770-00-3Relevant academic research and scientific papers
INHIBITORS OF COLLAGEN PROLYL 4-HYDROXYLASE
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Paragraph 0190; 0191; 0192, (2016/10/17)
Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R1 and R2 independently are —OR7, or —NHSO2R8, where R7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R′—CO—R″, —R′—CO—O—R″, —CO—R″, —R′—O—CO—R″, —R′—CO—NR″, —CO—NR″, or —R′—O—CO—NR″, and R8 is selected from hydrogen, alkyl, aryl, arylalkyl; R3, R4 and R6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, halo alkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R′— is a divalent straight chain or branched alkylene, and —R″ is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as Potent α4β2 nicotinic acetylcholine receptor ligands
Scanio, Marc J. C.,Shi, Lei,Bunnelle, William H.,Anderson, David J.,Helfrich, Rosalind J.,Malysz, John,Thorin-Hagene, Kirsten K.,Van Handel, Ceclia E.,Marsh, Kennan C.,Lee, Chih-Hung,Gopalakrishnan, Murali
experimental part, p. 7678 - 7692 (2012/01/06)
A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the α4β2 neuronal nicotinic acetylcholine receptor (nAChR). The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the α4β2 nAChR, with limited agonist activity. Carboxamide derivatives of 3-(diazabicyclo[3.3.0] octane)-substituted pyridines or 2-(diazabicyclo[3.3.0]octane)-substituted pyrazines were found to have the desired binding and activity profile. The structure-activity relationship of these compounds is presented.
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Nav1.8 sodium channel with efficacy in a model of neuropathic pain
Scanio, Marc J.C.,Shi, Lei,Drizin, Irene,Gregg, Robert J.,Atkinson, Robert N.,Thomas, James B.,Johnson, Matthew S.,Chapman, Mark L.,Liu, Dong,Krambis, Michael J.,Liu, Yi,Shieh, Char-Chang,Zhang, Xufeng,Simler, Gricelda H.,Joshi, Shailen,Honore, Prisca,Marsh, Kennan C.,Knox, Alison,Werness, Stephen,Antonio, Brett,Krafte, Douglas S.,Jarvis, Michael F.,Faltynek, Connie R.,Marron, Brian E.,Kort, Michael E.
experimental part, p. 7816 - 7825 (2011/02/22)
Nav1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons. It has been implicated in the pathophysiology of inflammatory and neuropathic pain, a
Selective Ligands for the Neuronal Nicotinic Receptors and Uses Thereof
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Page/Page column 10, (2009/12/04)
The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the α4β2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.
Studies on Pyrazines. 9. The Facile Synthesis of Pyrazine 1-Oxides Substituted at C-2 with Cyano, Methoxycarbonyl and Carboxy Groups
Sato, Nobuhiro
, p. 169 - 171 (2007/10/02)
The peroxysulfuric acid oxidation of 2-cyanopyrazine (1) gave its 1-oxide 3 (18percent yield) and pyrazinecarboxamide (8percent yield), while that of methyl pyrazinecarboxylate (2) provided the 1- and 4-oxides in 15 and 7percent yields, respectively.On the other hand, pyrazinecarboxylic acid 1-oxide (7) was prepared by condensation of 2-methylpyrazine 1-oxide (8) with benzaldehyde followed by oxidative cleavage (47percent overall yield).
