142818-01-7Relevant academic research and scientific papers
Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor
Raeppel, Stéphane L.,Raeppel, Franck,Therrien, Eric
, p. 2527 - 2531 (2015/06/02)
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.
Synthesis and antifungal activity of n-(substituted pyridinyl)- 1-methyl(phenyl)-3-(trifluoromethyl)-1h-pyrazole-4- carboxamide derivatives
Wu, Zhibing,Hu, Deyu,Kuang, Jiqing,Cai, Hua,Wu, Shixi,Xue, Wei
, p. 14205 - 14218 (2013/02/26)
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.
Inhibitors of Diacylglycerol Acyltransferase
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, (2010/06/22)
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.
Novel acyl coenzyme A (CoA): Diacylglycerol acyltransferase-1 inhibitors: Synthesis and biological activities of diacylethylenediamine derivatives
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
experimental part, p. 2785 - 2795 (2010/07/04)
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
DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
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, (2009/01/20)
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.
AMIDE COMPOUNDS
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Page/Page column 134-135, (2008/06/13)
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
AMIDE COMPOUNDS
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Page/Page column 270-271, (2008/06/13)
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
Diacylglycerol acyltransferase inhibitors
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Page/Page column 29, (2010/11/27)
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.
AMIDE COMPOUND
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, (2008/06/13)
The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.
AMIDE COMPOUND
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Page/Page column 175-176, (2008/06/13)
Disclosed is a compound represented by the formula (I) or (II) below, or a salt thereof. [In the formulae, ring A represents an optionally substituted ring (which is not a pyrrolidine, piperidine or piperazine); ring B represents an optionally substituted aromatic ring; ring D represents an optionally substituted ring; R1 and R2 independently represent a hydrogen atom or a substituent; R3 represents a hydrogen atom or a C1-6 alkyl group, or alternatively it combines with the ring A to form a non-aromatic ring; ring Aa represents an optionally substituted aromatic hydrocarbon; Y represents CH or N; Ra1 represents an optionally substituted hydrocarbon group; and Ra2 and Ra3 independently represent a hydrogen atom or a substituent.] The compound has a DGAT inhibitory effect and is useful for treatment or improvement of diseases or conditions caused by high expression or high activation of DGAT.
