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Claims for Patent: 5,532,241

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Claims for Patent: 5,532,241

Title: Piperidines and piperazines
Abstract:Piperidine and piperazine derivatives of the formula I ##STR1## wherein Ind is an indol-3-yl radical which is unsubstituted or mono- or polysubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2, R.sup.1 is benzofuran-5-yl or 2,3-dihydrobenzofuran-5-yl, chroman-6-yl, chroman-4-on-6-yl, 3-chromen-6-yl or chromen-4-on-6-yl, which is unsubstituted or monosubstituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2, Q is C.sub.m H.sub.2m, N or CR.sup.3, A is alkyl having 1-6 C atoms, Hal is F, C1, Br or I, R.sup.2 is OH, OA, NH.sub.2, NHA or NA.sub.2, R.sup.3 is H, OH or OA and m is 2, 3 or 4, and their physiologically acceptable salts, are active on the central nervous system.
Inventor(s): Bottcher; Henning (Darmstadt, DE), Seyfried; Christoph (Seeheim-Jugenheim, DE), Bartoszyk; Gerd (Darmstadt, DE), Greiner; Hartmut (Darmstadt, DE)
Assignee: Merck Patent Gesellschaft mit beschrankter Haftung (Darmstadt, DE)
Application Number:08/314,734
Patent Claims: 1. A compound according to formula I ##STR4## wherein Ind is unsubstituted indol-3-yl, indol-3-yl monosubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2, or indol-3-yl polysubstituted by OH, OA, CN, Hal, COR.sup.2, CH.sub.2 R.sup.2 or combinations thereof;

R.sup.1 is benzofuran-5-yl, chroman-4-on-6-yl, 3-chromen-6-yl or chromen-4-on-6-yl, which in each case is unsubstituted or monosubstituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2 ;

Q is C.sub.m H.sub.2m ;

Z is N;

A is alkyl having 1-6 C atoms;

Hal is F, Cl, Br or I;

R.sup.2 is OH, OA, NH.sub.2, NHA or NA.sub.2 ;

R.sup.3 is H, OH or OA; and

m is 2, 3 or 4; or

a physiologically acceptable salt thereof.

2. A compound according to claim 1, wherein said compound is:

(a) 1-[4-(5-methoxyindol-3-yl)butyl]-4-(2-hydroxymethylbenzofuran-5-yl)piperaz ine or a physiologically acceptable salt thereof;

(b) 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-ethoxycarbonylbenzofuran-5-yl ) piperazine or a physiologically acceptable salt thereof; or

(c) 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl) piperazine or a physiologically acceptable salt thereof.

3. A compound according to claim 1, wherein Ind is unsubstituted indol-3-yl, indol-3-yl monosubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2, or indol-3-yl disubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2.

4. A compound according to claim 1, wherein Ind is indol-3-yl monosubstituted in the 5-position by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2.

5. A compound according to claim 1, wherein Ind is indol-3-yl monosubstituted in the 4-, 6- or 7-position by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2.

6. A compound according to claim 1, wherein A is methyl or ethyl.

7. A compound according to claim 1, wherein R.sup.1 is benzofuran-5-yl, or chroman-4-on-6-yl which, in each case is unsubstituted or monosubstituted by --CH.sub.2 OH, --CONH.sub.2, --CO.sub.2 A or --CO.sub.2 NHA.

8. A compound according to claim 1, wherein Q is --(CH.sub.2).sub.4 --.

9. A compound according to claim 1, wherein Ind is indol-3-yl substituted in the 5-position by OH or OA.

10. A compound according to claim 1, wherein Ind is indol-3-yl substituted in the 5-position by CONH.sub.2 or CN.

11. A compound according to claim 1, wherein R.sup.1 is unsubstituted benzofuran-5-yl or benzofuran-5-yl substituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2.

12. A compound according to claim 1, wherein R.sup.1 is chromen-4-on-6-yl.

13. A compound according to claim 1, wherein R.sup.1 is unsubstituted 3-chromen-6-yl or 3-chromen-6-yl substituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2.

14. A compound according to claim 1, wherein R.sup.1 is unsubstituted chroman-4-on-6-yl or chroman-4-on-6-yl substituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2.

15. A compound according to claim 1, wherein R.sup.1 is unsubstituted chromen-4-on-6-yl or chromen-4-on-6-yl substituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2.

16. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

17. A composition according to claim 16, wherein said compound is present in an amount of 0.2-500 mg.
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