cas 84647-20-1, 2-AMINO-6-METHYL-NICOTINONITRILE

Articles about 84647-20-1Total 12 be found

POLYCYCLIC AMIDES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
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Page/Page column 19

(2019/05/15)

Method for producing 2-amino-6-methylnicotinic acid
The present invention provides a method for producing 2-amino-6-methylnicotinic acid represented by formula [I], wherein the production method comprises: (a) reacting 2-chloro-3-cyano-6-methylpyridine represented by formula [II] in an ammonia aqueous solution to obtain a reaction solution containing 2-amino-6-methylnicotinamide represented by formula [III]; and (b) removing the ammonia from the reaction solution, then reacting the 2-amino-6-methylnicotinamide represented by formula [III] with a base to produce 2-amino-6-methylnicotinic acid represented by formula [I].
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Paragraph 6; 7

(2017/02/02)

2-Aminonicotinic acid 1-oxides are chemically stable inhibitors of quinolinic acid synthesis in the mammalian brain: A step toward new antiexcitotoxic agents
3-Hydroxyanthranilic acid 3,4-dioxygenase (3-HAO) is the enzyme responsible for the production of the neurotoxic tryptophan metabolite quinolinic acid (QUIN). Elevated brain levels of QUIN are observed in several neurodegenerative diseases, but pharmacological investigation on its role in the pathogenesis of these conditions is difficult because only one class of substrate-analogue 3-HAO inhibitors, with poor chemical stability, has been reported so far. Here we describe the design, synthesis, and biological evaluation of a novel class of chemically stable inhibitors based on the 2-aminonicotinic acid 1-oxide nucleus. After the preliminary in vitro evaluation of newly synthesized compounds using brain tissue homogenate, we selected the most active inhibitor and showed its ability to acutely reduce the production of QUIN in the rat brain in vivo. These findings provide a novel pharmacological tool for the study of the mechanisms underlying the onset and propagation of neurodegenerative diseases.
Vallerini, Gian Paolo,Amori, Laura,Beato, Claudia,Tararina, Margarita,Wang, Xiao-Dan,Schwarcz, Robert,Costantino, Gabriele
p. 9482 - 9495
(2014/01/06)

DERIVATIVES OF NICOTINIC ACID N-OXIDE, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF ENZYME 3-HYDROXYANTHRANILATE-3, 4-DIOXYGENASE
A derivative of nicotinic acid N-oxide is described having formula (I): that acts as inhibitor of enzyme 3-hydroxyanthranilate-3,4-dioxygenase (3HAO), and is thus able to reduce QUIN biosynthesis in vivo under excitotoxic or pathological conditions, said compound being at the same time also chemically stable towards auto-oxidation.
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Paragraph 0052

(2013/11/06)

Novel Hepatitis C virus replicon inhibitors: Synthesis and structure-activity relationships of fused pyrimidine derivatives
The synthesis of several pyrido[2,3-d]pyrimidine and pyrimido[4,5-d] pyrimidine analogs is described with one such analog possessing subnanomolar potency in both genotype 1a and 1b cell culture HCV replicon assays.
Chris Krueger,Madigan, Darold L.,Beno, David W.,Betebenner, David A.,Carrick, Robert,Green, Brian E.,He, Wenping,Liu, Dachun,Maring, Clarence J.,McDaniel, Keith F.,Mo, Hongmei,Molla, Akhteruzzaman,Motter, Christopher E.,Pilot-Matias, Tami J.,Tufano, Michael D.,Kempf, Dale J.
scheme or table
p. 2212 - 2215
(2012/04/18)

DERIVATIVES OF NICOTINIC ACID N-OXIDE, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF ENZYME 3-HYDROXYANTHRANILATE-3,4-DIOXYGENASE
A derivative of nicotinic acid N-oxide is described having formula (I): that acts as inhibitor of enzyme 3-hydroxyanthranilate-3,4-dioxygenase (3HAO), and is thus able to reduce QUIN biosynthesis in vivo under excitotoxic or pathological conditions, said compound being at the same time also chemically stable towards auto-oxidation.
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Page/Page column 10-11

(2012/08/07)

Triselenium dicyanide (TSD) as a new cyanation reagent: Synthesis of cyano pterins and quinoxalines along with library of cyano N-heterocyclic compounds
Triselenium dicynide (TSD) has been reported for the first time to be a novel cyanation reagent for the microwave-assisted one-pot synthesis of a series of various types of cyano N-heterocycles such as pterin, deazapterin, quinoxaline, naphthyridine, and
Goswami, Shyamaprosad,Maity, Annada C.,Das, Nirmal K.,Sen, Debabrata,Maity, Sibaprasad
experimental part
p. 407 - 415
(2009/05/30)

ANTI-VIRAL COMPOUNDS
Compounds effective in inhibiting replication of Hepatitis C virus ( HCV ) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, coformulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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Page/Page column 60

(2008/12/08)

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors
Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mice with xenografted HCT-116 tumors were dosed with 1 ('N3′-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride), an analog of thiamine, the co-factor of transketolase. Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes α-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase. Synthesis and SAR of transketolase inhibitors is described.
Thomas, Allen A.,Le Huerou,De Meese,Gunawardana, Indrani,Kaplan, Tomas,Romoff, Todd T.,Gonzales, Stephen S.,Condroski, Kevin,Boyd, Steven A.,Ballard, Josh,Bernat, Bryan,DeWolf, Walter,Han, May,Lee, Patrice,Lemieux, Christine,Pedersen, Robin,Pheneger, Jed,Poch, Greg,Smith, Darin,Sullivan, Francis,Weiler, Solly,Wright, S. Kirk,Lin, Jie,Brandhuber, Barb,Vigers, Guy
p. 2206 - 2210
(2008/12/20)

ANTI-VIRAL COMPOUNDS
Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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Page/Page column 77-78

(2010/11/27)

Synthesis of substituted 2-aminonicotinonitriles
Mono-, di-, and trisubstituted 2-aminonicotinonitriles 8, 13, 14, and 19 are prepared from ketonic Mannich-bases hydrochlorides 4 · HCl, enones 12, β-aminovinylketones 17, 3-aminoacroleines 18, vinamidinium perchlorates 21, and 3,3-diaminoacrylonitrile (3
Troschutz,Dennstedt
p. 33 - 40
(2007/10/02)