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US 6,747,044 B2Granted
Neurokinin antagonists
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsHorst Dollinger, Franz Esser, Birgit Jung, Kurt Schromm, Georg Speck
Life of this patent
Estimating the term…
Abstract
The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1 denotes 3-hydroxypropyl, 1,3-dihydroxyprop-2-yl or C3-C6-cycloalkylmethyl, and R2, R3, R4 and Ar have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
Claims27
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 denotes 1,3-dihydroxyprop-2-yl,
- R2 denotes hydrogen, C1-C6alkyl, ω-hydroxy-C2-C4-alkyl, 1,3-dihydroxyprop-2-yl or C3-C6-cycloalkylmethyl,
- Ar denotes unsubstituted phenyl or phenyl which is 1- to 5-substituted by halogen, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-fluoroalkyl, C1-C4-fluoroalkoxy or —OCH2O—;
- R3 denotes phenyl-C1-C4-alkyl, wherein the phenyl group may be substituted by 1 to 3 substituents, wherein the substituents independently of one another are selected from halogen, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-fluoroalkyl, and C1-C4-fluoroalkoxy;
- and
- R4 denotes hydrogen, C1-C4-alkyl, C3-C8-cycloalkyl, CH2COOH, —CH2C(O)NH2, —OH or phenyl-C1-C4-alkyl.
5 more elements
A compound having the following formula:
A compound having the following formula:
Dependencies are inferred from the claim text.