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US 6,664,253 B2Granted
Neurokinin antagonists
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsHorst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, 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, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
Claims26
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 denotes C1-C6-alkyl or Ar2,
- R2 denotes hydrogen, C1-C6-alkyl or C3-C6-cycloalkylmethyl, or
- R1 and R2 taken together denote a C2-C3-alkylenediyl group optionally substituted by one or two oxo groups,
- X denotes O or NR5,
- Ar1 and Ar2 independently of one another denote 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 2-phenyl-ethyl, 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;
- denotes hydrogen, C1-C4-alkyl, C3-C8-cycloalkyl, CH2COOH, —CH2C(O)NH2, —OH or phenyl-C1-C4-alkyl;
- and
- R5 denotes hydrogen or C1-C6-alkyl.
8 more elements
A compound selected from the following compounds:
Dependencies are inferred from the claim text.