Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-09-15
1995-07-25
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31495
Patent
active
054362466
ABSTRACT:
The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.sub.4 or --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 are each independently hydrogen or C.sub.1-4 alkyl; and the pharmaceutically acceptable addition salts thereof; with the proviso that when n is O or X is --CH=CHX.sub.1, then X.sub.1 is not OH, OR.sub.2, or NR.sub.2 R.sub.3 ; that are serotonin 5HT.sub.1A and 5HT.sub.1D receptor agents.
REFERENCES:
patent: 4833142 (1989-05-01), Hartog et al.
patent: 5032598 (1991-07-01), Baldwin et al.
patent: 5051421 (1991-09-01), Ferrini
patent: 5143916 (1992-09-01), Lavielle et al.
patent: 5246935 (1993-09-01), Jeppesen et al.
Bernotas Ronald C.
Cheng Hsien C.
Sprouse Jeffrey S.
Merrell Dow Pharmaceuticals Inc.
Peabody John
Richter Johann
Sayles Michael J.
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