公开(公告)号：US20190276416A1

公开(公告)日：2019-09-12

申请号：US15912734

申请日：2018-03-06

申请人： INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN, R.O.C.

发明人： YU CHANG ,  CHENG-FANG HSU

IPC分类号： C07D255/02 ,  C07C303/38 ,  C07C303/28 ,  C07C311/18 ,  C07C309/30 ,  C07B51/00

摘要： A method for preparing a NOTA derivative is revealed. The method includes a plurality of steps. First take 4-toluenesulfonyl chloride and diethylenetriamine to carry out tosylation reaction and obtain a first product. Then the first substitution reaction takes place upon addition of the first product with sodium methoxide to get the second product. Next take 4-toluenesulfonyl chloride to react with ethylene glycol for preparing a third product by tosylation reaction therebewteen. Then a coupling reaction between the third product and the second product is carried out to produce a fourth product. The second substitution reaction occurs involving the fourth product in the presence of sulfuric acid. Lastly take the reaction product and hydrochloric acid to have bonding reaction and obtain a final product. The method solves the water-absorption problem of the cyclic organic compound TACN, a NOTA derivative.

公开(公告)号：US20190177478A1

公开(公告)日：2019-06-13

申请号：US16216143

申请日：2018-12-11

申请人： Evonik Degussa GmbH

发明人： Kévin MICOINE ,  Kristina ZUMBANSEN ,  Franz-Erich BAUMANN ,  Marcus Matthias STERGAR ,  Andreas PAWLIK ,  Christoph HILLER ,  Mirko MICHEL ,  Christoph KOOPMANN

IPC分类号： C08G69/16 ,  C07D255/02

摘要： Polymers can be prepared from monomers comprising laurolactam, by a process including a. Beckmann rearrangement of cyclododecanone oxime to give laurolactam in the presence of a Beckmann rearrangement catalyst, b. removal of impurities from the laurolactam to obtain purified laurolactam, and c. polymerization of monomers comprising purified laurolactam. For avoidance of discolouration or yellowing under ageing conditions, prior to the polymerization, polycyclic substances containing 24 carbon atoms and at least one heteroatom selected from oxygen and nitrogen and having a molar mass between 300 and 380 g/mol are limited to 500 ppm, based on laurolactam.

公开(公告)号：US10301254B2

公开(公告)日：2019-05-28

申请号：US15568555

申请日：2016-04-22

申请人： Temple University—Of The Commonwealth System of Higher Education ,  Villanova University

发明人： William M. Wuest ,  Kevin P. C. Minbiole

IPC分类号： C07D295/02 ,  C07C211/63 ,  A61K31/13 ,  A61K31/16 ,  A61K45/06 ,  C08G73/00 ,  C07D401/04 ,  C07D453/02 ,  C07D255/02 ,  C07D257/02 ,  C07D295/037 ,  C07D213/36 ,  A01N33/12 ,  A01N43/40 ,  A01N43/60 ,  A01N43/64 ,  A01N43/90 ,  C07C211/64 ,  C07D295/13 ,  C08F8/32 ,  C08F112/14 ,  C08F120/34 ,  C09D5/14

摘要： The present invention includes polycationic amphiphilic compounds of formula VII useful as antimicrobial agents. The present invention further includes novel polymers of polycationic amphiphilic compounds useful as antimicrobial agents. The present invention further includes methods useful for removing microorganisms and/or biofilm-embedded microorganisms from a surface. The present invention further includes compositions and methods useful for preventing or reducing the growth or proliferation of microorganisms and/or biofilm-embedded microorganisms on a surface.

公开(公告)号：US10201621B2

公开(公告)日：2019-02-12

申请号：US15633233

申请日：2017-06-26

申请人： Beth Israel Deaconess Medical Center, Inc. ,  Georgia State University Research Foundation Inc.

发明人： John V. Frangioni ,  Maged M. Henary

IPC分类号： A61K49/00 ,  C12Q1/02 ,  C07D209/02 ,  C07D255/02 ,  A61B6/00 ,  C09B23/01 ,  C09B23/08 ,  C07D209/42 ,  G01N33/58

摘要： The present invention relates to compositions for and methods of optically imaging tissues or cells using imaging agents having desirable in vivo properties that result in improved signal-to-background ratio.

公开(公告)号：US20170290928A1

公开(公告)日：2017-10-12

申请号：US15633349

申请日：2017-06-26

申请人： Beth Israel Deaconess Medical Center ,  Georgia State University Research Foundation Inc.

