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US 5,296,477 AGranted
Aminoalkyl benzoxazine and benzthiazine compounds having a high 5-HT.sub.1A affinity
AssigneeAdir et Compagnie
InventorsThierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
Life of this patent
Estimating the term…
Abstract
Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description. Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.
Claims16
A compound selected from those of formula (I):
- ##STR14## in which:
- R.sub.1 represents hydrogen or lower alkyl,
- n represents 1 or 2,
- A represents oxygen or sulfur,
- X represents a CH.sub.2 group,
- R.sub.2 represents hydrogen or lower alkyl or lower acyl and R.sub.3 represents (CH.sub.2)pR.sub.4, with p being an integer from 1 and 6, inclusive, and R.sub.4 represents:
- a nitrile group, in which case R.sub.3 represents (CH.sub.2).sub.p-1 R.sub.4, or halogen or amino optionally substituted with:
- (lower alkyl) sulfonyl,
- phenylsulfonyl optionally substituted on the phenyl ring with one or more lower alkyl, lower alkoxy, hydroxyl, or trifluoromethyl groups or a halogen atom,
- one or two (C.sub.1 -C.sub.6) acyl groups optionally substituted with a lower alkyl, lower alkoxy, or hydroxyl group, a halogen atom, or a phenyl, thienyl, benzothienyl, indolyl, furyl, or benzofuryl group, the phenyl, thienyl, benzo-thienyl, indolyl, furyl and benzofuryl groups themselves optionally being substituted with one or more lower alkyl, lower alkoxy, or hydroxyl groups or a halogen atom,
- one or two linear or branched (C.sub.1 -C.sub.6) alkyl groups,
- or R.sub.4 represents any one of the following groups:
- ##STR15## in which:
- Y and Y', which may be identical or different, represent hydrogen, halogen or lower alkyl, lower alkoxy, or hydroxyl group,
- m is 1 or 2,
- its enantiomers, diastereoisomers, and epimers, and its addition salts with a pharmaceutically-acceptable acid or a pharmaceutically-acceptable base when R.sub.1 =H.
13 more elements
Dependencies are inferred from the claim text.