- Synthesis of imidazole-activated ribonucleotides using cyanogen chloride
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We report the syntheses of ribonucleoside 5′-monophosphates activated with imidazole, using a mechanism which relies on the in situ generation of cyanogen chloride from the reaction of cyanide anion with hypochlorous acid. Cyanogen chloride reacts rapidly with imidazole to form diimidazole imine as the major product, a species which affords the activation of ribonucleoside 5′-monophosphates to their 5′-phosphorimidazolides.
- Yi, Ruiqin,Hongo, Yayoi,Fahrenbach, Albert C.
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Read Online
- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Paragraph 0910-0911
(2019/05/15)
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- REDUCTION OF PRO-INFLAMMATORY HDL USING A LEUKOTRIENE INHIBITOR
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A method involving the administration of a therapeutically effective amount of a leukotriene inhibitor, a pharmaceutically acceptable salt, a pharmaceutically acceptable N-oxide, a pharmaceutically active metabolite, a pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate thereof to a human for reducing a level of pro-inflammatory HDL in the human. Various examples of leukotriene inhibitors, including 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin- 3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2, 2-dimethyl-propionic acid, are disclosed for administration for the reduction of pro-inflammatory HDL in a human. Reduction of pro-inflammatory HDL by the leukotriene inhibitor may include conversion of at least a portion of pro-inflammatory HDL to anti-inflammatory HDL.
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Paragraph 00208
(2018/09/12)
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- Synthesis of Chiral Bicyclic Guanidinium Salts using Di(imidazole-1-yl)methanimine
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A detailed account of the synthesis of chiral bicyclic guanidinium salts is presented. This work represents the first systematic investigation of an approach toward the challenging target molecules via a key guanylation step employing di(imidazole-1-yl)methanimine (6) followed by a two-fold cyclization, which resulted in guanidinium salts 8 and 10. Factors governing the regioselectivity of the final cyclization step are discussed based on further data obtained in the course of the attempted syntheses of two additional bicyclic guanidinium salts.
- Turo?kin, Aleksej,Honeker, Roman,Raven, William,Selig, Philipp
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p. 4516 - 4529
(2016/07/06)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0507; 0508
(2018/10/03)
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- Probing the importance of π-stacking interactions in DNA-templated self-assembly of bisfunctionalized guanidinium compounds
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Bisfunctionalized guanidinium compounds displaying aromatic side groups of varying size are shown to self-assemble in aqueous solution with single-stranded DNA through phosphodiester backbone recognition. Competition experiments indicate the importance of
- Paolantoni, Delphine,Rubio-Magnieto, Jenifer,Cantel, Sonia,Martinez, Jean,Dumy, Pascal,Surin, Mathieu,Ulrich, Sbastien
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supporting information
p. 14257 - 14260
(2015/02/19)
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- Amido Compounds
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Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
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Page/Page column 35
(2012/06/18)
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- MEXILETINE PRODRUGS
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The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse G1 side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.
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Page/Page column 66; 68
(2012/07/13)
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- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 149
(2010/11/04)
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- HETEROCYCLIC MODULATORS OF PKB
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The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 91-92
(2009/03/07)
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- A novel synthesis of chiral guanidinium receptors and their use in unfolding the energetics of enantiorecognition of chiral carboxylates
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(Chemical Equation Presented) A novel synthetic route to the versatile chiral bicyclic guanidinium building block is described making use of L-methionine as a starting material from the natural chiral pool. Furthermore, the synthetic elaboration of this building block is shown in the construction of macrocyclic and open chain hosts, respectively. The host design employs urea functions as the connecting units and supplementary anchor groups for the complexation of anions. The binding studies of these hosts with various chiral and achiral oxoanions are performed by isothermal titration calorimetry. A trend analysis of the binding energetics in an ensemble of structurally similar guests discloses the importance of geometrical confinement of the guest. Association entropy rather than free energy (affinity) is identified as an indicator of structural uniqueness needed to distinguish configurational isomers in the recognition of enantiomeric carboxylates by the chiral guanidinium hosts.
- Jadhav, Vinod D.,Schmidtchen, Franz P.
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p. 1077 - 1087
(2008/09/18)
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- NOVEL HETEROARYL-SUBSTITUTED ARYLAMINOPYRIDINE DERIVATIVES AS MEK INHIBITORS
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The invention provides novel heteroaryl-substituted arylaminopyridine derivative MEK inhibitors of Formula (Ia) Formula (Ia) Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds
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Page/Page column 38
(2008/06/13)
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- 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS
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Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
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Page/Page column 65
(2008/06/13)
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- Formation of nitrogen-containing heterocycles using di(imidazole-1-yl)methanimine
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A mild and efficient synthesis of five- and six-membered nitrogen containing heterocyclic compounds, in which di(imidazole-1-yl)methanimine serves as a one-carbon source, is reported.
- Wu, Yong-Qian,Limburg, David C.,Wilkinson, Douglas E.,Hamilton, Gregory S.
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p. 191 - 193
(2007/10/03)
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- Direct synthesis of guanidines using di(imidazole-1-yl)methanimine
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A direct synthetic approach to guanidine compounds is reported here using di(imidazole-1-yl)methanimine and di(imidazole-1-yl)cyanomethanimine as guanylating reagents.
- Wu, Yong-Qian,Hamilton, Sean K.,Wilkinson, Douglas E.,Hamilton, Gregory S.
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p. 7553 - 7556
(2007/10/03)
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