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US 5,861,509 AGranted
Arylglycinamide derivatives and pharmaceutical compositions containing these compounds
AssigneeBoehringer Ingelheim GmbH
InventorsGerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
Life of this patent
Estimating the term…
Abstract
The invention relates to new arylglycinamide derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokin (tachykinin) antagonists.
Claims12
An arylglycinamide derivative of the formula I ##STR74## or the pharmaceutically acceptable salts thereof, wherein
- Ar denotes unsubstituted or mono- to penta-substituted phenyl, or unsubstituted or mono- or di-substituted naphthyl, in which the substituents of the phenyl and naphthyl independently of each other denote halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O--( C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of each other denote H, methyl or acetyl);
- R.sup.1 and R.sup.2 together with the N to which they are bound form a 6-membered ring of the formula ##STR75## wherein X denotes CR.sup.7 R.sup.8, wherein
- R.sup.7 and R.sup.8 have the following meanings:
- a) R.sup.7 is ##STR76## R.sup.8 is H, --CONH.sub.2, --NHC(O)CH.sub.3 or --N(CH.sub.3)C(O)CH.sub.3, R.sup.3 denotes H, (C.sub.1-4)alkyl, unsubstituted or mono- to tri-substituted phenyl, wherein the substituents independently of one another represent halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of one another denote H, methyl or acetyl);
- R.sup.4 denotes (CH.sub.2).sub.m phenyl or (CH.sub.2).sub.m naphthyl, wherein m is 1, 2 or 3 and phenyl may be substituted by 1 to 3 substituents, wherein the substituents independently of one another are halogen (F, Cl, Br, I),
- (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently or one another denote H, methyl or acetyl);
- and
- R.sup.5 denotes H, (C.sub.1-4)alkyl, (C.sub.3-6)cycloalkyl or CH.sub.2 COOH.
5 more elements
Dependencies are inferred from the claim text.