公开(公告)号：US20240072425A1

公开(公告)日：2024-02-29

申请号：US18023511

申请日：2021-08-25

申请人： MERCK PATENT GMBH

发明人： Constanze BROCKE ,  Carsten FRITZSCH ,  Dagmar KLASS

IPC分类号： H01Q1/36 ,  C07C331/28

CPC分类号： H01Q1/36 ,  C07C331/28

摘要： The present invention relates to a liquid crystal medium comprising aromatic isothiocyanates of formula C




as defined in claim 1, and to high-frequency components comprising these media, especially microwave components for high-frequency devices, such as devices for shifting the phase of microwaves, tunable filters, tunable metamaterial structures, and electronic beam steering antennas, e.g. phased array antennas.

公开(公告)号：US20180273441A1

公开(公告)日：2018-09-27

申请号：US15522859

申请日：2015-10-29

申请人： KATHOLIEKE UNIVERSITEIT LEUVEN

发明人： Ahamed Muneer Syed Musthakahmed ,  Emilie Billaud ,  Guy Bormans ,  Frederik Cleeren ,  Joan Lecina ,  Alfons Verbruggen

IPC分类号： C07B59/00 ,  G01N33/534 ,  C07K1/13 ,  A61K51/08 ,  A61K51/04 ,  A61K51/10 ,  C07C229/14 ,  C07C229/16 ,  C07C229/38 ,  C07C229/42 ,  C07C259/06 ,  C07C331/28 ,  C07D213/38 ,  C07D243/08 ,  C07D255/02

CPC分类号： C07B59/008 ,  A61K51/0482 ,  A61K51/088 ,  A61K51/1093 ,  A61K2123/00 ,  C07B2200/05 ,  C07B2200/07 ,  C07C215/50 ,  C07C229/14 ,  C07C229/16 ,  C07C229/38 ,  C07C229/42 ,  C07C259/06 ,  C07C331/28 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/38 ,  C07D243/08 ,  C07D255/02 ,  C07K1/13 ,  G01N33/534

摘要： New chelators such as H3L1, H3L2, H3L3, H3L26 and derivatives were synthesized for the complexation of {Al18F}2+. These new chelators are able to complex {AI18F}2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI18F-L3 and AI18F-L26 showed a stability comparable to that of the previously reported Al18F-NODA. Moreover, the biodistribution of Al18F-L3 and Al18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H3L3 and Al18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with 18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI18F}2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI18F-L3 and AI18F-L26 showed a stability comparable to that of the previously reported Al18F-NODA. Moreover, the biodistribution of Al18F-L3 and Al18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H3L3 and H3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with 18F-fluorine and several derivatives have been synthesized.

公开(公告)号：US10016444B2

公开(公告)日：2018-07-10

申请号：US15524257

申请日：2015-11-05

申请人： ISTITUTO ORTOPEDICO RIZZOLI ,  UNIVERSITA' DI PISA

发明人： Gina Lisignoli ,  Francesco Grassi ,  Vincenzo Calderone ,  Simona Rapposelli

IPC分类号： C07C331/28 ,  A61K31/663 ,  C07C331/24 ,  C07F9/38

CPC分类号： A61K31/663 ,  C07C331/24 ,  C07C331/28 ,  C07F9/38 ,  C07F9/3873

摘要： The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts thereof: (I) wherein Ri is selected from an SCN— group or is an RCONH— group; in particular, where Ri=RCONH, R is selected from an aromatic benzene ring substituted with an SCN— group in the ortho, meta or para position, according to the following formula: SCN— or R is a C1-C4 alkyl chain, substituted with an SCN— group; n can be equal to 0 or else 1. The invention also relates to the use of such compounds for the treatment of osteoporosis and in general of bone pathologies characterized by a progressive loss of bone mass, for example rheumatoid arthritis, hyperparathyroidism or bone tumor metastases.

公开(公告)号：US20170260124A1

公开(公告)日：2017-09-14

申请号：US15605195

申请日：2017-05-25

申请人： RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK

发明人： Khosrow Kashfi ,  Ravinder Kodela

IPC分类号： C07C203/04 ,  C07F9/6558 ,  C07D413/12 ,  C07D339/04 ,  C07D271/08 ,  C07C331/28 ,  C07C327/48 ,  A61K31/655 ,  C07F9/6578

CPC分类号： C07C203/04 ,  A61K31/655 ,  C07C327/48 ,  C07C331/28 ,  C07D271/08 ,  C07D339/04 ,  C07D413/12 ,  C07F9/65583 ,  C07F9/6578

摘要： This disclosure relates to compounds containing both an NO-releasing moiety and an H2S-releasing moiety and the use of such compounds in treating inflammatory diseases, including cancers.

