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US 5,672,602 AGranted
Substituted piperazine derivatives
AssigneeHoechst Marion Roussel, Inc.
InventorsTimothy P. Burkholder, Tieu-Binh Le, Elizabeth M. Kudlacz
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Abstract
The present invention relates to substituted piperazine derivatives (herein referred to as compounds or compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
Claims17
A compound of the formula ##STR28## wherein G.sub.1 is --CH.sub.2 -- or --C(O)--;
- G.sub.2 is --CH.sub.2 -- or --C(O)--;
- G.sub.3 is --CH.sub.2 -- or --C(O)--;
- m is 0 or 1;
- Ar.sub.1 is a radical chosen from the group:
- ##STR29## wherein Z.sub.1 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF.sub.3, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy;
- Ar.sub.2 is a radical chosen from the group ##STR30## wherein Z.sub.2 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF.sub.3, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy;
- Ar.sub.3 is a radical chosen from the group ##STR31## wherein Z.sub.3 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF.sub.3, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy;
- R.sub.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, or --CHO;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.q Ar.sub.4, or --CH.sub.2 C(O)Ar.sub.4 wherein q is an integer from 1 to 4 and Ar.sub.4 is a radical of the formula ##STR32## wherein Z.sub.4 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF.sub.3, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy;
- or stereoisomers, or pharmaceutically acceptable salt thereof;
- with the proviso that, when G.sub.1 is --C(O)--, then G.sub.2 is not --C(O)--;
- and with the further proviso that, when G.sub.3 is --CH.sub.2 --, then G.sub.1 and G.sub.2 are --CH.sub.2 --.
9 more elements
Dependencies are inferred from the claim text.