(EN)
[(BENZODIOXAN, BENZOFURAN OR BENZOPYRAN) ALKYLAMINO]
ALKYL SUBSTITUTED GUANIDINES
The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula
the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein Xis O, C¾ or a direct bond; R1 is hydrogen or Ci-6alkyl; R2 is hydrogen, Ci -6alkyl, C3-6alkenyl or C3-6alkynyl; R3 is hydrogen or Ci-6alkyl; or R2 and R3 may be taken together to form a bivalent radical of formula -(CH2)m-, wherein m is 4 or 5; or R1 and R2 taken together may form a bivalent radical of formula -CH=CH- or of formula -(0¾)η-, wherein n is 2, 3 or 4; or R3 may represent a bond when R1 and R2 taken together form a bivalent radical of formula -CH=CH-CH=, -CH=CH-N=, or -CH=N-CH=; R4 is hydrogen or Ci-oalkyljAlk1 is a bivalent Ci-3alkanediyl radical; A is a bivalent radical of formula :
(a) (b) (c)
(d) (e)
wherein each R5 is hydrogen or Ci^alkyl; wherein each R6 is hydrogen or Ci_4alkyl; Alk2 is C2-i5alkanediyl or C5.7cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro- l,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.