42471-56-7Relevant academic research and scientific papers
BENZODIAZEPINE DERIVATIVES AS CCK2/GASTRIN RECEPTOR ANTAGONISTS
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Page/Page column 41; 43, (2016/03/26)
The invention relates to benzodiazepine derivatives of formula (A) useful as CCK2/gastrin receptor antagonists, their preparation and their use in the treatment or prevention of disorders associated with CCK2/gastrin receptors, disorders caused by or associated with hypergastrinaemia, and gastric acid-related disorders.
Antiaromatic compounds and organic light-emitting device comprising the same
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Paragraph 0489-0492, (2016/10/10)
The present invention relates to an anti-aromatic compound and an organic light emitting device comprising the same. According to one embodiment of the present invention, provided is an anti-aromatic compound represented by chemical formula 1. The organic light emitting device comprising the anti-aromatic compound can obtain high efficiency and long lifespan properties.COPYRIGHT KIPO 2016
Enantioselective diamination with novel chiral hypervalent iodine catalysts
Mizar, Pushpak,Laverny, Aragorn,El-Sherbini, Mohammad,Farid, Umar,Brown, Michael,Malmedy, Florence,Wirth, Thomas
supporting information, p. 9910 - 9913 (2014/08/18)
Vicinal diamines constitute one the most important functional motif in organic chemistry because of its wide occurrence in a variety of biological and pharmaceutical molecules. We report an efficient metal-free, highly stereoselective intramolecular diamination using a novel chiral hypervalent iodine reagent together with its application as an efficient catalyst for the synthesis of diamines.
Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity
Spencer, John,Rathnam, Rajendra P.,Harvey, Alan L.,Clements, Carol J.,Clark, Rachel L.,Barrett, Michael P.,Wong, Pui Ee,Male, Louise,Coles, Simon J.,MacKay, Simon P.
experimental part, p. 1802 - 1815 (2011/04/17)
A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 μM.
AMIDE DERIVATIVES AS SIRTUIN MODULATORS
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Page/Page column 85, (2009/06/27)
Provided herein are novel sirtuin-modulating compounds represented by Structural Formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.
Process of preparing benzodiazepine compounds useful as antagonists of CCK or of gastrine
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, (2008/06/13)
A benzodiazepine derivative of formula I, or a pharmaceutically acceptable salt thereof: STR1 wherein: (a) R4 is an alkyl, cycloalkyl or aryl group. (b) R10 is chosen from halo, OH, CH3, OCH3, NR11 R12, NO2, NHCHO, CO2 H and CN, and R11 and R12 are independently selected from H and alkyl (C1 -C5) or together NR11 R12 form a cyclic structure II, STR2 wherein a is 1-6; and (c) R2 is an aromatic 5- or 6-membered, substituted or unsubstituted heterocycle containing at least two heteroatoms of which at least one is nitrogen. These compounds are gastrin and/or CCK-B receptor antagonists.
A facile large scale synthesis of optically active 3-amino-5-(2-pyridyl)-1,4-benzqdiazepin-2-one derivatives
Semple, Graeme,Ryder, Hamish,Ohta, Mitsuaki,Satoh, Masato
, p. 721 - 727 (2007/10/03)
A facile method for the synthesis of 3-amino-5-(2-pyridyl)-1,4-benzodiazepin-2-ones (8) mediated by benzotriazole is described. The synthesis and optical resolution of the product by fractional crystallisation proceeds in high yield, under mild conditions and without recourse to toxic reagents or chromatographic separations and hence is amenable to the large scale preparation of these important precursors to potent CCK receptor ligands.
The synthesis of substituted 2-aminophenyl heterocycic ketones
Fryer,Zhang,Rios
, p. 985 - 992 (2007/10/02)
The synthesis of substituted 2-aminophenyl heterocyclic ketones, key intermediates to the preparation of 1,4-benzodiazepines has been achieved in one step and in good, yield from the corresponding anthranilic acid, by treatment with heterocyclic lithium reagents and chlorotrimethylsilane.
[2-[(Nitropyridinyl)amino]phenyl]arymethanones
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, (2008/06/13)
[2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: STR1 wherein: B is carbonyl, thioxomethyl, ketal or thioketal, R is hydrogen or -alk1 -Q, Q is hydrogen, --NR1 R2 or halogen are disclosed in a process for preparing pyrido[1,4]benzodiazepines.
