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US 4,791,216 AGranted
Para ethyl amino phenol pharmaceutical compounds
AssigneeFisons Limited
InventorsFrancis Ince, Alan C. Tinker
Life of this patent
Estimating the term…
Abstract
There are provided paraethylamine phenol compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.
Claims9
A compound of formula I, ##STR18## in which R.sub.1 represents CH.sub.2 R.sub.12, or fluorine;
- R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C.sub.1 to C.sub.6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9 ;
- R.sub.12 represents hydrogen, OH, SO.sub.2 R.sub.13 or alkyl C.sub.1 to C.sub.6,
- R.sub.13 represents alkyl C.sub.1 to C.sub.6,
- W represents a single bond, a 1,2;
- 1,3;
- or 1,4-disubstituted benzene ring;
- a --CH.dbd.CH-- group or a 1,4-cyclohexanediyl group;
- X represents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;
- Y represents (CH.sub.2).sub.q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen, or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18, wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in which
- R.sub.17 and R.sub.18, together with the carbon atom to which they are attached from a carbonyl group, and R.sub.15, R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, or
- R.sub.15, R.sub.16, R.sub.17 and R.sub.18 each independently represent hydrogen or alkyl C.sub.1 to C.sub.6 and R.sub.20 represents hydrogen;
- Z represents a single bond, NR.sub.19, CH.sub.2, O, CO, S or SO.sub.2,
- in which R.sub.19 represents hydrogen or alkyl C.sub.1 to C.sub.6 ;
- n, and m each independently represent an integer from 1 to 4 inclusive;
- q represents an integer from 1 to 3 inclusive;
- p represents 0 or an integer from 1 to 3 inclusive;
- R.sub.9 represents phenyl or phenyl substituted by hydroxy, and
- R.sub.10 represents hydrogen or chlorine,
- provided that
- (i) when X represents SO.sub.2, CO, COO or CONH, Y does not represent CO, CS or SO.sub.2 ;
- (ii) when Y represents CO, CS or SO.sub.2, then Z does not represent CO or SO.sub.2,
- and pharmaceutically acceptable derivatives thereof.
19 more elements
Dependencies are inferred from the claim text.