NETUPITANT
- Ro 67-3189/000
- UNII-7732P08TIR
- Ro-67-3189
- Netupitant, an NK-1 antagonist is under development for the treatment of overactive bladder. HELSINN GROUP
CAS: 290297-26-6
290296-54-7 (di HCl)
U.S. Pat. Nos. 6,303,790, 6,531,597, 6,297,375 and 6,479,483, 6,719,996 and 6,593,472 to Hoffmann La Roche(originator).
IUPAC/Chemical name:
2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide
Chemical Formula: C30H32F6N4O
Exact Mass: 578.24803
Molecular Weight: 578.59
Elemental Analysis: C, 62.28; H, 5.57; F, 19.70; N, 9.68; O, 2.77
Netupitant is another selective NKi receptor antagonist under development by Helsinn Healthcare, having the formula 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2- methylphenyl)-6-(4-methylpiperazin- l-yl)pyridin-3-yl]propanamide, or Benzeneacetamide, N,a,a-trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-l-piperazinyl)-3-pyridinyl]-3,5- bis(trifluoromethyl)-, and the below chemical structure:
Netupitant is a tachykinin NK-1 antagonist which had been in phase III clinical trials at Helsinn for the prophylaxis of chemotherapy-induced nausea and vomiting and in phase II clinical studies for the treatment of overactive bladder. However, no recent development has been reported for this research.
NK-1 receptor antagonists work by blocking the action of neurokinin-1 (Substance…
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