Claims for Patent: 5,532,241
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Summary for Patent: 5,532,241
| Title: | Piperidines and piperazines |
| Abstract: | Piperidine and piperazine derivatives of the formula I |
| Inventor(s): | Henning Bottcher, Christoph Seyfried, Gerd Bartoszyk, Hartmut Greiner |
| Assignee: | Merck Patent GmbH |
| Application Number: | US08/314,734 |
| 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, COR2 or CH2 R2, or indol-3-yl polysubstituted by OH, OA, CN, Hal, COR2, CH2 R2 or combinations thereof;R1 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, CH2 OH, CH2 OA or COR2 ; Q is Cm H2m ; Z is N; A is alkyl having 1-6 C atoms; Hal is F, Cl, Br or I; R2 is OH, OA, NH2, NHA or NA2 ; R3 is H, OH or OA; and m is 2, 3 or 4; ora 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)piperazine 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, COR2 or CH2 R2, or indol-3-yl disubstituted by OH, OA, CN, Hal, COR2 or CH2 R2. 4. A compound according to claim 1, wherein Ind is indol-3-yl monosubstituted in the 5-position by OH, OA, CN, Hal, COR2 or CH2 R2. 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, COR2 or CH2 R2. 6. A compound according to claim 1, wherein A is methyl or ethyl. 7. A compound according to claim 1, wherein R1 is benzofuran-5-yl, or chroman-4-on-6-yl which, in each case is unsubstituted or monosubstituted by --CH2 OH, --CONH2, --CO2 A or --CO2 NHA. 8. A compound according to claim 1, wherein Q is --(CH2)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 CONH2 or CN. 11. A compound according to claim 1, wherein R1 is unsubstituted benzofuran-5-yl or benzofuran-5-yl substituted by CN, CH2 OH, CH2 OA or COR2. 12. A compound according to claim 1, wherein R1 is chromen-4-on-6-yl. 13. A compound according to claim 1, wherein R1 is unsubstituted 3-chromen-6-yl or 3-chromen-6-yl substituted by CN, CH2 OH, CH2 OA or COR2. 14. A compound according to claim 1, wherein R1 is unsubstituted chroman-4-on-6-yl or chroman-4-on-6-yl substituted by CN, CH2 OH, CH2 OA or COR2. 15. A compound according to claim 1, wherein R1 is unsubstituted chromen-4-on-6-yl or chromen-4-on-6-yl substituted by CN, CH2 OH, CH2 OA or COR2. 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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