770-00-3Relevant articles and documents
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.
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
Studies on pyrazines; 21. A convenient synthesis of pyrazinecarboxylic acid derivatives from chloropyrazines
Takeuchi,Suzuki,Sato
, p. 923 - 924 (2007/10/02)
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