N-substituted azaheterocyclic carboxylic acids and esters
AssigneeNovo Nordisk A/S
InventorsTine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Abstract
The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
Claims25
A compound of formula I ##STR13## wherein R.sup.1 and R.sup.2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;
- Y is --CH.sub.2 --N--CH.sub.2 --, --(C.dbd.O)--N--CH.sub.2 --, or --CH.sub.2 --N--(C.dbd.O)--, wherein only the underscored atoms participate in the ring system;
- X is --O--, --S--, or --(S.dbd.O)--;
- p is 0;
- q is 0;
- r is 1, 2 or 3;
- m is 1 or 2;
- n is 1 when m is 1 and n is 0 when m is 2;
- R.sup.3 and R.sup.4 each represents hydrogen or may--when m is 2--together represent a bond;
- and
- R.sup.5 is --OH or C.sub.1-6 -alkoxy;
- or
- a pharmaceutically acceptable salt thereof.
A compound of formula I ##STR14## wherein R.sup.1 and R.sup.2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;
- Y is --O--CH--CH.sub.2 --, --CH.sub.2 --CH--O--, --S--CH--CH.sub.2 -- or --CH.sub.2 --CH--S--wherein only the underscored atoms participate in the ring system;
- X is --N(R.sup.9)--wherein R.sup.9 is hydrogen or C.sub.1-6 -alkyl;
- p is 0;
- q is 0;
- r is 1, 2 or 3;
- m is 1 or 2;
- n is 1 when m is 1 and n is 0 when m is 2;
- R.sup.3 and R.sup.4 each represents hydrogen or may--when m is 2--together represent a bond;
- and
- R.sup.5 is --OH or C.sub.1-6 -alkoxy;
- or
- a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.