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Paramétrages

Paramétrages

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1. US5688952 - (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. An intermediate of formula (IX-a): the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein:
X is CH 2 or a direct bond;
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;
or
R 2 and R 3 may be taken together to form a bivalent radical of the formula --(CH 2) m --wherein m is 4 or 5;
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: each R 5 is hydrogen or C 1-4 alkyl;
each R 6 is hydrogen or C 1-4 alkyl;
Alk 2 is C 2-15 alkanediyl or C 5-7 cycloalkanediyl; and each p is 0, 1 or 2; and
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, mono-or di(C 1-6 alkyl)amino, or C 1-6 alkylcarbonylamino,
wherein in the bivalent radical (c), the free bond from the --N(R 5)--moiety is bonded to the Alk 1 moiety.
2. An intermediate according to claim 1 wherein Alk 1 is CH 2.
3. An intermediate according to claim 1 wherein X is CH 2 and wherein R 7 and R 8 each independently hydrogen, halo, C 1-6 alkyloxy, hydroxy, cyano, nitro, aminoC 1-6 alkyl, amino or C 1-6 alkylcarbonylamino.
4. An intermediate according to claim 2 wherein A is the bivalent radical of formula (a) wherein R 6 is hydrogen.
5. An intermediate according to claim 3 wherein A is the bivalent radical of formula (a) wherein R 6 is hydrogen.