Wednesday, June 22, 2016 9:09:50 AM
U.S. Pat. App. No. 13/777,471
“Sigma-Receptor Ligands with Anti-Apoptotic and/or Pro-Apoptotic Properties Over Cellular Biochemical Mechanisms, with Neuroprotective, Anti-Cancer, Anti-Metastatic and Anti-(Chronic) Inflammatory Action”
Not yet published
Identical to parent U.S. Pat App. No. 12/522,761 / U.S. Pub. No. 20100069484
Another patent app I watch, 14/534698, recently got abandoned. It contained this info which I felt supported the A2-73 MOA:
[0007] There is also pharmacological evidence implicating activation of muscarinic receptors as a potential therapeutic approach to schizophrenia. For example, the muscarinic antagonist scopolamine, which is used to treat motion sickness, produces cognitive impairment and delusions of the type seen in schizophrenia. (Ellis et al. Int. J. Neuropsychopharmacol. 9:175. 2006). More selective M1 agonists have been suggested to potentiate glutamate signaling which could help exert a therapeutic effect. (Jones et al. J. Neurosci. 28:10422. 2008). In a double-blind placebo controlled trial of schizophrenic patients using xanomeline, which has preferential activity at the M1 and M4 receptors, alleviation of schizophrenia was observed. (Shekhar et al. Am. J. Psych. 165: 1033. 2008). However, because xanomeline also bound to subtypes of receptors other than M1, a number of various serious side effects were observed including GI side effects, cardiac side effects and problems with hyper-salivation.
[0008] To date, nobody has been able to harness the approach of employing muscarinic agonists because of the side effects associated with the agents' binding certain muscarinic receptor subtypes. A need exists for a method of using muscarinic agonists and for a medicament employing such muscarinic agonists that would allow for the therapeutic effects associated with activation of muscarinic receptors, but with fewer side effects.
More evidence that side effects have been keeping Mx compounds from successful development. So far A2-73's saftey profile is excellent. Enough so that it seems the company feels it is safe for infants. It could even supplant diazepam for it's indications there...febrile seizures, etc.
Alzheimer's, Parlinson's, Epilepsy, TBI, Huntington's, ALS, Stroke, MS, Rett, FTD, CDKL5, Dimentia with Lewy Bodies, Autism, Tourette, Cerebral Palsy, Coma, Down Syndrome, Prion Diseases, West, Diabetes, MD, Schizophrenia...dare I say Zellweger Syndrome?
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