851678-89-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 851678-88-1 (S)-[2-(3-bromo-phenyl)-ethyl]-{1-[6-(tert-butyl-dimethyl-silanyloxymethyl)-pyridin-2-yl]-ethyl}-amine 
• 717879-40-8 (S)-1-[6-(tert-butyl-dimethyl-silanyloxymethyl)-pyridin-2-yl]-ethylamine 
• 717879-39-5 (R)-1-[6-(tert-butyl-dimethyl-silanyloxymethyl)-pyridin-2-yl]-ethanol 

Downstream Products

• 851678-90-5 (S)-[2-(3-bromo-phenyl)-ethyl]-[1-(6-hydroxymethyl-pyridin-2-yl)-ethyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN

The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.

Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the α2δ -1 subunit of voltage gated calcium channel

We have identified and synthesized a series of [1,2,4]triazolo[3,4-a] phthalazine derivatives as high-affinity ligands to α2δ-1 subunit of voltage gated calcium channels. Structure-activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC50=15nM) and (S)-22 (IC50=30nM). A potent and selective radioligand, [3H]-(S)-22 was also synthesized to demonstrate that this ligand binds to the same site as gabapentin.