Indane and tetrahydronaphthalene derivatives as calcium channel antagonists
AssigneeSmithKline Beecham Corporation
InventorsJohn David Harling, Barry Sidney Orlek
Life of this patent
Estimating the term…
Abstract
This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.
Claims17
Method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I):
- ##STR16## wherein X represents O, S or NH;
- R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl;
- n is 1, 2 or 3;
- and
- Ar represents an phenyl optionally substituted by 1 to 3 substituents selected from:
- halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di-alkylamino, optionally substituted benzoyl and Ph(CH.sub.2).sub.r Y(CH.sub.2).sub.s -- where Ph is optionally substituted phenyl, Y is oxygen or a bond and r and s each independently represent 0-4 provided that the sum of r+s is not greater than 4, or
- Ar represents an optionally substituted unsaturated monocyclic heteroaryl ring system containing 5 or 6 ring members, or an optionally substituted, unsaturated or partially saturated bicyclic aryl or heteroaryl ring system containing 8-10 ring members,
- or a pharmaceutically acceptable salt thereof.
A compound of formula (IA):
- ##STR17## wherein X represents O, S or NH;
- R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl;
- n is 1, 2 or 3;
- and
- Ar represents phenyl optionally substituted by 1 to 3 substituents selected from:
- halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino, optionally substituted benzoyl and Ph(CH.sub.2).sub.r Y(CH.sub.2).sub.s -- where Ph is optionally substituted phenyl, Y is oxygen or a bond and r and s each independently represent 0-4 provided that the sum of r+s is not greater than 4, or
- Ar represents an optionally substituted unsaturated monocyclic heteroaryl ring system containing 5 or 6 ring members, or an optionally substituted, unsaturated or partially saturated bicyclic aryl or heteroaryl ring system containing 8-10 ring members,
- with the proviso that when X is O or S then Ar is not an unsubstituted phenyl group or phenyl substituted by lower alkyl, lower alkoxy, trifluoromethyl or halogen;
- or a salt thereof.
Dependencies are inferred from the claim text.