1. A pharmaceutical composition comprising a compound having the structure: ##STR00659## or a pharmaceutically acceptable salt or conjugate thereof in admixture with a pharmaceutically acceptable excipient.
2. A method to treat epilepsy, said method comprising administering to a subject in need of such treatment an amount of the pharmaceutical composition of claim 1 effective to ameliorate epilepsy.
The invention relates to compounds useful in treating conditions associated with calcium channel function, and particularly conditions associated with T-type calcium channel activity. More specifically, the invention concerns compounds containing substituted amino N-piperidinyl acetamide derivatives that are useful in treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
Thanks for the post and interesting thought. It appears the delay for 944 news may be worth while:
"Their findings were published today in Science Translational Medicine.
The new drugs, known as Z941 and Z944, block the flow of calcium ions into those neurons. When given to rats with absence epilepsy, they suppressed seizures by 85 to 90 percent.”
Terry Snutch’s thoughts on the drugs:
“Z941 and Z944 were designed to target a specific type of nerve cell calcium channel associated with epilepsy, as well as other hyper-excitability disorders such as chronic pain,” says Snutch, a professor in the departments of psychiatry and zoology. “The dramatic effect of the drugs in rats with absence epilepsy, together with the drugs’ ability to be administered orally and easily absorbed, and its good safety profile in animals, provide us with cautious optimism for the current clinical trial.”
"Although Z941 and Z944 appear to show promise as treatments for absence seizures, they have a long way to go before they displace ethosuximide and valproic acid as first-line treatments, cautioned Jacqueline A. French, MD, professor of neurology at the New York University Langone Medical Center, co-director of epilepsy research and epilepsy clinical trials at the NYU Comprehensive Epilepsy Center, and Fellow of the AAN."
Z944 is what big pharma will be paying the big $$$ for. The patent is now in place and good to 2029. (just what big pharma wanted)
It (the patent) has great broad range, pain being just one of them.
"The wide distribution of T-type calcium channels found in brain, heart, endocrine cells and other tissues provides the possibility of developing therapeutics for multiple indications, including treatment of pain."