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1. ZA1993/01404 - (BENZODIOXAN,BENZOFURAN OR BENZOPYRAN) ALKYLAMINO ALKYL SUBSTITUTED GUANIDINES

Office Afrique du Sud
Numéro de la demande 1993/01404
Date de la demande 26.02.1993
Numéro de publication 1993/01404
Date de publication 26.10.1994
Type de publication B
CIB
C07D
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
A61K
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
KPRÉPARATIONS À USAGE MÉDICAL, DENTAIRE OU POUR LA TOILETTE
CPC
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
A61P 9/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
C07D 307/81
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
78Benzo [b] furans; Hydrogenated benzo [b] furans
79with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals directly attached to carbon atoms of the hetero ring
81Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 311/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
58other than with oxygen or sulfur atoms in positions 2 or 4
Déposants JANSSEN PHARMACEUTICA N.V.
Inventeurs GUY ROSALIA EUGENE VAN LOMMEN
MARCEL FRANS LEOPOLD DE BRYUN
WALTER JACOBUS JOSEPH JANSSENS
Mandataires ADAMS & ADAMS
Données relatives à la priorité 842,560 27.02.1992 US
Titre
(EN) (BENZODIOXAN,BENZOFURAN OR BENZOPYRAN) ALKYLAMINO ALKYL SUBSTITUTED GUANIDINES
Abrégé
(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.