Abstract: Compounds a formula (I) ##STR1## wherein the substituents and symbols have the meanings given in the specification, are new compounds with marked cardiovascular activity.
Type:
Grant
Filed:
January 22, 1993
Date of Patent:
January 3, 1995
Assignee:
Cedona Pharmaceuticals B.V.
Inventors:
Jan Bron, Geert J. Sterk, Hendrik Timmerman, Jan F. Van Der Werf
Abstract: A process is provided for preparing novel substituted or unsubstituted 4(5)-.omega.-aminoalkyl)imidazoles of the formula ##STR1## wherein n is 1 to 6, R.sub.1 is hydrogen or a linear, branched or cyclic, saturated or unsaturated alkyl group having 1-6 C-atoms or a phenyl ring being unsubstituted, or mono- or di-substituted with groups such as lower alkyl, halogen, alkoxy, methylenedioxy or a combination thereof, and R.sub.2 is hydrogen or methyl. The process comprises brominating an .omega.-phthalimidoalkan-2-one with bromine in anhydrous methanol to a 1- or 3-bromo-.omega.-phthalimido-alkan-2-one, subjecting said derivative to ring closure with an amidine in N.N-dimethylformamide with potassium carbonate under mild conditions followed by hydrolytic separation of the phthalic residue. Pharmaceutical compounds, compositions and a method of treatment are also provided.
Type:
Grant
Filed:
December 3, 1990
Date of Patent:
March 2, 1993
Assignee:
Cedona Pharmaceuticals B.V.
Inventors:
John C. Eriks, Henderikus van der Goot, Hendrik Timmerman, Jan G. Koper
Abstract: The invention relates to pharmaceutical compositions containing novel nitrate esters, of which it was found that they are useful for the treatment of ischemiatic heart diseases, decompensatio cordis, myocardial infarction and hypertension.
Type:
Grant
Filed:
September 14, 1989
Date of Patent:
September 17, 1991
Assignee:
Cedona Pharmaceuticals B.V.
Inventors:
Jan Bron, Geert J. Sterk, Jan F. van der Werf, Hendrik Timmerman
Abstract: N-(2-substituted alkyl)-N'[(imidazole-4-yl)alkylguanidines are provided by the reaction of a primary amine with benzoylisothiocyante to a benzoylthiourea derivative, followed by hydrolysis of this derivative to form the corresponding thiourea, converting this thiourea with methyliodide into an isothiourea and producing the desired compound by reaction of the isothiourea with aminopropylimidazole or aminoethylimidazole. The compound can be converted into an acid addition salt or the free compound obtained from such salt. The compounds are useful as the active ingredient in pharmaceutical compositions for the treatment of congestion, heart failure and some allergic conditions.
Type:
Grant
Filed:
November 23, 1988
Date of Patent:
April 23, 1991
Assignee:
Cedona Pharmaceuticals B.V.
Inventors:
Geert J. Sterk, Henk Timmerman, Henk van der Goot