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1. US5703115 - (benzodioxan, benzofuran or benzopyran) alkylamino! alkyl substituted guanidines

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]
We claim:
1. A compound having the formula: a pharmaceutically acceptable acid addition salt thereof, or a stereochemically isomeric form thereof, wherein:
X is CH 2 or a direct bond;
R 1 is hydrogen or C 1-6 alkyl;
R 2 is hydrogen, C 1-6 alkyl, C 3-6 alkenyl or C 3-6 alkynyl;
R 3 is hydrogen or C 1-6 alkyl;
R 4 is hydrogen or C 1-6 alkyl;
Alk 1 is a bivalent C 1-3 alkanediyl radical;
A is a bivalent radical of the formula:
--N(R 5)--Alk 2 --N(R 6)--
wherein:
R 5 and R 6 individually are hydrogen or C 1-4 alkyl and Alk 2 is C 2-5 alkanediyl or C 5-7 cycloalkanediyl;
R 7 and R 8 each independently are hydrogen, halo, C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, hydroxy, C 1-6 alkyloxy, cyano, aminoC 1-6 alkyl, carboxyl, C 1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C 1-6 alkylcarbonylamino, or mono- or di(C 1-6 alkyl)amino;
provided that �2-�(2,3-dihydro-1,4-benzodioxin-2-yl)methyl!-amino!ethyl guanidine is excluded.
2. A compound according to claim 1, wherein Alk 1 is CH 2.
3. A compound according to claim 1, wherein X is CH 2 and wherein R 7 and R 8 each independently are hydrogen, halo, C 1-6 alkyl, C 1-6 alkyloxy, hydroxy, cyano, nitro, aminoC 1-6 alkyl, amino, C 1-6 alkylcarbonylamino.
4. A compound according to claim 2 wherein R 6 is hydrogen.
5. A compound according to claim 3 wherein R 6 is hydrogen.
6. A compound according to claim 4 wherein R 5 is hydrogen.
7. A compound according to claim 5 wherein R 5 is hydrogen.
8. A compound according to claim 6 wherein Alk 2 is C 2-5 alkanediyl.
9. A compound according to claim 7 wherein Alk 2 is C 2-5 alkanediyl.
10. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 1.
11. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 2.
12. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 3.
13. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 4.
14. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 5.
15. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 6.
16. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 7.
17. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 8.
18. A composition comprising a pharmaceutically acceptable carrier and as an active ingredient an effective vasoconstricting amount of a compound as defined in claim 9.
19. A method of treating migraine, which method comprises administering to patients in need of such treatment a therapeutically effective amount of a compound as defined in claim 1.