 Carboxyalkyl dipeptides and anti-hypertensive use thereof |
| We claim: 1. A compound represented by the formula ##STR12## and the pharmaceutically acceptable ... |
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| Optically active bicyclic imino-alpha-carboxylic esters |
| We claim: 1. A compound of the formulae Ia or Ib essentially free of its racemate, and salts of ... |
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| 5-HT.sub.3 receptor antagonists for treatment of cough and bronchoconstriction |
| I claim: 1. A method of treatment of cough and/or bronchoconstriction in mammals, which method ... |
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| Therapeutic compositions with enhanced bioavailability |
| OF THE INVENTION This invention relates to compositions of a drug with a water soluble polymer ... |
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| Medicament adsorbates and their preparation |
| In particular, it has been found that a good tasting medicament adsorbate is produced from ... |
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| Sustained release formulations |
| We claim: 1. In combination, a drug suitable for oral delivery and a delivery system for sustained ... |
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| Water dispersible gemfibrozil compositions |
| What is claimed is: 1. A water-dispersible formulation of gemfibrozil comprising finely divided ... |
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| Method and composition for enhancing the effect of indirect-acting sympathomimetic amines |
| OF SPECIFIC EMBODIMENTS In accordance with this invention, tyrosine or a tyrosine precursor such ... |
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| 1-azabicycloalkane derivatives, their preparation process and their use as medicaments |
| What is claimed is: 1. A compound of formula (I) ##STR5## in which n represents the number 1, R.sub.... |
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[(benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines
| Details |
Inventors: Van Lommen, Guy R. E.; De Bruyn, Marcel F. L.; Janssens, Walter J. J.;
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Primary Examiner: Gupta; Yogendra N.
Assistant Examiner:
Attorney, Agent or Firm: Metz; Charles J.
The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-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. |
|
DETAILED DESCRIPTION We claim: 1.
A compound of the formula: ##STR259## a pharmaceutically acceptable acid addition salt thereof, or a stereochemically isomeric form thereof, wherein: X is O, CH.
sub.
2 or a direct bond; R.
sup.
1 and R.
sup.
2 taken together form a bivalent radical of the formula --CH.
dbd.
CH-- or --(CH.
sub.
2).
sub.
n --, wherein n is 2, 3 or 4, and R.
sup.
3 represents hydrogen or C.
sub.
1-6 alkyl; or R.
sup.
1 and R.
sup.
2 taken together form a bivalent radical of the formula --CH.
dbd.
CH--CH.
dbd.
, --CH.
dbd.
CH--N.
dbd.
or --CH.
dbd.
N--CH.
dbd.
, and R.
sup.
3 represents a bond, wherein one or two hydrogen atoms in the bivalent radical --CH.
dbd.
CH--CH.
dbd.
, --CH.
dbd.
CH--N.
dbd.
or --CH.
dbd.
N--CH.
dbd.
can be replaced by halo, C.
sub.
1-6 alkyl, C.
sub.
1-6 alkyloxy, cyano, amino, mono- or di(C.
sub.
1-6 alkyl)amino, mono- or di(C.
sub.
3-6 cycloalkyl)amino, aminocarbonyl, C.
sub.
1-6 alkyloxycarbonylamino, or C.
sub.
1-6 alkylaminocarbonylamino; R.
sup.
4 is hydrogen or C.
sub.
1-6 alkyl; Alk.
sup.
1 is a bivalent C.
sub.
1-3 alkanediyl radical; A is a bivalent radical of the formula: ##STR260## wherein: each R.
sup.
5 is hydrogen or C.
sub.
1-4 alkyl; each R.
sup.
6 is hydrogen or C.
sub.
1-4 alkyl; Alk.
sup.
2 is C.
sub.
2-15 alkanediyl or C.
sub.
5-7 cycloalkanediyl; and each p is 0, 1 or 2; and R.
sup.
7 and R.
sup.
8 each independently are hydrogen, halo, C.
sub.
1-6 alkyl, C.
sub.
3-6 alkenyl, C.
sub.
3-6 alkynyl, hydroxy, C.
sub.
1-6 alkyloxy, cyano, aminoC.
sub.
1-6 alkyl, carboxyl, C.
sub.
1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, mono- or di (C.
sub.
1-6 alkyl)amino, or C.
sub.
1-6 alkylcarbonylamino.
2.
A compound according to claim 1 wherein Alk.
sup.
1 is CH.
sub.
2.
3.
A compound according to claim 1 wherein X is CH.
sub.
2 and wherein R.
sup.
7 and R.
sup.
8 each independently are hydrogen, halo, C.
sub.
1-6 alkyl, hydroxy, C.
sub.
1-6 alkyloxy, cyano, aminoC.
sub.
1-6 alkyl, nitro, amino, or C.
sub.
1-6 alkylcarbonylamino.
4.
A compound according to claim 2 wherein X is CH.
sub.
2 and wherein R.
sup.
7 and R.
sup.
8 each independently are hydrogen, halo, C
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Vasodialators 