公开(公告)号：US20170174634A1

公开(公告)日：2017-06-22

申请号：US15327531

申请日：2015-07-21

申请人： BAYER CROPSCIENCE AKTIENGESELLSCHAFT

发明人： JOACHIM TELSER ,  PETER DAHMEN ,  ULRIKE WACHENDORFF-NEUMANN ,  PIERRE CRISTAU ,  PHILIPPE RINOLFI

IPC分类号： C07D231/38 ,  C07C331/28 ,  C07C217/76 ,  A01N43/56

CPC分类号： C07D231/38 ,  A01N43/56 ,  C07C217/76 ,  C07C331/28 ,  C07D401/04

摘要： The present invention relates to novel pyrazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for controlling harmful microorganisms in crop protection and in the protection of materials. Further, the present invention also relates to certain intermediates useful for producing said novel pyrazole derivatives.

公开(公告)号：US09663454B2

公开(公告)日：2017-05-30

申请号：US14899883

申请日：2014-07-04

申请人： Universite de Strasbourg ,  Centre National de la Recherche Scientifique

发明人： Alain Wagner ,  Oleksandr Koniev

IPC分类号： C12P21/00 ,  C07C255/43 ,  C07C255/44 ,  C07C323/60 ,  C07K1/13 ,  C07C255/34 ,  C07C255/35 ,  C07C255/37 ,  C07C255/41 ,  C07C255/42 ,  G01N33/58 ,  G01N33/84 ,  C07F9/54 ,  C07C319/02 ,  C07D311/88 ,  C07D405/12 ,  C07C331/28 ,  C07C335/22 ,  C07D207/452 ,  C07D249/06 ,  C07F5/04 ,  C07F7/08 ,  C07K14/705 ,  C07K16/28 ,  C07K16/30 ,  C07K19/00 ,  C12N9/36

CPC分类号： C07C255/43 ,  C07B2200/05 ,  C07C255/34 ,  C07C255/35 ,  C07C255/37 ,  C07C255/41 ,  C07C255/42 ,  C07C255/44 ,  C07C271/16 ,  C07C271/22 ,  C07C271/28 ,  C07C275/42 ,  C07C309/42 ,  C07C319/02 ,  C07C323/42 ,  C07C323/60 ,  C07C331/28 ,  C07C335/22 ,  C07C2602/24 ,  C07D207/452 ,  C07D207/46 ,  C07D249/06 ,  C07D265/38 ,  C07D311/82 ,  C07D311/88 ,  C07D337/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D495/04 ,  C07F5/04 ,  C07F7/08 ,  C07F7/081 ,  C07F9/5442 ,  C07K1/13 ,  C07K14/70596 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/32 ,  C07K19/00 ,  C07K2317/24 ,  C07K2317/76 ,  C12N9/2462 ,  C12Y302/01017 ,  G01N33/58 ,  G01N33/84

摘要： The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

公开(公告)号：US09527870B2

公开(公告)日：2016-12-27

申请号：US14749158

申请日：2015-06-24

申请人： JNC CORPORATION ,  JNC PETROCHEMICAL CORPORATION

发明人： Yasuyuki Gotoh ,  Masahide Kobayashi

IPC分类号： G02F1/1333 ,  C07D519/00 ,  C09K19/34 ,  C09K19/30 ,  C09K19/32 ,  C07C25/18 ,  C07D239/26 ,  C07D319/06 ,  C07C321/28 ,  C07C255/50 ,  C07C331/28 ,  C07C25/22 ,  C07D309/04 ,  C07D213/26 ,  C07D413/04 ,  C07C25/24 ,  C09K19/12

CPC分类号： C07D519/00 ,  C07C25/18 ,  C07C25/22 ,  C07C25/24 ,  C07C255/50 ,  C07C321/28 ,  C07C331/28 ,  C07D213/26 ,  C07D239/26 ,  C07D309/04 ,  C07D319/06 ,  C07D413/04 ,  C09K19/3098 ,  C09K19/322 ,  C09K19/3444 ,  C09K19/3458 ,  C09K2019/122 ,  C09K2019/123 ,  C09K2019/124 ,  C09K2019/3016 ,  C09K2019/3018 ,  C09K2019/3019 ,  C09K2019/3025 ,  C09K2019/3027 ,  C09K2019/325 ,  C09K2019/326 ,  C09K2019/3422 ,  C09K2019/3425 ,  C09K2019/3427

