77278-77-4Relevant articles and documents
Sulfonamides incorporating piperazine bioisosteres as potent human carbonic anhydrase I, II, IV and IX inhibitors
Chiaramonte, Niccolò,Bua, Silvia,Angeli, Andrea,Ferraroni,Picchioni, Ilaria,Bartolucci, Gianluca,Braconi,Dei, Silvia,Teodori, Elisabetta,Supuran, Claudiu T.,Romanelli, Maria Novella
, (2019/08/01)
Starting from the molecular simplification of (R) 4-(3,4-dibenzylpiperazine-1-carbonyl)benzenesulfonamide 9a, a compound endowed with selectivity for human Carbonic Anhydrase (hCA) IV, a series of piperazines and 4-aminopiperidines carrying a 4-sulfamoylb
1,1,1-TRIFLUORO-3-HYDROXYPROPAN-2-YL CARBAMATE DERIVATIVES AND 1,1,1-TRIFLUORO-4-HYDROXYBUTAN-2-YL CARBAMATE DERIVATIVES AS MAGL INHIBITORS
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Page/Page column 120, (2017/02/28)
The present invention provides, in part, compounds of Formula I and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses
Novel bicyclic nitroimidazole carbamate compounds, process for preparation thereof and pharmaceutical composition for preventing or treating tuberculosis containing the same as an active ingredient
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Paragraph 0191; 0192; 0199-0201, (2021/06/01)
A bicyclic nitroimidazole carbamate compound represented by chemical formula 1, an optical isomer thereof or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition for preventing or treating tuberculosis disease containing the same as an active ingredient. Chemical Formula 1. In Chemical Formula 1, R. 1 And R2 Are as defined in the description of the invention. The bicyclic nitroimidazole carbamate compounds of the present invention exhibit excellent inhibitory effects on vitality and non-active tuberculosis. The compounds can be useful in the treatment of tuberculosis.
NOVEL BENZODIOXANE AND BENZOXAZINE DERIVATIVES USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 22, (2010/06/22)
The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo
Perez, Michel,Lamothe, Marie,Maraval, Catherine,Mirabel, Etienne,Loubat, Chantal,Planty, Bruno,Horn, Clemens,Michaux, Julien,Marrot, Sebastien,Letienne, Robert,Pignier, Christophe,Bocquet, Arnaud,Nadal-Wollbold, Florence,Cussac, Didier,De Vries, Luc,Le Grand, Bruno
experimental part, p. 5826 - 5836 (2010/03/24)
Protease activated receptors (PARs) or thrombin receptors constitute a class of G-protein-coupled receptors (GPCRs) implicated in the activation of many physiological mechanisms. Thus, thrombin activates many cell types such as vascular smooth muscle cells, leukocytes, endothelial cells, and platelets via activation of these receptors. In humans, thrombin-induced platelet aggregation is mediated by one subtype of these receptors, termed PAR1. This article describes the discovery of new antagonists of these receptors and more specifically two compounds: 2-[5-oxo-5-(4-pyridin-2-ylpiperazin-1-yl)penta-1,3- dienyl]benzonitrile 36 (F 16618) and 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl) piperazin-1-yl]propenone 39 (F 16357), obtained after optimization. Both compounds are able to inhibit SFLLR-induced human platelet aggregation and display antithrombotic activity in an arteriovenous shunt model in the rat after iv or oral administration. Furthermore, these compounds are devoid of bleeding side effects often observed with other types of antiplatelet drugs, which constitutes a promising advantage for this new class of antithrombotic agents. 2009 American Chemical Society.
CINNAMOYL-PIPERAZINE DERIVATIVES AND THEIR USE AS PAR- I ANTAGONISTS
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Page/Page column 8, (2008/06/13)
The present invention relates to compounds of general formula (I), wherein: R1 represents halogen, CN or NO2; R2 represents hydrogen or halogen; n represents 1 or 2; R3 represents phenyl substituted by one or mo