224817-12-3Relevant academic research and scientific papers
ANTIMICROBIAL COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT OF INFECTIONS
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Page/Page column 33, (2016/12/22)
The present disclosure provides compositions including a compound (e.g., compounds A-D), pharmaceutical compositions including the compound, methods of treatment of a condition (e.g., an infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE DERIVATIVES AND THEIR USE AS PHD INHIBITORS
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Paragraph 0248; 0249, (2014/10/15)
The present invention provides compounds of formula (I) which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.
Lanthanum(III) triflate catalyzed direct amidation of esters
Morimoto, Hiroyuki,Fujiwara, Risa,Shimizu, Yuhei,Morisaki, Kazuhiro,Ohshima, Takashi
supporting information, p. 2018 - 2021 (2014/05/06)
Lanthanum trifluoromethanesulfonate is an effective single-component catalyst for synthesizing a variety of amides directly from esters and amines under mild conditions. Highly selective amidation of esters and amines, as well as catalyst-controlled amidation of esters, demonstrated the effectiveness of the catalyst system.
New derivatives of benzylamide with anticonvulsant activity
Strupinska, Marzanna,Rostafinska-Suchar, Grazyna,Stables, James. P.,Paruszewski, Ryszard
experimental part, p. 155 - 159 (2009/06/18)
Previously obtained picolinic acid benzylamide is a potent anticonvulsant with low neurotoxicity. In search for new effective anticonvulsants twelve new benzylamides (1-12) were synthesized and preliminary evaluated in the Anticonvulsant Screening Program (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Two of them appeared the most promising: 1- cyclopentenecarboxylic acid benzylamide (1- Cpc-BZA) (9) showed MES ED 50 = 85,36 mg/kg (PI = 2,49), scPTZ ED50 = 1,37 mg/kg (PI = 1,37), 6Hz-EST ED50 = 50,29 mg/kg and cyclopentanecarboxylic acid benzylamide (Cpc-BZA) (11) showed pilocarpine ED50 = 154.75 mg/kg and pilocarpine ED97 = 270.95 mg/kg.
Efficient synthesis of novel NK1 receptor antagonists: Selective 1,4-addition of Grignard reagents to 6-chloronicotinic acid derivatives
Hoffmann-Emery, Fabienne,Hilpert, Hans,Scalone, Michelangelo,Waldmeier, Pius
, p. 2000 - 2008 (2007/10/03)
A new efficient synthesis of two novel classes of NK1 receptor antagonists, among them befetupitant and netupitant, starting from 6-chloronicotinic acid is described. The introduction of the o-tolyl substituent at C(4) of the pyridine ring was achieved by a one-pot selective 1,4-Grignard addition/oxidation sequence to 6-chloronicotinic acid or a derivative of it. The scope of this addition/oxidation sequence was examined. It was also shown that the carboxylic function can be converted to a methyl amino group by a Hofmann rearrangement followed by reduction. Furthermore, a new high-yielding synthesis of 2-(3,5-bistrifluoromethylphenyl)-2-methyl propionic acid based on the carbonylation of the tertiary alcohol obtained by Grignard addition of 3,5-bis(trifluoromethyl)bromobenzene to acetone was established.
Process for the preparation of pyridine derivatives
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, (2008/06/13)
A process is described for preparing certain 4-alkyl- or 4-aryl-pyridine derivatives.
4-phenyl-pyridine derivatives
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, (2008/06/13)
The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.
Substituted pyridine compounds and methods of use
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, (2008/06/13)
Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF- alpha , IL-1 beta , IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
