4-Amino-benzo[b]pyran-3-ol derivatives
AssigneeBeecham Group Limited
InventorsJohn M. Evans, Robin E. Buckingham, Kenneth Willcocks
Life of this patent
Estimating the term…
Abstract
Anti-hypertensive compounds of formula (I): ##STR1## wherein: one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl; one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl; R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 acyl; and n is 1 or 2; the lactam group being trans to the OR.sub.5 group; or, when the other of R.sub.1 and R.sub.2 is amino, a pharmaceutically acceptable salt thereof.
Claims11
A compound of formula (I):
- ##STR19## wherein:
- one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;
- one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl;
- R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 carboxylic acyl;
- and
- n is 1 or 2;
- the lactam group being trans to the OR.sub.5 group;
- or, when the other of R.sub.1 and R.sub.2 is amino, a pharmaceutically acceptable salt thereof.
6-Acetamido-7-nitro-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)- 2,2-dimethyl-2H-benzo[b]pyran-3-ol;
- or 6-amino-7-nitro-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-b enzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof.
6-Nitro-7-acetamido-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)- 2,2-dimethyl-2H-benzo[b]pyran-3-ol;
- or 6-nitro-7-amino-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-b enzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof;
- or 6-cyano-7-amino-3,4-dihydro-trans-4-(2-ketopyrrolidinyl)-2,2-dimethyl-2H-b enzo[b]pyran-3-ol or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.