Antichlorinergic bronchodilators
AssigneeSyntex (U.S.A.) Inc.
InventorJurg R. Pfister
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Abstract
Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 and C.sub.6 alkyl, C.sub.1 and C.sub.6 alkoxy and halo; or C.sub.4 or C.sub.5 heterocyclic aryl, the heteroatom selected from the group oxygen, nitrogen and sulfur; R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl; m is the integer 2 through 5; and X is selected from the group methanesulfonate, benzenesulfonate, p-toluene-sulfonate, nitrate, chloride, bromide and iodide. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.
Claims5
Compounds of the formula ##STR6## wherein R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy and halo;
- or monovalent heterocyclic radical of aromatic character containing, in addition to a heteroatom which is oxygen, nitrogen or sulfur, 4 or 5 carbon atoms in the ring;
- R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl;
- m is the integer 2 through 5;
- and X is an anion which effectively forms a pharmaceutically acceptable, non-toxic salt.
An anticholinergic composition which comprises a suitable pharmaceutical solvent or dispersant and at least one compound of the formula ##STR7## wherein R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy and halo;
- or;
- monovalent heterocyclic radical of aromatic character containing, in addition to a heteroatom which is oxygen, nitrogen or sulfur, 4 or 5 carbon atoms in the ring;
- R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl;
- m is the integer 2 through 5;
- and X is an anion which effectively forms a pharmaceutically acceptable, non-toxic salt.
A method for effecting bronchodilation in mammals which comprises administering to said mammals an effective amount of compounds of the formula ##STR8## wherein R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy and halo;
- or;
- monovalent heterocyclic radical of aromatic character containing, in addition to a heteroatom which is oxygen, nitrogen or sulfur, 4 or 5 carbon atoms in the ring;
- R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl;
- m is the integer 2 through 5;
- and X is an anion which effectively forms a pharmaceutically acceptable, non-toxic salt.
Dependencies are inferred from the claim text.