发明人： John V. Frangioni

IPC分类号： A61K49/00 ,  C07D209/42 ,  G01N33/58 ,  C07D209/02 ,  C09B23/01 ,  C09B23/08 ,  A61B6/00 ,  C07D255/02

CPC分类号： A61K49/0032 ,  A61B5/0059 ,  A61B6/00 ,  C07D209/02 ,  C07D209/42 ,  C07D255/02 ,  C09B23/0066 ,  C09B23/086 ,  C09B67/0025 ,  G01N33/582 ,  G01N2800/347

摘要： The present invention relates to a method for detecting renal disease and for assessing the efficacy of dialysis treatment using imaging agents having desirable in vivo properties.

公开(公告)号：US20170283442A1

公开(公告)日：2017-10-05

申请号：US15621571

申请日：2017-06-13

申请人： Immunomedics, Inc.

发明人： Christopher A. D'Souza ,  William J. McBride ,  David M. Goldenberg

IPC分类号： C07F5/06 ,  C07D207/452 ,  C07D405/12 ,  C07D475/04 ,  C07D255/02 ,  C07B59/00 ,  C07K7/06 ,  C07D403/12

CPC分类号： C07F5/069 ,  C07B59/002 ,  C07B2200/05 ,  C07D207/452 ,  C07D255/02 ,  C07D403/12 ,  C07D405/12 ,  C07D475/04 ,  C07K7/06

摘要： The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F 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 18F or 19F 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 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

公开(公告)号：US09765071B2

公开(公告)日：2017-09-19

申请号：US15068892

申请日：2016-03-14

申请人： 3M INNOVATIVE PROPERTIES COMPANY

发明人： Larry R. Krepski ,  Joseph F. Dellaria, Jr. ,  Daniel E. Duffy ,  Matthew R. Radmer ,  David T. Amos

IPC分类号： C07D471/14 ,  C07D471/04 ,  C07D255/02 ,  C07D213/74

CPC分类号： C07D471/04 ,  C07D213/74 ,  C07D255/02 ,  C07D471/14

摘要： Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

公开(公告)号：US20170217922A1

公开(公告)日：2017-08-03

申请号：US15423436

申请日：2017-02-02

申请人： Rigel Pharmaceuticals, Inc.

发明人： Matthew Duncton ,  Rajinder Singh

IPC分类号： C07D401/04 ,  C07D255/02 ,  C07D257/04

CPC分类号： C07D401/04 ,  C07D249/12 ,  C07D255/02 ,  C07D257/04

摘要： Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

公开(公告)号：US09562113B2

公开(公告)日：2017-02-07

申请号：US14989041

申请日：2016-01-06

申请人： Bellerophon BCM LLC

发明人： Fuqiang Ruan ,  Thomas L. Deckwerth ,  Martin D. Meglasson

IPC分类号： A61K51/00 ,  A61M36/14 ,  C08B37/00 ,  A61K51/06 ,  C07B59/00 ,  C07D255/02 ,  C07F1/08 ,  C07F5/00 ,  A61K49/04 ,  A61K51/04

CPC分类号： C08B37/0084 ,  A61K49/04 ,  A61K51/04 ,  A61K51/065 ,  C07B59/002 ,  C07D255/02 ,  C07F1/08 ,  C07F5/003

摘要： Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.

摘要翻译： 描述了能够与藻酸盐和金属离子共轭的双功能NOTA基衍生物，以及可以用稳定或放射性金属离子标记的NOTA-藻酸盐缀合物。 还描述了双官能NOTA-基接头与藻酸盐的缀合方法，以及使用放射性金属标记的NOTA-藻酸盐缀合物或其它放射性标记的藻酸盐缀合物作为成像试剂的方法。

公开(公告)号：US20160235870A1

公开(公告)日：2016-08-18

申请号：US15027104

申请日：2014-10-06

申请人： ILLINOIS INSTITUTE OF TECHNOLOGY

发明人： Hyun-Soon CHONG

IPC分类号： A61K51/04 ,  C07D255/02

CPC分类号： A61K51/0482 ,  A61K51/0474 ,  C07D255/02 ,  C07D257/02 ,  C07D401/12

摘要： Multifunctional chelators, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.

摘要翻译： 多功能螯合剂，其金属络合物，其组合物，以及制备和用于细胞病症诊断成像和治疗的方法。