Organic nitrates, processes for their preparation and their use in the treatment of cardiovascular diseases

• Main Authors: DR GERHARD ZOLLER, DR MELITTA JUST, DR WOLFGANG KONING, DR BERND JABLONKA
• Format: Patent
• Language: English
• Published: 28.07.1993
• Edition: 5
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Organic nitrates, processes for preparing them as well as their use in the treatment of vascular diseases and especially in the treatment of angina. The said nitrates correspond to the following formula I: R-CO-(A)n-Y-B (I> in which: R represents especially a sulphur-containing residue and a sulphur-containing amino acid residue; A represents especially a CH2 group or a substituted amino acid; n is equal to 0 or 1 or greater than 1; Y represents an oxygen atom or an NH group and B represents especially a 1,4:3,6-dianhydrohexitol mononitrate, an -itol nitrate residue, and an inositol residue. The said organic nitrates are prepared by reacting: I. either a thioacid of the R-COOH type, in which R has the same meaning as above, with a derivative of the formula II: (A)n-Y-B, in which A, Y, B and n have the same meaning as above, II. or a derivative of formula III: R-CO-(A)n, in which R, A and n have the same meaning as above, with a derivative of formula Y-B, in which Y and B have the same meaning as above, in an appropriate solvent and under nonepimerising conditions.