24922-00-7Relevant articles and documents
ALCOHOL DERIVATIVES AS KV7 POTASSIUM CHANNEL OPENERS
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Paragraph 0385-0386; 0392-0393, (2021/02/05)
The present invention provides novel compounds which activate the Kv7 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders responsive to the activation of Kv7 potassium channels.
Modular Tuning of Electrophilic Reactivity of Iridium Nitrenoids for the Intermolecular Selective α-Amidation of β-Keto Esters
Lee, Minhan,Jung, Hoimin,Kim, Dongwook,Park, Jung-Woo,Chang, Sukbok
, p. 11999 - 12004 (2020/08/06)
We report herein an Ir-catalyzed intermolecular amino group transfer to β-keto esters (amides) to access α-aminocarbonyl products with excellent chemoselectivity. The key strategy was to engineer electrophilicity of the putative Ir-nitrenoids by tuning electronic property of the κ2-N,O chelating ligands, thus facilitating nucleophilic addition of enol π-bonds of 1,3-dicarbonyl substrates.
BIARYL PYRAZOLES AS NRF2 REGULATORS
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Page/Page column 156; 157, (2017/08/01)
The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
GLYCINE B ANTAGONISTS
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Page/Page column 67-68, (2010/12/29)
The invention relates to pyrazolopyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.
CuSO4-catalyzed diazo decomposition in water: a practical synthesis of β-keto esters
Liao, Mingyi,Wang, Jianbo
, p. 8859 - 8861 (2007/10/03)
CuSO4 was found to be an efficient catalyst for the diazo decomposition of β-hydroxy α-diazoesters in water. 1,2-H shift occurred efficiently to give β-keto esters in high yields. No O-H bond insertion products were identified.
A3 adenosine receptor antagonists
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, (2008/06/13)
Disclosed are pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of selectively blocking an A3adenosine receptor of a mammal by the use of one or more of these derivatives. An example of the pyridine derivative is of the formula (I): wherein R2is ethyl, R3is ethylsulfanyl; R4is ethyl, propyl, or hydroxypropyl; R5is ethyl, propyl, fluoroethyl, or fluoropropyl; and R6is phenyl or fluorophenyl. The derivatives of the present invention can be used for inhibiting binding of ligands to an adenosine receptor. The derivatives also can be used for characterizing an adenosine receptor.
ARYL PYRIMIDINE DERIVATIVES
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, (2008/06/13)
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT 2B-antagonists. The invention is also directed to formulations and methods for treatment.
ARYL PYRIMIDINE DERIVATIVES
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, (2008/06/13)
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists.
ARYL PYRIMIDINE DERIVATIVES AND USES THEREOF
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, (2008/06/13)
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists. The 5-HT 2B antagonist is a compound of the formula: STR1 wherein: R. sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl,--NR 6 R. sup.7,--CO 2 R 8,--O(CH 2) n R 9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in which n is 1, 2, or 3;R 6 and R 7 are hydrogen or lower alkyl; R 8 is hydrogen or lower alkyl; andR 9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R. sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl; R 3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R 4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl,--(CH 2) m NR. sup.10 R 11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, alkoxy carbonyl, tetrahydrofuran-2-yl, hydroxyalkoxy, or sulfonamido;in whichR 10 and R. sup.11 are hydrogen or lower alkyl; andR 5 is hydrogen or lower alkyl; provided that: (i) when R 3 is naphthyl, indol-1-yl, or 2,3-dihydroindol-1-yl, and R 2, R 4 and R 5 are all hydrogen, R. sup.1 is not methyl; (ii) when R 3 is phenyl or naphthyl, R 1 is not--NR 6 R 7 ;(iii) when R 3 is phenyl, R 2 is not lower alkoxy, and R 1 and R 2 are not halo;(iv) when R 3 is phenyl and R 1 is H, R 2 is not methyl; and (v) when R 3 is 1,2,3,4-tetrahydroquinolinyl, R 4 and R. sup.5 are hydrogen;or a pharmaceutically acceptable salt or N-oxide thereof.
