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US 6,747,026 B2Granted
NK-1 receptor active amine oxide prodrugs
AssigneeHoffman-La Roche Inc.
InventorsTorsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
Life of this patent
Estimating the term…
Abstract
Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
Claims7
A compound of the formula
- wherein
- R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;
- R1 is hydrogen or halogen;
- or
- R2 and R2′ are hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;
- or
- R3, R3′ are hydrogen, lower alkyl or cycloalkyl;
- R4 and R4′ together with the N-atom to which they are attached form a morpholine ring;
- R6 is lower alkyl;
- X is —C(O)N(R6)—;
- and
- n is 0, 1, 2, 3 or 4;
- or a pharmaceutically acceptable acid addition salt thereof.
10 more elements
The compound N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-oxy-morpholin -4-yl)-4-o-tolyl-nicotinamide.
The compound N-(2-methoxy-benzyl)-N-methyl-6-(4-oxy-morpholin-4-yl)-4-o -tolyl-nicotinamide.
The compound N-(5-chloro-2-methoxy-benzyl)-N-methyl-6-(4-oxy-morpholin-4-yl)-4-o-tolyl-nicotinamide.
The compound N-(2-chloro-5-methoxy-benzyl)-N-methyl-6-morpholin-4-yl-4-o -tolyl-nicotinamide.
Dependencies are inferred from the claim text.