Generated: May 25, 2017
|Abstract:||Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12; Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group; R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4; and the physiologically acceptable salts and solvates thereof. The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients. The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.|
|Inventor(s):||Skidmore; Ian F. (Herts, GB2), Lunts; Lawrence H. C. (Herts, GB2), Finch; Harry (Herts, GB2), Naylor; Alan (Herts, GB2)|
|Assignee:||Glaxo Group Ltd. (London) N/A)|
|Filing Date:||Dec 19, 1991|
|Claims:||1. A compound of the formula ##STR33## wherein m is an integer from 3 to 6; |
n is an integer from 2 to 6 with the proviso that the sum total of m+n is 4 to 12;
Ar represents a phenyl group which may be constituted or substituted by one or two substituents selected from halogen atoms, C.sub.1-3 alkyl and C.sub.1-3 alkoxy groups;
R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group with the proviso that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4; and Y.sup.1 represents a hydrogen atom or a group convertible thereto by catalytic hydrogenation; or an acid addition salt thereof.
2. The compound according to claim 1 wherein m is 3 and n is 6; or m is 4 and n is 3, 4 or 5; or m is 5 and n is 2, 3, 4 or 5; or m is 6 and n is 2 or 3.
3. A compound according to claim 1 wherein the sum total of m+n is 7, 8, 9 or 10.
4. A compound according to claim 1 wherein R.sup.1 and R.sup.2, which may be the same or different, each represent a hydrogen atom or a methyl group.
5. A compound according to claim 1 wherein Ar represents an unsubstituted phenyl group or a phenyl group substituted by one substituent selected from a chlorine or fluorine atom or a methoxy or methyl group.
6. A compound according to claim 1 wherein Y.sup.1 represents an arylmethyl group.
7. A compound according to claim 1 wherein R.sup.1 represents a benzyl, benzhydryl or .alpha.-methylbenzyl group.
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