Piperidine derivatives useful as 5-HT.sub.3 antagonists

Details Piperidine derivatives useful as 5-HT.sub.3 antagonists Piperidine derivatives useful as 5-HT.sub.3 antagonists

1989-02-21

1990-09-25

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514316, 546187, 546199, 546200, 546201, A61K 31445, C07D21198

Patent

active

049593757

ABSTRACT:
Piperidine derivatives of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein A represents an aromatic radical selected from ##STR2## wherein R.sup.3 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or halogen; X.sup.1 -X.sup.2 represents CH.sub.2 --CH, NR.sup.4 --CH, O--CH, S--CH, CH.sub.2 --N, O--N, S--N, NR.sup.4 --N, CH--NR.sup.4 or N--NR.sup.4 [where R.sup.4 is hydrogen, (C.sub.1-4)alkyl, phenyl or phenyl(C.sub.1-4)alkyl] or ##STR3## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, hydroxy, nitro, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkyl-amino, (C.sub.2-4)alkanoylamino, mercapto or (C.sub.1-4)alkylthio and R.sup.1 and R.sup.2 are independently hydrogen, (C.sub.1-4)alkyl or (C.sub.1-4)alkylphenyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent pyrrolidino or piperidino possess 5-HT.sub.3 -antagonistic activity.

REFERENCES:
patent: 4758668 (1988-07-01), Strupczewski
Irikura et al., J. Med. Chem. 14, 357-361 (1971).

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