Mirogabalin for diabetic neuropathy
Larry H. Bernstein, MD, FCAP, Curator
LPBI
Mirogabalin |
Originator |
Daiichi Sankyo
|
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Therapeutic Claim |
Treatment of fibromyalgia
|
Phase III clinical trials at Daiichi Sankyo for the treatment of pain associated with fibromyalgia
Class |
Analgesic drugs (small molecules)
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Mechanism of action |
CACNA2D1 protein modulators
|
Mirogabalin (DS-5565) is a drug developed by Daiichi Sankyo and related to drugs such as gabapentin and pregabalin. Similarly to these drugs, mirogabalin binds to the α2δ calcium channels (1 and 2), but with significantly higher potency than pregabalin. It has shown promising results in Phase II clinical trials for the treatment of diabeticperipheral neuropathic pain,[1][2] and is currently in Phase III trials.
Mirogabalin, a voltage-dependent calcium channel subunit alpha-2/delta-1 ligand, is in phase III clinical trials at Daiichi Sankyo for the treatment of pain associated with fibromyalgia. The company is also conducting phase III clinical studies for the treatment of chronic pain and pain associated with diabetic peripheral neuropathy.
PATENTS
WO 2009041453
https://www.google.co.in/patents/EP2192109A1
JP 2010241796
WO 2012169475
WO 2012169474
https://patentscope.wipo.int/search/en/detail.jsf
In the present invention, compounds having formula (IX) prepared via the process F from Step A (and / or its enantiomer) may be very produced as pure compounds. Compounds of formula (IX) which can be obtained by the present invention typically have a quality below.


The internal standard substance in a magnetic resonance spectra (NMR), and using tetramethylsilane and abbreviations indicate the multiplicity, s = singlet, d = doublet, t = triplet, q = quartet, m = multiplet, and brs = It shows a broad singlet.
In the name of the compound, “R” and “S” indicate the absolute configuration at the asymmetric carbon. Furthermore, “RS” and “SR” indicates that the asymmetric carbon atom is racemic. In addition, “(1RS, and 5SR) -” if such a can shows the relative arrangement of the 1-position and the 5-position, as well shows only one of the diastereomers, its diastereomers are racemic We show that.
In the name of the compound, “E” and “Z” indicates the arrangement of positional isomers in the structure of the compound having a position isomerism.
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