36309-43-0Relevant academic research and scientific papers
A copper(ii)-dipicolylamine-coumarin sensor for maltosyltransferase assay
Lee, Wei-Li,Hsu, Tse-Wei,Hung, Wei-Cheng,Fang, Jim-Min
, p. 8026 - 8029 (2019)
A Cu(ii)-[di(2-methylpyridyl)methylamino]coumarin fluorescence turn-on sensor (Cu-1b) is designed to detect phosphate ions with Kass = 1.4 × 105 M-1 in HEPES buffer. Cu-1b is applied to probe the GlgE-catalyzed maltose-tra
Discovery of M3Antagonist-PDE4 Inhibitor Dual Pharmacology Molecules for the Treatment of Chronic Obstructive Pulmonary Disease
Armani, Elisabetta,Rizzi, Andrea,Capaldi, Carmelida,De Fanti, Renato,Delcanale, Maurizio,Villetti, Gino,Marchini, Gessica,Pisano, Anna Rita,Pitozzi, Vanessa,Pittelli, Maria Gloria,Trevisani, Marcello,Salvadori, Michela,Cenacchi, Valentina,Puccini, Paola,Amadei, Francesco,Pappani, Alice,Civelli, Maurizio,Patacchini, Riccardo,Baker-Glenn, Charles A.G.,Van De Po?l, Hervé,Blackaby, Wesley P.,Nash, Kevin,Amari, Gabriele
, p. 9100 - 9119 (2021/07/19)
In this paper, we report the discovery of dual M3 antagonist-PDE4 inhibitor (MAPI) compounds for the inhaled treatment of pulmonary diseases. The identification of dual compounds was enabled by the intuition that the fusion of a PDE4 scaffold derived from our CHF-6001 series with a muscarinic scaffold through a common linking ring could generate compounds active versus both the transmembrane M3 receptor and the intracellular PDE4 enzyme. Two chemical series characterized by two different muscarinic scaffolds were investigated. SAR optimization was aimed at obtaining M3 nanomolar affinity coupled with nanomolar PDE4 inhibition, which translated into anti-bronchospastic efficacy ex vivo (inhibition of rat trachea contraction) and into anti-inflammatory efficacy in vitro (inhibition of TNFα release). Among the best compounds, compound 92a achieved the goal of demonstrating in vivo efficacy and duration of action in both the bronchoconstriction and inflammation assays in rat after intratracheal administration.
A synthetic method of 3 - (3 - hydroxyphenyl) -1, 1 -dimethylurea. Intermediate and use
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Paragraph 0029; 0031; 0032; 0037; 0039; 0042; 0044, (2021/11/19)
The invention discloses 3 - (3 - hydroxyphenyl) -1, 1 -dimethylurea synthesis method, an intermediate and application thereof, and uses m-aminophenol as a raw material to generate HDMS, 3 - 1 dimethyl 1 (- trimethylsilyl phenyl) urea under catalysis -3 -
HETEROARYL DERIVATIVES
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Paragraph 0474; 0475; 0476, (2015/06/17)
Compounds of formula (I) described herein are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
HETEROARYL DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES
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Page/Page column 103, (2015/06/18)
The invention relates to novel compounds of formula (I) which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
PHENYLETHYLPYRIDINE DERIVATIVES AS PDE4-INHIBITORS
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Page/Page column 174, (2014/06/24)
The invention relates to novel compounds which are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
NOVEL COMPOUNDS
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Page/Page column, (2014/06/23)
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstru
Silica triflate as a new, efficient, and reusable reagent for the chemoselective silylation of alcohols and phenols and deprotection of silyl ethers
Shirini,Marjani,Nahzomi, H. Taherpour,Zolfigol
, p. 168 - 177 (2008/12/22)
Silica triflate was easily prepared via reaction of silica gel and trifluoromethane sulfonyl chloride at room temperature. This compound can be employed as an efficient and reusable reagent for the chemoselective silylation of alcohols and phenols in solution and under solvent-free conditions. This reagent also effectively catalyzed the deprotection of silyl ethers in refluxing methanol.
Tungstophosphoric acid (H3PW12O40) as a heterogeneous inorganic catalyst. Activation of hexamethyldisilazane (HMDS) by tungstophosphoric acid for efficient and selective solvent-free O-silylation reactions
Firouzabadi, Habib,Iranpoor, Nasser,Amani, Kamal,Nowrouzi, Farhad
, p. 2601 - 2604 (2007/10/03)
The role of tungstophosphoric acid (H3PW12O40) as heterogeneous organic catalysts was discussed. Activation of hexamethyldisilazane by tungstophosphoric acid for efficient and selective solvent-free O-silylation reactions
Process for the preparation of isocyanates and their use for the preparation of polyisocyanates containing ester
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, (2008/06/13)
This invention relates to a novel process for the preparation of isocyanates containing silylated alcoholic or phenolic hydroxyl groups as substituents and to the use of the compounds obtained by this process as reactants for isocyanatocarboxylic acid halides in the preparation of polyisocyanates containing ester groups.
