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US 6,319,917 B1Granted
Acylaminoalkenylene-amide derivatives as NK1 and NK2 antagonists
AssigneeNovartis AG
InventorsMarc Gerspacher, Andreas von Sprecher, Robert Mah, Silvio Roggo, Stefan Stutz
Life of this patent
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Abstract
Compounds of formula I wherein R1, R1-R3, R4′, R4″ and R5 are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists. They are prepared in a manner known per se.
Claims14
A compound of formula I
- wherein
- R is phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy,
- R1 is hydrogen or lower alkyl,
- R2 is hydrogen, lower alkyl or phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy,
- R3 is phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy;
- or is naphthyl, 1H-indol-3-yl or 1-lower alkyl-indol-3-yl,
- R4′ and R4″ are each independently of the other hydrogen or lower alkyl, at least one of the radicals R4′ and R4″ being hydrogen, and
- R5 is C3-C8cycloalkyl, D-azacycloheptan-2-on-3-yl or L-azacycloheptan-2-on-3-yl;
- or a salt thereof.
6 more elements
Dependencies are inferred from the claim text.