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US 5,177,084 AGranted
Therapeutic use of substituted benzenes, formulations thereof and novel substituted benzenes
AssigneeMerck Sharp & Dohme Corp.
InventorsRaymond Baker, Graham A. Showell
Life of this patent
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Abstract
Benzenes, substituted by a non-aromatic, non-fused 1-azabicycle and a substituent of low lipophilicity or a hydrocarbon substituent, their salts and prodrugs are useful in medicine, for example, in treating dementia. Some formulations of such benzenes are novel as are some of the compounds per se. They can be synthesized by methods analogous to those known in the art.
Claims2
A method for the treatment of neurological and mental disorders, which comprises the administration to a patient in need of such treatment a benzene compound of Formula I:
- ##STR6## salt or prodrug thereof, substituted on one of the ring carbon atoms with a R.sup.1 substituent selected from the group consisting of non-aromatic 1-azabicyclic and non-fused 1-azabicyclic ring system and independently substituted on each of the other ring carbon atoms with a R.sup.2, R.sup.11 and R.sup.12 substituent selected from the group consisting of hydrogen, halo, --CF.sub.3, OR.sup.6, --NR.sup.6 R.sup.7, --NHOR.sup.6, --NHNH.sub.2, --CN, COR.sup.8, and substituted or unsubstituted, saturated or unsaturated hydrocarbon groups, provided that at least one of R.sup.2, R.sup.11 and R.sup.12 is other than hydrogen or a hydrocarbon group, or R.sup.2 and R.sup.11 or R.sup.12 taken together form a C.sub.1-6 alkylenedioxy ring, wherein R.sup.6 is selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl and C.sub.2-6 alkynyl, wherein R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl and --COCH.sub.3, and R.sup.8 is selected from the group consisting of OH, --OR.sup.6, NHR.sup.7 and --NR.sup.6 R.sup.7.
Dependencies are inferred from the claim text.