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Voltage-gated sodium channel blockers

A phenyl and viral technology, applied in antiviral agents, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as unknown mechanisms

Inactive Publication Date: 2014-04-30
GLAXO GRP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite extensive research, the mechanism is still unknown

Method used

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  • Voltage-gated sodium channel blockers
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  • Voltage-gated sodium channel blockers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[1583] 1-methylethyl 2-{4-[(5-ethyl-2-thienyl)methyl]-1-piperazinyl}-3-pyridinecarboxylate

[1584]

[1585] LC-MS m / z374.2(M+H) + , 1.94 minutes (retention time); 1 H NMR (400MHz, CDCl 3 )δ8.26-8.24(m,1H),7.94-7.91(m,1H),6.74-6.61(m,3H),5.19-5.16(m,1H),3.72(s,2H),3.48-3.46( m,4H),2.82(q,J=7.6,14.8Hz,2H),2.64-2.63(m,4H),1.35(d,J=6.4Hz,6H),1.30(t,J=7.6Hz,3H ).

Embodiment 2

[1587] 1-methylethyl 2-{4-[(4,5-dimethyl-2-thienyl)methyl]-1-piperazinyl}-3-pyridinecarboxylate

[1588]

[1589] LC-MS m / z374.2(M+H) + , 1.93 minutes (retention time); 1 H NMR (400MHz, CDCl 3 )δ8.26-8.24(m,1H),7.94-7.91(m,1H),6.72-6.69(m,1H),6.60(s,1H),5.19-5.16(m,1H),3.64(s, 2H),3.46(t,J=5.2Hz,4H),2.59(t,J=5.2Hz,4H),2.30(s,3H),2.08(s,3H),1.34(d,J=6.4Hz, 6H).

Embodiment 3

[1591] 1-methylethyl 2-{4-[(4-ethylphenyl)methyl]-1-piperazinyl}-3-pyridinecarboxylate

[1592]

[1593] LC-MS m / z368.2(M+H) + , 2.23 minutes (retention time); 1 H NMR (400MHz, CDCl 3)δ8.27-8.24(m,1H),7.93-7.90(m,1H),7.27-7.15(m,4H),6.72-6.69(m,1H),5.19-5.16(m,1H),3.55( s,2H),3.45(t,J=4.8Hz,4H),2.67-2.61(q,J=7.6,14.8Hz,2H),2.58(t,J=4.8Hz,4H),1.33(d,J =6.4Hz, 6H), 1.23(t, J=7.6Hz, 3H).

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Abstract

In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.

Description

field of invention [0001] In general, the present invention relates to the use of voltage-gated sodium channel blocker compounds, said compounds including corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, methods for the preparation of the compounds, and therapeutic Respiratory disease or respiratory disease method. [0002] In particular, the present invention also relates to methods and uses for the treatment of respiratory or respiratory diseases comprising administering to a subject in need thereof an effective amount of a compound of the present invention. Background of the invention [0003] By rapidly transmitting electrical impulses throughout cells and cellular networks, sodium channels play an important role in neural networks that help coordinate higher processes in mammals, from movement to cognition. [0004] Sodium channels are generally described in the prior art as large transmembrane proteins that can s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/497
CPCC07D401/14C07D401/12C07D405/14C07D409/12C07D213/80C07D409/14A61K31/497A61P11/14A61P31/00A61P31/12A61P43/00
Inventor J.C.博姆R.S.戴维斯J.科恩斯林国良R.D.默多科聂红
Owner GLAXO GRP LTD