copper-free click chemistry for delivery of therapeutic and/or diagnostic agents 发明人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use involving click chemistry reactions for in vivo or in vitro formation of therapeutic and/or diagnostic complexes. Preferably, the diagnostic complex is of use for 18 F imaging, while the therapeutic complex is of use for targeted delivery of chemotherapeutic drugs or toxins. More preferably, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment, using a click chemistry reaction involving cyclooctyne, nitrone or azide reactive moieties. In most preferred embodiments, the click chemistry reaction occurs in vivo. In vivo click chemistry is not limited to 18 F labeling but can be used for delivering a variety of therapeutic and/or diagnostic agents.
参考标题:Structure-Based Design Of Highly Potent Toll-Like Receptor 7/8 Dual Agonists For Cancer Immunotherapy 作者:Zhisong Wang,Yan Gao,Lei He,Shuhao Sun,Tingting Xia,Lu Hu,Licheng Yao,Liangliang Wang,Dan Li,Hui Shi,Xuebin Liao |发布日期:2021.6.10 摘要:Activation Of The Toll-Like Receptors 7 And 8 Has Emerged As A Promising Strategy For Cancer Immunotherapy. Herein, We Report The Design And Synthesis Of A Series Of Pyrido[3,2-D]Pyrimidine-Based Toll-Like Receptor 7/8 Dual Agonists That Exhibited Potent And Near-Equivalent Agonistic Activities Toward Tlr7 And Tlr8. In Vitro, Compounds 24E And 25A Significantly Induced The Secretion Of Ifn-α, Ifn-γ