241499-50-3

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 540-37-4 p-aminoiodobenzene 
• 917-92-0 3,3-Dimethylbut-1-yne 
• 159217-89-7 N-Boc-4-iodoaniline 

Downstream Products

• 241499-17-2 [1-(4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-amine 
• 241499-54-7 4-[[4-(3,3-Dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester 
• 241499-53-6 4-[4-(3,3-Dimethyl-butyl)-phenylamino]-piperidine-1-carboxylic acid tert-butyl ester 
• 241499-55-8 [4-(3,3-dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-piperidin-4-yl-amine 
• 241499-52-5 4-(3,3-dimethyl-butyl)-phenylamine 

Relevant academic research and scientific papers

Heterocyclic substituted aniline calcium channel blockers

The present invention provides compounds that block calcium channels having the Formula I shown below. STR1The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.

The discovery of [1-(4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phenyl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia

Our drug discovery efforts for N-type calcium channel blockers in the 4-piperidinylaniline series led to the discovery of an orally active analgesic agent 26. 1-[4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-amine (26) showed high affinity to functionally block N-type calcium channels (IC50=0.7 μM in the IMR32 assay) and exhibited high efficacy in the anti-writhing analgesia test with mice (ED50=12 mg/kg by po and 4 mg/kg by iv). In this report, the rationale for the design, synthesis, biological evaluation, and pharmacokinetics of this series of blockers is described. Copyright (C) 2000 Elsevier Science Ltd.