Derivatives of 2-amino-1-phenylethanol having antiulcer activity
AssigneeA. H. Robins Company, Incorporated
InventorsHarry R. Munson, Jr., Robert F. Boswell
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Abstract
Derivatives of 2-amino-1-phenylethanol were prepared from substituted amines and benzoin, stilbene oxide or styrene oxide to give compounds of Formula: ##STR1## where R is H or (un)substituted phenyl and C is a linking group or terminal group. The compounds of this invention can inhibit ulceration in in-vivo studies in rats.
Claims5
A compound according to the formula:
- ##STR41## wherein X is H, --Cl, --CH.sub.3 or --OCH.sub.3 ;
- A is --H, --CH.sub.3 or ##STR42## n is 2;
- B is C.sub.1 -C.sub.6 alkylene, optionally substituted with --OH, --CH.sub.2 OH or --CH.sub.3 ;
- C is a linking group selected from the group consisting of --O--(CH.sub.2).sub.2-6 --O--, --O--, --S--, or ##STR43## R is H or ##STR44## where X is as defined above;
- a diastereomer, or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition for the treatment of gastric and duodenal ulcers comprised of:
- a. A therapeutically effective amount of a compound according to the formula:
- ##STR45## wherein X is H, --Cl, --CH.sub.3, or --OCH.sub.3 ;
- A is H, --CH.sub.3 or ##STR46## n is 2;
- B is C.sub.1 -C.sub.6 alkylene, optionally substituted with --OH, --CH.sub.2 OH, or --CH.sub.3 ;
- C is a linking group selected from the group consisting of ##STR47## a diastereomer, or a pharmaceutically acceptable salt thereof and b. a pharmaceutical carrier.
A method of treatment or gastric or duodenal ulceration in warm-blooded animals which comprises administering thereto a therapeutically effective amount of a compound of the formula:
- ##STR48## wherein X is H, --Cl, --CH.sub.3 or --OCH.sub.3 ;
- A is --H, --CH.sub.3 or ##STR49## n is 2 to 3;
- B is C.sub.1 -C.sub.6 alkylene, optionally substituted with --OH, --CH.sub.2 OH or --CH.sub.3 ;
- C is a linking group selected from the group consisting of --O--(CH.sub.2).sub.2-6 --O--, --O--, --S--, ##STR50## R is H or ##STR51## where X is as defined above;
- a diastereomer, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.