TY - PAT
T1 - Kainate receptor-selective epimeric analogs of dysiherbaine
AU - Swanson, Geoffrey
N1 - filingdate: 2008-10-1
issueddate: 2011-7-5
Status: published
attorneydocketnumber: 2007-036-02
PY - 2011/7/5
Y1 - 2011/7/5
N2 - Small Molecule for Treatment of Epilepsy, Pain, and Other Neurological Disorders
NU 2007-036
Inventors
Leanne Lash
Geoffrey Swanson*
Ryuichi Sakai
Abstract
Over-activation of AMPA receptors contributes to the pathology of a number of neurological diseases, particularly epilepsy, neuropathic pain, and stroke. A new group of heterotricyclic molecules called "IKM" analogs have been determined to act pharmacologically as AMPA receptor antagonists. Northwestern researchers have discovered a new class of small molecules that may be used to target specific AMPA receptors. A small molecule, 2,4-epi-neodysiherbaine (2,4-epi-NDH), has been determined to act as a selective kainate receptor antagonist. 2,4-epi-NDH is a synthetic analog of a natural molecule, dysiherbaine, which is itself a rigid analog of the excitatory amino acid neurotransmitter L-glutamate. The novelty of 2,4-epi-NDH is structural in that it has altered stereochemistry at the C2 and C4 positions and thus is not strictly considered an L-glutamate congener. The molecular also exhibits a novel pharmacological profile. There currently is no commercially available small molecule with similar pharmacological activity, making 2,4-epi-neodysiherbaine a desirable candidate for therapeutic use.
Applications
o Small molecule therapy for epilepsy, pain, and stroke
Advantages
o Selective antagonist for kainite receptor
o No other commercially available molecule with similar activity
IP Status
Issued US Patent No. 7,973,075
Marketing Contact
Michael Moore, PhD
Invention Manager
(e) [email protected]
(p) 847.491.4645
AB - Small Molecule for Treatment of Epilepsy, Pain, and Other Neurological Disorders
NU 2007-036
Inventors
Leanne Lash
Geoffrey Swanson*
Ryuichi Sakai
Abstract
Over-activation of AMPA receptors contributes to the pathology of a number of neurological diseases, particularly epilepsy, neuropathic pain, and stroke. A new group of heterotricyclic molecules called "IKM" analogs have been determined to act pharmacologically as AMPA receptor antagonists. Northwestern researchers have discovered a new class of small molecules that may be used to target specific AMPA receptors. A small molecule, 2,4-epi-neodysiherbaine (2,4-epi-NDH), has been determined to act as a selective kainate receptor antagonist. 2,4-epi-NDH is a synthetic analog of a natural molecule, dysiherbaine, which is itself a rigid analog of the excitatory amino acid neurotransmitter L-glutamate. The novelty of 2,4-epi-NDH is structural in that it has altered stereochemistry at the C2 and C4 positions and thus is not strictly considered an L-glutamate congener. The molecular also exhibits a novel pharmacological profile. There currently is no commercially available small molecule with similar pharmacological activity, making 2,4-epi-neodysiherbaine a desirable candidate for therapeutic use.
Applications
o Small molecule therapy for epilepsy, pain, and stroke
Advantages
o Selective antagonist for kainite receptor
o No other commercially available molecule with similar activity
IP Status
Issued US Patent No. 7,973,075
Marketing Contact
Michael Moore, PhD
Invention Manager
(e) [email protected]
(p) 847.491.4645
M3 - Patent
M1 - 7973075
ER -