摘要： To provide a liquid crystal compound satisfying at least one physical property such as high stability to light, a high clearing point, low minimum temperature of a liquid-crystal phase, small viscosity, suitable optical anisotropy, large dielectric anisotropy, a large dielectric constant in a minor axis direction, a suitable elastic constant, excellent compatibility with other liquid crystal compounds. The compound is represented by formula (1-1): for example, R is alkyl having 1 to 10 carbons or alkoxy having 1 to 9 carbons, rings A1 to A3 are 1,4-cyclohexylene, 1,4-phenylene, or 1,4-phenylene in which at least one hydrogen is replaced by halogen; X is halogen, —CF3 or —OCF3; l is 1, and m, n is 0 or 1; W1 is a group represented by formula (1a) or (1b); W2 is a group represented by formula (1c) or (1d); Y1 to Y2 are hydrogen, Y3 to Y5 and L1 to L5 are fluorine.

摘要翻译： 为了提供满足光稳定性，高透明点，液晶相的最低最低温度，低粘度，适当的光学各向异性，大介电各向异性，大介电常数各向异性等的至少一种物性的液晶化合物 短轴方向，合适的弹性常数，与其他液晶化合物的相容性优异。 化合物由式（1-1）表示：例如，R为碳数为1〜10的烷基或碳数为1〜9的烷氧基，A 1〜A 3为1,4-亚环己基，1,4-亚苯基或1 其中至少一个氢被卤素取代的4-亚苯基; X是卤素，-CF 3或-OCF 3; l为1，m，n为0或1; W1是由式（1a）或（1b）表示的基团; W2是由式（1c）或（1d）表示的基团; Y1〜Y2为氢，Y3〜Y5，L1〜L5为氟。

公开(公告)号：US09102602B2

公开(公告)日：2015-08-11

申请号：US13990312

申请日：2010-11-29

申请人： Junko Takada ,  Shunsuke Iwamoto ,  Satoshi Nakano

发明人： Junko Takada ,  Shunsuke Iwamoto ,  Satoshi Nakano

IPC分类号： C07C331/28

CPC分类号： C07C331/28

摘要： The object of the present invention is to provide a novel method for producing an isothiocyanate compound having a carboxyl group(s) by a reaction of the corresponding amino compound having a carboxyl group(s), thiocarbonyldiimidazole and a base, in one step with high purity. An amino compound having a carboxyl group(s) is reacted with thiocarbonyldiimidazole in a solvent in the presence of a base to obtain an isothiocyanate compound having a carboxyl group(s).

摘要翻译： 本发明的目的是提供一种具有羧基的具有羧基的相应氨基化合物，硫代羰基二咪唑和碱的具有羧基的异硫氰酸酯化合物的新方法，其中一步具有高的 纯度。 具有羧基的氨基化合物与硫代羰基二咪唑在溶剂中在碱存在下反应，得到具有羧基的异硫氰酸酯化合物。

公开(公告)号：US08987316B2

公开(公告)日：2015-03-24

申请号：US14346744

申请日：2012-09-18

申请人： Jochen Kalbe

发明人： Jochen Kalbe

IPC分类号： C07C265/12 ,  C07C331/28 ,  C07C309/15 ,  C07D233/64

CPC分类号： C07D233/64 ,  C07C265/12 ,  C07C309/15 ,  C07C331/28

摘要： The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.

摘要翻译： 本发明涉及新颖的异氰酸酯和异硫氰酸酯化合物，包含它们的药物组合物，以及其在治疗人和动物中的癌症疾病中的用途。 与已知的异氰酸酯和异硫氰酸酯化合物相比，新型异氰酸酯和异硫氰酸酯化合物通过改善的治疗宽度，即具有较高抗肿瘤活性的副作用较小。

公开(公告)号：US20130259802A1

公开(公告)日：2013-10-03

申请号：US13898131

申请日：2013-05-20

申请人： HAMMERSMITH IMANET LIMITED

发明人： ERIK ARSTAD ,  MATTHIAS EBERHARD GLASER

IPC分类号： A61K51/08 ,  C07D205/04 ,  C07C215/08 ,  C07K14/47 ,  C07C331/28

CPC分类号： A61K51/087 ,  A61K51/088 ,  C07B59/008 ,  C07C215/08 ,  C07C215/14 ,  C07C271/28 ,  C07C331/28 ,  C07D205/04 ,  C07K1/13 ,  C07K14/47

摘要： The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

摘要翻译： 本发明提供了含有伯氨基的生物分子如蛋白质和肽，特别是肽的[18 F] - 氟化方法。 本发明还提供用于该方法的试剂，特别是用于制备的18F标记的假基团以及可用于制备[18 F] - 标记的假体基团的未标记的中间体。 也可用作用作放射性药物的[18F]标记化合物，专门用于正电子发射断层扫描（PET）。