- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Paragraph 0192
(2016/10/06)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula(I) or a pharmaceutically acceptable salt thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure, kidney disease, edema, and conditions associated with excessive salt and water retention.
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Page/Page column 54
(2014/09/03)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Page/Page column 83
(2013/03/26)
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- Selective nitration of phenols using bismuth subnitrate/charcoal in the presence of trichloroisocyanuric acid under aprotic conditions
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A mild, efficient and regioselective method for the mononitration of phenolic compounds is described using bismuth subnitrate/charcoal in the presence of trichloroisocyanuric acid in CH2Cl2 at room temperature.
- Pourali, Ali Reza,Fatemi, Fatemeh
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experimental part
p. 1283 - 1286
(2011/10/05)
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- Hydroxylation of Nitroarenes with Alkyl Hydroperoxide Anions via Vicarious Nucleophilic Substitution of Hydrogen
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tert-Butyl and cumyl hydroperoxides in strongly basic media react with a variety of nitroarenes to produce o- and/or p-nitrophenols.The reaction proceeds via an addition-base-induced β-elimination pathway analogous to that of vicarious nucleophilic substitution.
- Makosza, Mieczyslaw,Sienkiewicz, Krzysztof
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p. 4979 - 4981
(2007/10/02)
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- Formation of 4-Halo-4-nitrocyclohexa-2,5-dienones on Nitration of p-Halophenols and p-Halophenyl Acetates.
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Nitration of p-chloro-, p-fluoro-, and p-bromo-phenol or the corresponding p-halophenyl acetates at -40 deg C and below gives the 4-halo-4-nitrocyclohexa-2,5-dienones in addition to the 4-halo-2-nitrophenols.The dienones isomerize to the nitrophenols at temperatures between -40 deg C and 0 deg C.Nitration of 4-chloro-2-methylphenol or its acetate gives both 4-chloro-2-methyl-4-nitrocyclohexa-2,5-dienone and 4-chloro-6-methyl-6-nitrocyclohexa-2,4-dienone. 4-Chloro-3-methylphenol and its acetate give 4-chloro-3-methyl-4-nitrocyclohexa-2,5-dienone.
- Clewley, Robin G.,Cross, Gordon G.,Fischer, Alfred,Henderson, George N.
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p. 1299 - 1310
(2007/10/02)
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- Certain 3,5-disubstituted-2-pyridyloxy-fluorophenoxy-alkanoic acids, derivatives thereof and herbicidal properties
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Certain novel fluorophenoxy compounds, principally aryloxyfluorophenoxyalkanoic acids and derivatives thereof, are described. More specifically, these novel compounds bear 1 to 4 fluorine substituents on the phenyl ring. These novel compounds exhibit surprising preemergent and postemergent activity when used according to the method of the invention in the control of grassy weeds.
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- Etude des complexes du cobalt (II) transporteurs d'oxygene: Nouvelle synthese du fluoro-3 hydroxy-2 benzaldehyde
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Synthetic chelates of cobalt (II) derived from Schiff bases have remarkable behavior of reversibly absorbing and releasing molecular oxygene.Among these, bis (3-fluorosalicylaldehydeethylenediimide) Co (II) (fluomine: Formula A, X=F) is most interesting in allowing to isolate pure oxygen from air, because it absorbs with extreme rapidity 4.43percent of its weight of oxygen.Fluomine is easily prepared from 3-fluorosalicylaldehyde (3FSA), ethylenediamine and cobalt (II) chloride; but substances such as 3-substituted salicylaldehydes have proven to be extremely difficult to prepare in other than small laboratory quantities from the corresponding ortho-substituted phenol.Many author have prepared 3-fluorosalicylaldehyde, as described in patents, but often these syntheses are very long and the yields are generally less than 20percent.We now describe a new synthesis from o-fluorophenol.Nitration of o-fluorophenol with liquid nitrogen dioxide is convenient: - on the one hand, ortho-substitution to the hydroxyl group, is easy, -on the other hand, the para substituted by-product, is reinserted in the course of the synthesis, so that it is possible to minimize loss of the starting phenol, an expensive product. o-Fluorophenol 1 in solution in pentane, at about 0 deg C, is treated with liquid nitrogen dioxide (slight excess).The reaction is rapid and leads to 2-fluoro 6-nitrophenol 2 which remains in solution, and 2-fluoro 4-nitrophenol 7 which cristallizes rapidly (approximatively 50percent of each one). 2-Fluoro 6-nitrophenol 2 is converted into the anisole 3, the NO2 group of which is catalytically reduced by hydrogen into 3-fluoro 2-methoxy-aminobenzene 4.This amine 4 is diazotized, and treated with formaldoxime to lead to 3-fluoro 2-methoxybenzaldehyde 5 (Eb12 = 82 deg C). 3FSA is finally obtained by heating under reflux anisole 5 and a solution of hydrobromic acid (48percent). 2-Fluoro 4-nitrophenol 7 is converted in five steps into 3-fluoro 2-methoxyaminobenzene 4 by the same reactions as these used for its isomer.Finally the total yield of amine 4 from o-fluorophenol is 73percent, and 3FSA is obtained in 25percent yield.No primary amines are required during the isolation, so that no possible contamination of the final product is possible and therefore the fluomine prepared therefrom is not contaminated and deactivated.
- Aymes, Daniel J.,Paris, Michel R.
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p. 175 - 178
(2007/10/02)
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