Claims
- 1. An alkanolamine derivative selected from the group consisting of a compound of the formula: ##STR9## wherein A.sup.1 is alkylene of from 2 to 6 carbon atoms; wherein A.sup.2 is a direct link or alkylene of up to 6 carbon atoms; wherein R.sup.2, R.sup.3, R.sup.12 and R.sup.13, which may be the same or different, each is hydrogen, halogen, hydroxy, amino, nitro, carbamoyl, cyano or alkyl, alkenyl, alkoxy, alkylthio, alkenyloxy, alkanoyl or alkanoyl-amino each of up to 6 carbon atoms, or wherein R.sup.2 and R.sup.3 together and/or R.sup.12 and R.sup.13 together, form trimethylene, tetramethylene or buta-1,3-dienylene such that together with the adjacent benzene ring they form respectively indanyl, 5,6,7,8-tetrahydronaphthyl or naphthyl; and wherein Y.sup.2 is a direct link, or alkylene or alkyleneoxy each of up to 6 carbon atoms; and the non-toxic pharmaceutically-acceptable acid-addition salts thereof.
- 2. An alkanolamine derivative as claimed in claim 1 wherein A.sup.1 is ethylene, trimethylene, tetramethylene, hexamethylene, 1-methylethylene, 2-methylethylene or 1,1-dimethylethylene; wherein A.sup.2 is methylene, ethylene, trimethylene, tetramethylene, hexamethylene, 1-methylethylene, 2-methylethylene, 1,1-dimethylethylene or ethylidene; wherein R.sup.2, R.sup.3, R.sup.12 and R.sup.13, which may be the same or different, each is hydrogen, fluorine, chlorine, bromine, iodine, hydroxy, amino, nitro, carbamoyl, cyano, methyl, ethyl, n-propyl, allyl, methoxy, isopropoxy, methylthio, allyloxy, formyl, acetyl or acetamido, or wherein R.sup.2 and R.sup.3 together, and/or R.sup.12 and R.sup.13 together, form trimethylene, tetramethylene or buta-1,3-dienylene; and wherein Y.sup.2 is a direct link or methylene, ethylene, methyleneoxy, ethyleneoxy, trimethyleneoxy, 1-methylethylideneoxy or 1-methylpropylideneoxy; and the non-toxic pharmaceutically-acceptable acid-addition salts thereof.
- 3. An alkanolamine derivative as claimed in claim 1 wherein A.sup.1 is ethylene, 1-methylethylene or 1,1-dimethylethylene; wherein A.sup.2 is a direct link or methylene, ethylidene or ethylene; wherein either R.sup.12 is hydrogen, chlorine, hydroxy or nitro and R.sup.13 is hydrogen, or R.sup.12 and R.sup.13 together with the adjacent benzene ring form 1-naphthyl; wherein either R.sup.2 is hydrogen, chlorine, hydroxy, carbamoyl, cyano, methyl, allyl, methoxy or allyloxy and R.sup.3 is hydrogen, or R.sup.2 and R.sup.3 together with the adjacent benzene ring form 1-naphthyl; and wherein Y.sup.2 is a direct link, methylene or methyleneoxy; and the non-toxic, pharmaceutically-acceptable salts thereof.
- 4. An alkanolamine derivative as claimed in claim 3 wherein A.sup.1 is ethylene; wherein A.sup.2 is methylene or ethylene; wherein ##STR10## is 1-naphthyl, phenyl, chlorophenyl, hydroxyphenyl or nitrophenyl; wherein either R.sup.2 is hydrogen, or chlorine, cyano, methyl, methoxy or allyloxy in the 2-position of the phenyl nucleus, and R.sup.3 is hydrogen, or R.sup.2 and R.sup.3 together with the adjacent benzene ring form 1-naphthyl; and wherein Y.sup.2 is a direct link or methylene, or a non-toxic pharmaceutically-acceptable acid-addition salt thereof.
- 5. An alkanolamine derivative as claimed in claim 1 wherein A.sup.1 is ethylene, A.sup.2 is a direct link or methylene or ethylene, ##STR11## is phenyl, monochlorophenyl, mononitrophenyl, monohydroxyphenyl or 1-naphthyl, either R.sup.2 is hydrogen, chloro or cyano, or alkyl, alkenyl, alkoxy or alkenyloxy each of up to 3 carbon atoms and R.sup.3 is hydrogen, or R.sup.2 and R.sup.3 together with the adjacent benzene ring form 1-naphthyl and Y.sup.2 is a direct link or methylene; or a non-toxic pharmaceutically-acceptable acid-addition salt thereof.
- 6. The compound:
- 1-(o-cyanophenoxy)-3-.beta.-(benzamidoacetamido)ethylaminopropan-2-ol; or
- 1-(o-chlorophenoxy)-3-.beta.-(phenylacetamidoacetamido)ethylaminopropan-2-ol;
- or a non-toxic pharmaceutically-acceptable acid-addition salt thereof.
- 7. A non-toxic, pharmaceutically-acceptable acid-addition salt as claimed in claim 1 which is a hydrochloride, hydrobromide, phosphate, sulphate, oxalate, lactate, tartrate, acetate, salicylate, citrate, benzoate, .beta.-naphthoate, adipate or 1,1-methylene-bis-(2-hydroxy-3-naphthoate), or a salt derived from a sulphonated polystyrene resin.
- 8. A pharmaceutical composition comprising as active ingredient at least one alkanolamine derivative or an acid-addition salt thereof, claimed in claim 1, in association with a pharmaceutically-acceptable diluent or carrier therefor.
- 9. A method for the treatment or prophylaxis of heart diseases and hypertension in a warm-blooded animal which comprises administering to said animal an effective amount of at least one compound claimed in claim 1.
- 10. A method for producing coronary .beta.-adrenergic blockade in a warm-blooded animal in need of such blockade which comprises administering to said animal an effective amount of at least one compound claimed in claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
41714/76 |
Oct 1976 |
GBX |
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Parent Case Info
This is a division of application Ser. No. 839,568, filed Oct. 5, 1977, now U.S. Pat. No. 4,211,878 issued July 8, 1980.
US Referenced Citations (12)
Divisions (1)
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Number |
Date |
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Parent |
839568 |
Oct 1977 |
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