56680-75-2Relevant academic research and scientific papers
ION CHANNEL MODULATORS
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Paragraph 0261; 0266, (2021/06/11)
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
Mutual kinetic resolution of 3-methyl-3,4-dihydro-2H-1,4-benzoxazines and 2-alkoxyacyl chlorides
Vakarov, Sergey A.,Gruzdev, Dmitry А.,Sadretdinova, Liliya Sh.,Kodess, Mikhail I.,Tumashov, Andrey A.,Gorbunov, Evgeny B.,Levit, Galina L.,Krasnov, Victor P.
, p. 437 - 446 (2018/06/14)
[Figure not available: see fulltext.] Stereoselective acylation of racemic 3-methyl-3,4-dihydro-2Н-1,4-benzoxazine and its 7,8-difluoro-substituted analog with racemic 2-alkoxyacyl chlorides was stidied. The reactions of 3-methyl-3,4-dihydro-2H-1,4-benzoxazines with 2-methoxyisopentanoyl chloride were found to be more selective (selectivity factor s 31–32) compared to the acylation with other studied propanoyl chlorides (s 18–21). This fact was probably caused by the significant steric hindrance due to the isopropyl substituent in acyl chloride compared to the methyl group in reagents derived from propanoic acid.
FUNGICIDAL COMPOSITIONS
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Page/Page column 104, (2018/10/25)
A fungicidal composition comprising a mixture of components (A) and (B), wherein components (A) and (B) are as defined in claim 1, and use of the compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
METABOTROPIC GLUTAMATE RECEPTORS 5 MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 99, (2012/12/13)
Compounds that modulate GluR5 activity and methods of using the same are disclosed.
Investigation of solvolysis kinetics of new synthesized fluocinolone acetonide C-21 esters-an in vitro model for prodrug activation
Markovic, Bojan D.,Dobricic, Vladimir D.,Vladimirov, Sote M.,Cudina, Olivera A.,Savic, Vladimir M.,Karljikovic-Rajic, Katarina D.
body text, p. 2658 - 2671 (2011/05/08)
In this study the solvolysis of newly synthesized fluocinolone acetonide C-21 esters was analysed in comparison with fluocinonide during a 24-hour period of time. The solvolysis was performed in an ethanol-water (90:10 v/v) mixture using the excess of NaHCO3. The solvolytic mixtures of each investigated ester have been assayed by a RPHPLC method using isocratic elution with methanol-water (75:25 v/v); flow rate 1 mL/min; detection at 238 nm; temperature 25 °C. Solvolytic rate constants were calculated from the obtained data. Geometry optimizations and charges calculations were carried out by Gaussian W03 software. A good correlation (R = 0.9924) was obtained between solvolytic rate constants and the polarity of the C-O2 bond of those esters. The established relation between solvolytic rate constant (K) and lipophilicity (cLogP) with experimental anti-inflammatory activity could be indicative for topical corticosteroid prodrug activation.
PYRROLE ANTIFUNGAL AGENTS
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Page/Page column 79, (2009/12/05)
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
1,3-THIAZOLE-5-CARBOXAMIDES USEFUL AS CANCER CHEMOTHERAPEUTIC AGENTS
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Page/Page column 41-42, (2008/06/13)
This invention relates to novel 1, 3- thiazole-5 -carboxamide compounds of formula (I), pharmaceutical compositions containing such compounds, and the use of those compounds or compositions as cancer chemotherapeutic agents.
2-AMINOARYLCARBOXAMIDES USEFUL AS CANCER CHEMOTHERAPEUTIC AGENTS
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Page/Page column 50, (2010/02/15)
A compound having the formula (1) in which the ring containing E is a phenyl, a pyridine, or a pyrimidine. In formula (1) the symbol A represents (see structures) wherein the group R4 represents halogen, CF3, or H, provided that the maximum number of CF3 groups on any A is 2, and the maximum number of hydrogens on A is 2 for the A groups which together with the carbon atoms to which they are attached form 6-membered rings, and the maximum number of hydrogens on A is 1 for the A group which together with the carbon atoms to which it is attached forms a 5-membered ring. Z represents N or CH when E forms a phenyl ring, and represents CH when E forms a pyridine or pyrimidine. The groups R1, R2 and R3 and the subscripts a, b, and d are as defined in the text and claims. Pharmaceutical compositions containing a compound of formula (1) and methods of treating cancer using compounds of formula (1) are also disclosed and claimed.
1-METHYL-1H-PYRAZOLE-4-CARBOXAMIDES USEFUL AS CANCER CHEMOTHERAPEUTIC AGENTS
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Page/Page column 47, (2010/11/25)
This invention relates to novel 1 -Methyl- lH-pyrazole-4-carboxamide compounds, pharmaceutical compositions containing such compounds, and the use of those compounds or compositions as cancer chemotherapeutic agents.
Esters of alkoxy-acylderivatives of carnitine and pharmaceutical compositions containing same
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, (2008/06/13)
A novel class of esters of alkoxy-acylderivatives of carnitine, wherein the alkoxy-acyl radical has from 3 to 6 carbon atoms (typically: methoxyacetyl, methoxypropionyl, ethoxyacetyl, ethoxypropionyl and propoxyacetyl) is prepared by esterifying carnitine and then acylating the carnitine ester. Such esters are therapeutically useful in the treatment of cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias.
