Diazabicyclic neuokinin antagonists
AssigneePfizer Inc.
InventorsHarry R. Howard, Kevin D. Shenk
Life of this patent
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Abstract
The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
Claims17
A compound of the formula ##STR4## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is phenyl, thienyl or benzhydryl wherein one of the phenyl moieties of said benzhydryl may optionally be replaced by naphthyl, thienyl, furyl or pyridyl and wherein said phenyl, thienyl and benzhydryl may be substituted with one or more substituents independently selected from halo, nitro, (C.sub.1 -C.sub.6)alkyl optionally substituted with from one to three fluorine atoms, (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three fluorine atoms, amino, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)-alkylamino, (C.sub.1 -C.sub.6)alkyl--O--CO--, (C.sub.1 -C.sub.6)alkyl--CO--O--, (C.sub.1 -C.sub.6)alkyl--CO--, (C.sub.1 -C.sub.6)alkyl--O--, (C.sub.1 -C.sub.6)alkyl--CO--(C.sub.1 -C.sub.6)alkyl-, di-(C.sub.1 -C.sub.6)alkylamino, --CONH--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)-alkyl--CO--NH--(C.sub.1 -C.sub.6)alkyl, --NHCOH and --NHCO--(C.sub.1 -C.sub.6)alkyl;
- R.sup.2 is hydrogen or (C.sub.1 -C.sub.6)alkyl, or R.sup.1 and R.sup.2, together with the carbon to which they are attached, form a saturated carbocyclic ring having from 3 to 7 carbon atoms;
- A is phenyl, thienyl, benzothiazolyl or naphthyl wherein said phenyl, thienyl, benzothiazolyl and naphthyl may be substituted with one or more substituents independently selected from halo, nitro, (C.sub.1 -C.sub.6)alkyl optionally substituted with from one to three fluorine atoms, (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three fluorine atoms, amino, hydroxy(C.sub.l -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)-alkylamino, (C.sub.1 -C.sub.6)alkyl--O--CO--, (C.sub.1 -C.sub.6)alkyl--CO--O--, (C.sub.1 -C.sub.6)alkyl--CO--, (C.sub.1 -C.sub.6)alkyl--O--, (C.sub.1 -C.sub.6)alkyl--CO--(C.sub.1 -C.sub.6)alkyl-, di-(C.sub.1 -C.sub.6)alkylamino, --CONH--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)-alkyl--CO--NH--(C.sub.1 -C.sub.6)alkyl, --NHCOH and --NHCO--(C.sub.1 -C.sub.6)alkyl;
- n is 0, or 1;
- m is 0, or 1;
- the sum of n and m is 1;
- R.sup.3 is hydrogen or (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three fluorine atoms;
- R.sup.4 and R.sup.5 are hydrogen, or R.sup.4 and R.sup.5, together with the carbons to which they are attached, form an aromatic or non-aromatic carbocyclic or heterocyclic ring;
- R.sup.6 and R.sup.7 are hydrogen, or R.sup.3 together with R.sup.4, R.sup.5, R.sup.6 or R.sup.7, along with the carbon to which they are attached, form a saturated carbocyclic group having from 3 to 6 carbons;
- G is (CR.sup.8 R.sup.9).sub.p wherein p is 1, and R.sup.8 and R.sup.9 are each independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, naphthyl or heteroaryl wherein said alkyl may be substituted by one to three fluorine atoms.
Dependencies are inferred from the claim text.