- KCNT1 INHIBITORS AND METHODS OF USE
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The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
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Paragraph 000853
(2020/11/23)
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- Hydroxymethylation of Quinolines with Na2S2O8 by a Radical Pathway
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Quinolines and isoquinolines were treated with Na2S2O8 in a mixture of methanol and water at 70 °C to form hydroxymethylated quinolines and isoquinolines in good to moderate yields, under transition-metal-free conditions. The formed hydroxymethyl group was smoothly converted into aldehyde, ester, amide, bromomethyl, (N,N-diethylamino)methyl, cyano, and tetrazole groups, in good yields.
- Zhou, Luan,Okugawa, Naoyuki,Togo, Hideo
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p. 6239 - 6245
(2017/11/15)
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- AROMATIC RING COMPOUND
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Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
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Paragraph 0406
(2015/01/18)
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- OXIME COMPOUNDS AND THE USE THEREOF
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The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CRsu
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Page/Page column 356
(2008/06/13)
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- 4-HETEROARYLMETHYL SUBSTITUTED PHTHALAZINONE DERIVATIVES
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A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRx or CRxRy; if X=NRx then n is 1 or 2 and if X=CRxRy then n is 1; Rx is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; Ry is selected from H, hydroxy, amino; or Rx and Ry may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRxRy, RC1, RC2, Rx and Ry, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: (i) formula (i), where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; and (ii) formula (ii), where Q is O or S.
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Page/Page column 46-47
(2008/06/13)
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- POTENTIATORS OF GLUTAMATE RECEPTORS
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The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.
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Page/Page column 136
(2010/11/08)
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- Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as inhibitors of viral reverse transcriptase
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The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4 is selected from the group consisitng of --H or --NR 15 R 16 where R 15 is --H and R 16 is --H, C 1 -C 6 alkyl, NH 2 or R 15 and R 16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R 6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R 4 and R 6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase. STR1
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- Process for the selective mono-ortho-hydroxyalkylation of 4-substituted pyridine derivatives
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A process is described for the selective mono-ortho-hydroxyalkylation of 4-substituted pyridine derivatives. In this case a nucleophilic hydroxyalkylation is carried out on the protonated pyridine derivative under the action of peroxodisulfate.
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- AN IMPROVED METHOD FOR THE MONO-HYDROXYMETHYLATION OF PYRIDINES. A MODIFICATION OF THE MINISCI PROCEDURE
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The reaction of N-methoxy-derivatives of pyridines in methanol with ammonium persulphate gives improved yields of mono-hydroxymethylated products.In contrast to the original Minisci procedure the reaction requires only catalytic amounts of ammonium persulphate.Evidence is presented which establishes that the reaction does not proceed via an intramolecular pathway.
- Katz, R B,Mistry, J,Mitchell, M B
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p. 317 - 326
(2007/10/02)
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- α-HYDROXYALKYLATION OF HETEROAROMATIC BASES BY ALCOHOLS AND HYDROXYLAMINE-O-SULPHONIC ACID
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The homolytic decomposition of hydroxylamine-O-sulphonic acid in alcoholic solvents was investigated in the presence or absence of protonated heteroaromatic bases and Fe(II) salt.THe addition of the α-hydroxyalkyl radicals to the base and their oxidation by Fe(III) salt to the corresponding alkyl cyanide were competitive processes.A redox chain process involving the amino radical cation NH3+, is suggested and the factors affecting the yields of the homolytic substitution are discussed.
- Citterio, Attilio,Gentile, Anna,Minisci, Francesco,Serravalle, Marco,Ventura, Susanna
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p. 617 - 620
(2007/10/02)
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- PYRIMIDONE DERIVATIVES
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This invention relates to 2-amino-4-pyrimidone derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal 4-dialkylaminomethyl-2-pyridyl group. The compounds have histamine H 2-antagonist activity. A specific compound of this invention is 2-[2-(4-dimethylaminomethyl-2-pyridylmethylthio)ethylamino]-5-(6-methyl-3-p yridylmethyl)-4-pyrimidone.
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