Back to results
US 5,212,316 AGranted
Ethers and thioethers having therapeutical activity, their preparation and pharmaceutical compositions containing them
AssigneeBoehringer Mannheim Italia S.p.A.
InventorsSilvano Spinelli, Roberto Di Domenico, Ernesto Menta, Bruno Lumachi, Licia Gallico, Sergio Tognella
Life of this patent
Estimating the term…
Abstract
Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=or 2, a a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.
Claims1
Compounds of formula I ##STR12## wherein:
- Ar is phenyl;
- R.sub.1, R.sub.2, and R.sub.3 are substituents of the phenyl group Ar in 2-, 3-, 4-, and 5- position, which are the same or different, and are selected from the group consisting of hydrogen, hydroxy, (C.sub.1 -C.sub.5)-acyloxy, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxyl, (C.sub.2 -C.sub.4)-alkenyl, halogen, (C.sub.1 -C.sub.5)-acylamino, phenyl, phenoxy, imidazol-1yl, carboxyl-(C.sub.1 -C.sub.3)-alkoxycarbonyl, and carboxy-(C.sub.1 -C.sub.4)-alkyl;
- B is a valency bond, or a --(CH.sub.2 --O--CH.sub.2).sub.n -group;
- X is sulphur or oxygen;
- R is --(CH.sub.2).sub.n, --CH(R.sub.4)--, CH.sub.2 CH(NH.sub.2)--, or --CH.sub.2 --CH(NH--CORa) group;
- T is 2-, 3-, or 4-pyridyl, carboxyl, --CO.sub.2 R.sub.6, --COR.sub.6, --CO.sub.2 NH.sub.2, --CONRdRe, --CO--NH--CH(Rc)--CO.sub.2 Ra, di-(C.sub.1 -C.sub.4)-alkylamino-(C.sub.1 -C.sub.4)--alkyl-aminocarbonyl, hydroxy-(C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkyl-aminocarbonyl, di-(C.sub.1 -C.sub.4)-alkyl-amino-(C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)--alkyl-aminocarbonyl, or 2-, 3-, 4-pyridylmethylaminocarbonyl;
- n is 1 or 2;
- R.sub.4 is (C.sub.1 -C.sub.4)-alkyl or (C.sub.2 -C.sub.4)alkenyl;
- R.sub.6 is (C.sub.1 -C.sub.6)-alkyl, unsubstituted or substituted by (C.sub.1 -C.sub.6)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)-alkyoamino, di-(C.sub.1 -C.sub.4)alkylamino, (C.sub.3 -C.sub.6)-alkenyl, phenyl, or phenyl-(C.sub.1 -C.sub.6)-alkyl;
- Ra is hydrogen or (C.sub.1 -C.sub.4)-alkyl;
- and Rd is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.6 -C.sub.14)-Ar-(C.sub.1 -C.sub.4)-alkyl,
- Rd and Re, which are the same or different, are hydrogen or (C.sub.1 -C.sub.6)-alkyl, wherein the alkyl is unsubstituted or substituted by (C.sub.1 -C.sub.6)-alkoxy, hydroxy, --(C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkyl, or di-(C.sub.1 -C.sub.4)-alkyl-amino-(C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkyl, wherein the molecule contains either an imidazolyl group or a pyridyl group or both,
- as well as their enantiomers or diastereomers and the pharmacologically acceptable salts thereof.
10 more elements
Dependencies are inferred from the claim text.