- PROCESS FOR THE REGIOSELECTIVE SYNTHESIS OF PYRAZOLES
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A process is described for the synthesis of pyrazoles having general formula (I) which comprises the steps of mixing a compound having general formula (II) and a 1,2-disubstituted hydrazine having general formula (III) to form a reaction intermediate having general formula (IV) and the reaction mixture obtained in step i), in an acid environment, cyclizes to form a pyrazole having general formula (I), according to reaction scheme 1 Scheme 1.
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Page/Page column 19; 20
(2015/07/15)
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- Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor
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Abstract New carboxamide head group analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent and selective inhibitors of RON enzyme versus c-Met RTK were obtained.
- Raeppel, Stéphane L.,Raeppel, Franck,Therrien, Eric
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p. 2527 - 2531
(2015/06/02)
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- Synthesis and antifungal activity of n-(substituted pyridinyl)- 1-methyl(phenyl)-3-(trifluoromethyl)-1h-pyrazole-4- carboxamide derivatives
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A series of N-(substituted pyridinyl)-1-methyl(phenyl)-3-trifluoromethyl- 1Hpyrazole- 4-carboxamide derivatives were synthesized. All target compounds were characterized by spectral data (1H-NMR, 13C-NMR, IR, MS) and elemental analysis and were bioassayed in vitro against three kinds of phytopathogenic fungi (Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results showed that some of the synthesized N-(substituted pyridinyl)-1-methyl-3- trifluoromethyl-1H-pyrazole-4-carboxamides exhibited moderate antifungal activities, among which compounds 6a, 6b and 6c displayed more than 50% inhibition activities against G. zeae at 100 μg/mL, which was better than that of the commercial fungicides carboxin and boscalid.
- Wu, Zhibing,Hu, Deyu,Kuang, Jiqing,Cai, Hua,Wu, Shixi,Xue, Wei
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p. 14205 - 14218
(2013/02/26)
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- Novel acyl coenzyme A (CoA): Diacylglycerol acyltransferase-1 inhibitors: Synthesis and biological activities of diacylethylenediamine derivatives
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A series of diacylethylenediamine derivatives were synthesized and evaluated for their inhibitory activity against DGAT-1 and pharmacokinetic profile to discover new small molecule DGAT-1 inhibitors. Among the compounds, N-[2-({[1-phenyl-3-(trifluoromethy
- Nakada, Yoshihisa,Aicher, Thomas D.,Huerou, Yvan Le,Turner, Timothy,Pratt, Scott A.,Gonzales, Stephen S.,Boyd, Steve A.,Miki, Hiroshi,Yamamoto, Toshihiro,Yamaguchi, Hiroshi,Kato, Koki,Kitamura, Shuji
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experimental part
p. 2785 - 2795
(2010/07/04)
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- Inhibitors of Diacylglycerol Acyltransferase
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Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 8
(2010/06/22)
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- DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
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Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 55
(2009/01/20)
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- AMIDE COMPOUNDS
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The present invention provides compounds represented by the formula (Ie) and the formula (If) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT
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Page/Page column 134-135
(2008/06/13)
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- AMIDE COMPOUNDS
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The present invention provides compounds represented by the formula (Ia) the formula (Ib) the formula (Ic) and the formula (Id) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibit
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Page/Page column 270-271
(2008/06/13)
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- Diacylglycerol acyltransferase inhibitors
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 29
(2010/11/27)
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- PYRAZOLE DERIVATIVES
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A compound represented by the general formula (I), which is useful as a peroxisome proliferator-activated receptor α/γ agonist, a salt of the compound, and a solvate of either. (In the formula, X, Y, and Z each represents nitrogen or carbon; m is an integ
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Page/Page column 47-48
(2010/10/19)
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- Copper-diamine-catalyzed N-arylation of pyrroles, pyrazoles, indazoles, imidazoles, and triazoles
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This paper details the copper-catalyzed N-arylation of π-excessive nitrogen heterocycles. The coupling of either aryl iodides or aryl bromides with common nitrogen heterocycles (pyrroles, pyrazoles, indazoles, imidazoles, and triazoles) was successfully performed in good yield with catalysts derived from diamine ligands and CuI. General conditions were found that tolerate functional groups such as aldehydes, ketones, alcohols, primary amines, and nitriles on the aryl halide or heterocycle. Hindered aryl halides or heterocycles were also found to be suitable substrates using the conditions reported herein.
- Antilla, Jon C.,Baskin, Jeremy M.,Barder, Timothy E.,Buchwald, Stephen L.
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p. 5578 - 5587
(2007/10/03)
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