Spasmolytics
AssigneeDuphar International Research B.V.
InventorsJan Hartog, Johannes M. A. Zwagemakers
Life of this patent
Estimating the term…
Abstract
Tertiary amines of formula 3 have a strong and prolonged spasmolytic effect, also after oral administration, on the smooth musculature of the tractus gastrointestinalis, the tractus urogenitalis and the bronchial system and have a low toxicity. The compounds can be synthetized according to methods known per se and been formulated to pharmaceutical compositions.
Claims15
A compound selected from the group consisting of
- 8-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-octanone-3,
- 9-[N-ethyl-[1-methyl-2-(3-methoxyphenyl)]-ethylamino]-nonanone-6,
- 6-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-2-methylhexanone-3,
- 8-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-octanone-4,
- 8-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-octanone-5,
- 9-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-nonanone-6,
- 8-[N-ethyl-[(1-methyl-2-phenyl)ethylamino]-octanone-5, and
- a pharmaceutically acceptable acid salt thereof.
A compound of the formula ##STR5## wherein R.sub.1 is selected from the group consisting of alkyl, alkoxy, alkylthio, and dialkylamino having up to 2 carbon atoms per substituent;
- hydroxy, halogen atom, chlorine atom, and fluorine atom,
- R.sub.2 is a hydrogen atom, or if R.sub.1 is a hydrogen atom, in addition one of the remaining meanings of R.sub.1, with the proviso that R.sub.1 and R.sub.2 both may represent an alkoxy group having up to 2 carbon atoms,
- R.sub.3 is alkyl having up to 2 carbon atoms,
- R.sub.4 is alkyl having up to 3 carbon atoms,
- R.sub.5 is a branched or straight chain alkylene having 3 to 5 carbon atoms, and
- R.sub.6 is cycloalkyl or 5 to 6 carbon atoms
- and a salt thereof formed with a pharmaceutically acceptable acid.
A method of treating a patient suffering from a spastic condition comprising administering to said patient a spasmolytically effective amount of a spasmolytic composition comprising a spasmolytically effective amount of a compound of the formula ##STR6## in which R.sub.1 represents an alkyl group, an alkoxy group, an alkylthio group or a dialkylamino group having up to 2 carbon atoms per substituent, a hydroxy group, a hydrogen atom, a chlorine atom or a fluorine atom, R.sub.2 is a hydrogen atom or, if R.sub.1 represents a hydrogen atom, in addition one of the remaining meanings of R.sub.1, while R.sub.1 and R.sub.2 both may represent an alkoxy group having up to 2 carbon atoms, R.sub.3 is an alkyl group having up to 2 carbon atoms, R.sub.4 is an alkyl group having up to 3 carbon atoms, R.sub.5 is a branched or non-branched alkylene group having 3 to 12 carbon atoms, X is an oxygen atom, R.sub.6 is a branched or non-branched or cyclic alkyl group having up to 8 carbon atoms and R.sub.5 together with R.sub.6 contains at least 6 carbon atoms and a salt thereof formed with a pharmaceutically acceptable acid and a pharmaceutically acceptable carrier therefor.
Dependencies are inferred from the claim text.