Aryl amide derivatives of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives useful as ASK1 inhibitors, an evaluation of WO2012080735

doi:10.1517/13543776.2012.718760

Paper

Aryl amide derivatives of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives useful as ASK1 inhibitors, an evaluation of WO2012080735

Published Nov 19, 2012 · P. Norman

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Abstract

Novel 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives and their salts, compositions containing them and their use as ASK1 inhibitors in the treatment of inflammation and pain are claimed. The compounds have a broad potential utility with osteoarthritis and neuropathic pain among the likely preferred indications.

Study Snapshot

The compounds are novel ASK1 inhibitors with potential for treating inflammation and pain, particularly in osteoarthritis and neuropathic pain.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Aryl amide derivatives of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives useful as ASK1 inhibitors, an evaluation of WO2012080735

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References

Citations

Levo-corydalmine attenuates microglia activation and neuropathic pain by suppressing ASK1-p38 MAPK/NF-κB signaling pathways in rat spinal cord

Levo-corydalmine effectively reduces chronic neuropathic pain by suppressing microglia activation and the ASK1-p38 MAPK/NF-B signaling pathway in the spinal cord.

Identification of apoptosis signal-regulating kinase 1 (ASK1) inhibitors among the derivatives of benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one.

The novel chemical class benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one shows potential as a treatment for various diseases by inhibiting apoptosis signal-regulating kinase 1.

Targeting Apoptosis Signalling Kinase-1 (ASK-1) Does Not Prevent the Development of Neuropathy in Streptozotocin-Induced Diabetic Mice

Targeting ASK1 does not prevent or ameliorate diabetic neuropathy in mice, suggesting that ASK1 activation is not responsible for nerve deficits in this model.

ASK1 pharmacophore model derived from diverse classes of inhibitors.

The developed pharmacophore model accurately predicts active and inactive compounds, aiding in virtual screening for novel ASK1 inhibitors.