85290-78-4Relevant academic research and scientific papers
An efficient synthesis of 1-H-pyrazole-4-carboxylic acid esters with Vilsmeier reagent under neat conditions
Sridhar,Sivaprasad,Perumal
, p. 405 - 408 (2004)
A convenient, solvent-free Vilsmeier reagent is experimented under neat condition (both thermal and microwave conditions). An efficient method for the synthesis of various substituted 1H-pyrazole-4-carboxylic acid esters is reported.
PREPARATION OF SUBSTITUTED PYRAZOLES AND THEIR USE AS ANTHRANILAMIDES PRECURSORS
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Page/Page column 18, (2020/10/28)
A method is disclosed for preparing pyrazole derivative 3-bromo- 5-methyl- 1-H- pyrazole- N-2-chloropyridine (compound of Formula I) by reacting of a compound of Formula II with halogen substituted pyridine optionally in the presence of base and organic solvent or by decarboxylation of pyrazole carboxylic acid of Formula XI in the presence of acid. In addition, provided a method of preparation of synthetic precursors of Formula II, Formula IV, Formula V, Formula VI, Formula XI, and a method of preparing a compound of Formula VII comprising reacting a compound of Formula I with an oxidant optionally in the presence of a catalyst. Also disclosed a compound of Formula I as useful synthetic precursor for preparation of anthranilamide of Formula VIII.
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 1255, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate
Sun, Jialong,Zhou, Yuanming
, p. 4383 - 4394 (2015/05/06)
A series of pyrazole carboxamide and isoxazolol pyrazole carboxylate derivatives were designed and synthesized in this study. The structures of the compounds were elucidated based on spectral data (infrared, proton nuclear magnetic resonance and mass spectroscopy). Then, all of the compounds were bioassayed in vitro against four types of phytopathogenic fungi (Alternaria porri, Marssonina coronaria, Cercospora petroselini and Rhizoctonia solani ) using the mycelium growth inhibition method. The results showed that some of the synthesized pyrazole carboxamides displayed notable antifungal activity. The isoxazole pyrazole carboxylate 7ai exhibited significant antifungal activity against R. solani, with an EC50 value of 0.37 μg/mL. Nonetheless, this value was lower than that of the commercial fungicide, carbendazol.
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7′-thieno[2,3- C ]pyran) scaffold
Toledo, Miguel A.,Pedregal, Concepción,Lafuente, Celia,Diaz, Nuria,Martinez-Grau, Maria Angeles,Jiménez, Alma,Benito, Ana,Torrado, Alicia,Mateos, Carlos,Joshi, Elizabeth M.,Kahl, Steven D.,Rash, Karen S.,Mudra, Daniel R.,Barth, Vanessa N.,Shaw, David B.,McKinzie, David,Witkin, Jeffrey M.,Statnick, Michael A.
supporting information, p. 3418 - 3429 (2014/05/20)
Nociceptin/OFQ (N/OFQ) is a 17 amino acid peptide that is the endogenous ligand for the ORL1/NOP receptor. Nociceptin appears to regulate a host of physiological functions such as biological reactions to stress, anxiety, mood, and drug abuse, in addition
SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS
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Page/Page column 11, (2011/06/10)
An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described.
SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS
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Page/Page column 24, (2011/06/16)
An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines.
PYRIDINE DERIVATIVES
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Page/Page column 151, (2009/01/20)
The present invention relates to compounds of the formula (I): (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
