120363-13-5Relevant articles and documents
CBTF: New amine-to-thiol coupling reagent for preparation of antibody conjugates with increased plasma stability
Kolodych, Sergii,Koniev, Oleksandr,Baatarkhuu, Zoljargal,Bonnefoy, Jean-Yves,Debaene, Fran?ois,Cianférani, Sarah,Van Dorsselaer, Alain,Wagner, Alain
, p. 197 - 200 (2015)
Amine-to-thiol coupling is the most common route for the preparation of antibody-drug conjugates (ADC). It is usually achieved by using heterobifunctional reagents possessing an activated ester at one end and a maleimide group at the other. However, malei
Development of High-Performance Pyrimidine Nucleoside and Oligonucleotide Diarylethene Photoswitches
Kolmar, Theresa,Büllmann, Simon M.,Sarter, Christopher,H?fer, Katharina,J?schke, Andres
supporting information, p. 8164 - 8173 (2021/03/08)
Nucleosidic and oligonucleotidic diarylethenes (DAEs) are an emerging class of photochromes with high application potential. However, their further development is hampered by the poor understanding of how the chemical structure modulates the photochromic properties. Here we synthesized 26 systematically varied deoxyuridine- and deoxycytidine-derived DAEs and analyzed reaction quantum yields, composition of the photostationary states, thermal and photochemical stability, and reversibility. This analysis identified two high-performance photoswitches with near-quantitative, fully reversible back-and-forth switching and no detectable thermal or photochemical deterioration. When incorporated into an oligonucleotide with the sequence of a promotor, the nucleotides maintained their photochromism and allowed the modulation of the transcription activity of T7 RNA polymerase with an up to 2.4-fold turn-off factor, demonstrating the potential for optochemical control of biological processes.
A New Class of Rigid Multi(azobenzene) Switches Featuring Electronic Decoupling: Unravelling the Isomerization in Individual Photochromes
Galanti, Agostino,Santoro, Jasmin,Mannancherry, Rajesh,Duez, Quentin,Diez-Cabanes, Valentin,Valá?ek, Michal,De Winter, Julien,Cornil, Jér?me,Gerbaux, Pascal,Mayor, Marcel,Samorì, Paolo
supporting information, p. 9273 - 9283 (2019/06/07)
We report a novel class of star-shaped multiazobenzene photoswitches comprising individual photochromes connected to a central trisubstituted 1,3,5-benzene core. The unique design of such C3-symmetric molecules, consisting of conformationally r
Electronic Decoupling in C3-Symmetrical Light-Responsive Tris(Azobenzene) Scaffolds: Self-Assembly and Multiphotochromism
Galanti, Agostino,Diez-Cabanes, Valentin,Santoro, Jasmin,Valá?ek, Michal,Minoia, Andrea,Mayor, Marcel,Cornil, Jér?me,Samorì, Paolo
, p. 16062 - 16070 (2018/11/23)
We report the synthesis of a novel C3-symmetrical multiphotochromic molecule bearing three azobenzene units at positions 1, 3, 5 of the central phenyl ring. The unique geometrical design of such a rigid scaffold enables the electronic decouplin
NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT
-
Paragraph 0116, (2018/06/07)
The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, comprising same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.
Metal-free radical aromatic carbonylations mediated by weak bases
Koziakov, Denis,Jacobi Von Wangelin, Axel
supporting information, p. 6715 - 6719 (2017/08/22)
We report a new method of metal-free alkoxycarbonylation. This reaction involves the generation of aryl radicals from arenediazonium salts by a very weak base (HCO2Na) under mild conditions. Subsequent radical trapping with carbon monoxide and alcohols gives alkyl benzoates. The conditions (metal-free, 1 equiv. base, MeCN, r.t., 3 h) tolerate various functional groups (I, Br, Cl, CF3, SF5, NO2, ester). Mechanistic studies indicate the operation of a radical aromatic substitution mechanism.
Ultrahigh Surface Area Zirconium MOFs and Insights into the Applicability of the BET Theory
Wang, Timothy C.,Bury, Wojciech,Gómez-Gualdrón, Diego A.,Vermeulen, Nicolaas A.,Mondloch, Joseph E.,Deria, Pravas,Zhang, Kainan,Moghadam, Peyman Z.,Sarjeant, Amy A.,Snurr, Randall Q.,Stoddart, J. Fraser,Hupp, Joseph T.,Farha, Omar K.
, p. 3585 - 3591 (2015/03/30)
An isoreticular series of metal-organic frameworks (MOFs) with the ftw topology based on zirconium oxoclusters and tetracarboxylate linkers with a planar core (NU-1101 through NU-1104) has been synthesized employing a linker expansion approach. In this se
OXIME DERIVATIVE, METHOD OF PRODUCING THE SAME AND INSECTICIDE COMPRISING THE SAME AS ACTIVE INGREDIENT
-
, (2018/10/03)
PROBLEM TO BE SOLVED: To provide a compound having excellent insecticidal effect and useful as an active ingredient of an insecticide. SOLUTION: This invention provides an oxime derivative represented by general formula (1) (where Ra, X and n represent definitions described in the specifications) and an insecticide that comprises the same as an active ingredient. COPYRIGHT: (C)2015,JPOandINPIT
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity
Filipski, Kevin J.,Bian, Jianwei,Ebner, David C.,Lee, Esther C.Y.,Li, Jian-Cheng,Sammons, Matthew F.,Wright, Stephen W.,Stevens, Benjamin D.,Didiuk, Mary T.,Tu, Meihua,Perreault, Christian,Brown, Janice,Atkinson, Karen,Tan, Beijing,Salatto, Christopher T.,Litchfield, John,Pfefferkorn, Jeffrey A.,Guzman-Perez, Angel
scheme or table, p. 415 - 420 (2012/02/16)
A novel series of glucagon receptor antagonists has been discovered. These pyrazole ethers and aminopyrazoles have lower molecular weight and increased polarity such that the molecules fall into better drug-like property space. This work has culminated in
INSULIN DERIVATIVE
-
Page/Page column 90, (2008/06/13)
The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.